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Vishwakarma A, Yadav H, Lakra P, Sulakhiya K, Paliwal R, Maiti S. Madhuca indica oil-entrapped buoyant galactomannan hydrogel microspheres for controlling epileptic seizures. Int J Biol Macromol 2024; 272:132739. [PMID: 38825290 DOI: 10.1016/j.ijbiomac.2024.132739] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/03/2024] [Revised: 05/20/2024] [Accepted: 05/27/2024] [Indexed: 06/04/2024]
Abstract
A stable Madhuca indica oil-in-water nanoemulsion (99-210 nm, zeta potential: > - 30 mV) was produced employing Tween 20 (surfactant) and Transcutol P (co-surfactant) (3:1). The nanoemulsion (oil: Smix = 3:7, 5:5, and 7:3) were subsequently incorporated into oxcarbazepine-loaded carboxymethylxanthan gum (DS = 1.23) dispersion. The hydrogel microspheres were formed using the ionic gelation process. Higher oil concentration had a considerable impact on particle size, drug entrapment efficiency, and buoyancy. The maximum 92 % drug entrapment efficiency was achieved with the microspheres having oil: Smix ratio 5:5. FESEM study revealed that the microspheres were spherical in shape and had an orange peel-like surface roughness. FTIR analysis revealed a hydrogen bonding interaction between drug and polymer. Thermal and x-ray examinations revealed the transformation of crystalline oxcarbazepine into an amorphous form. The microspheres had a buoyancy period of 7.5 h with corresponding release of around 83 % drug in 8 h in simulated stomach fluid, governed by supercase-II transport mechanism. In vivo neurobehavioral studies on PTZ-induced rats demonstrated that the microspheres outperformed drug suspension in terms of rotarod retention, number of crossings, and rearing activity in open field. Thus, Madhuca indica oil-in-water nanoemulsion-entrapped carboxymethyl xanthan gum microspheres appeared to be useful for monitoring oxcarbazepine release and managing epileptic seizures.
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Affiliation(s)
- Aman Vishwakarma
- Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, Madhya Pradesh 484887, India
| | - Harsh Yadav
- Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, Madhya Pradesh 484887, India
| | - Preeti Lakra
- Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, Madhya Pradesh 484887, India
| | - Kunjbihari Sulakhiya
- Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, Madhya Pradesh 484887, India
| | - Rishi Paliwal
- Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, Madhya Pradesh 484887, India
| | - Sabyasachi Maiti
- Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, Madhya Pradesh 484887, India.
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Soiklom S, Siri-anusornsak W, Petchpoung K, Kansandee W. Development of Anthocyanin-Rich Gel Beads from Colored Rice for Encapsulation and In Vitro Gastrointestinal Digestion. Molecules 2024; 29:270. [PMID: 38202851 PMCID: PMC10781165 DOI: 10.3390/molecules29010270] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Grants] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/14/2023] [Revised: 12/30/2023] [Accepted: 01/01/2024] [Indexed: 01/12/2024] Open
Abstract
Colored rice anthocyanins are water-soluble natural pigments that can be used as an active ingredient in healthy food and pharmaceutical products. However, anthocyanin utilization is limited because of its instability. This work produced anthocyanin-rich gel beads from colored rice using a modified ionotropic gelation technique for encapsulation, and their efficacy was studied in vitro in the gastrointestinal tract. In total, 15 colored rice samples of three types (whole grain rice, ground rice, and ground germinated rice) were screened to identify the highest anthocyanin content. The anthocyanin content of the whole grain rice was significantly (p < 0.05) higher than it was in the ground and ground germinated rice. The sample with the highest anthocyanin content (1062.7 µg/g) was the black glutinous rice grain from Phrae, chosen based on its anthocyanin-rich crude extract. A new formula using a modified ionotropic gelation technique was prepared for the inclusion of the extract in gel beads. The results indicated that the incorporation of oil and wax significantly increased the encapsulation efficiency of the gel beads (% EE value of 85.43%) and improved the bioavailability of the active ingredient. Moreover, after simulated digestion, the release of anthocyanin and total phenolic content occurred more than five times. Scanning electron microscopy revealed that the surface of the gel beads was smooth. Furthermore, the presence of polyphenols and polysaccharides in the gel beads was confirmed using FTIR. The oil-wax-incorporated, anthocyanin-rich gel beads could be implemented for antioxidant delivery into the gastrointestinal tract to further improve healthy food and nutraceutical products.
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Affiliation(s)
- Siriwan Soiklom
- Scientific Equipment and Research Division, Kasetsart University Research and Development Institute, Kasetsart University, Bangkok 10900, Thailand; (W.S.-a.); (K.P.); (W.K.)
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3
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Optimization and release characteristics of catechin-loaded calcium pectinate beads by internal gelation. Food Sci Biotechnol 2022; 31:1401-1409. [DOI: 10.1007/s10068-022-01126-8] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 03/14/2022] [Revised: 06/02/2022] [Accepted: 06/27/2022] [Indexed: 11/04/2022] Open
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Kaur M, Wadhwa A, Kumar V. Pectin-Based Nanomaterials: Synthesis, Toxicity and Applications. ASIAN JOURNAL OF CHEMISTRY 2021; 33:2579-2588. [DOI: 10.14233/ajchem.2021.23382] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Track Full Text] [Subscribe] [Scholar Register] [Indexed: 01/12/2025]
Abstract
Nanomaterials of biological origin are very useful for drug delivery applications. The stability,
biodegradability and biocompatibility of pectin nanomaterials in the human body make them an effective
drug carrier. This review focus on different aspect of synthesis, drug encapsulation, drug release and
safety of pectin-based nanomaterials. The nanomaterials can be used for the delivery of different
hydrophilic and hydrophobic drugs to various organs. The release kinetics of drug loaded pectin-based
nanoparticles can be studied in vitro as well as in vivo. The pectin-based nanomaterials have good
pharmaco-kinetics and can ensure controlled drug delivery. However, the toxicity of pectin-based
nanomaterials to human body needs to be evaluated carefully before industrial scale application.
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Affiliation(s)
- Mandeep Kaur
- Department of Biotechnology, School of Bioengineering and Biosciences, Lovely Professional University, Phagwara-144111, India
| | - Aditya Wadhwa
- Department of Biotechnology, School of Bioengineering and Biosciences, Lovely Professional University, Phagwara-144111, India
| | - Vineet Kumar
- Department of Biotechnology, School of Bioengineering and Biosciences, Lovely Professional University, Phagwara-144111, India
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6
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Wahba MI. Calcium pectinate-agar beads as improved carriers for β-d-galactosidase and their thermodynamics investigation. 3 Biotech 2020; 10:356. [PMID: 32766097 DOI: 10.1007/s13205-020-02341-y] [Citation(s) in RCA: 5] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/12/2020] [Accepted: 07/12/2020] [Indexed: 05/20/2025] Open
Abstract
Polyethyleneimine (PEI) glutaraldehyde-refined calcium pectinate (CaP)-agar beads were presented as improved covalent immobilization matrices. The CaP-agar beads exhibited incremented mechanical stability which facilitated their handling. The beads' concoction and activation processes were honed using the Box-Behnken design which recommended utilizing 5.4% agar, and a 2.95% PEI solution of pH 8.67. The honed CaP-agar beads established a more efficient ionic interaction with PEI which enabled the immobilization of more enzyme while utilizing less PEI than that required to activate the neat CaP beads. Furthermore, the activated CaP-agar beads granted superior operational stability to the immobilized enzyme, β-d-galactosidase (βgal), where it preserved 86.84 ± 0.37% of its precursive activity during its thirteenth reusability round. The CaP-agar immobilized βgal (iβgal) also showed incremented storage stability where it preserved 85.05 ± 3.32% of its precursive activity after 38 days of storage. The thermal stability of the iβgal was shown to be superior to that of the free enzyme as the iβgal exhibited incremented thermodynamic parameters, such as the t 1/2 values, the D values, the thermal denaturation activation energy, the enthalpies, and the Gibb's free energies. The βgal's immobilization onto the activated CaP-agar beads also shifted the enzyme's optimal pH from 4.6-5.1 to 3.3-4.9, whereas its optimal temperature was retained at 55 °C. The procured biocatalyst was exploited to efficiently hydrolyze the lactose in whey permeate.
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7
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Optimized Ellagic Acid-Ca Pectinate Floating Beads for Gastroprotection against Indomethacin-Induced Gastric Injury in Rats. Biomolecules 2020; 10:biom10071006. [PMID: 32640741 PMCID: PMC7408148 DOI: 10.3390/biom10071006] [Citation(s) in RCA: 5] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/17/2020] [Revised: 06/23/2020] [Accepted: 07/01/2020] [Indexed: 01/18/2023] Open
Abstract
A peptic ulcer is an alimentary tract injury that leads to a mucosal defect reaching the submucosa. This work aimed to optimize and maximize ellagic acid (EA) loading in Ca pectinate floating beads to maximize the release for 24 h. Three factors were selected: Ca pectinate concentration (X1, 1–3 w/v %), EA concentration (X2, 1–3 w/v %) and the dropping time (X3, 10–30 min). The factorial design proposed eight formulations. The optimized EA–Ca pectinate formulation was evaluated for the gastric ulcer index and the oxidative stress parameter determination of gastric mucosa. The results indicated that the optimum EA–Ca pectinate formula significantly improved the gastric ulcer index in comparison with raw EA. The protective effect of the optimized EA–Ca pectinate formula was further indicated by the histopathological features of the stomach. The results of the study indicate that an EA formulation in the form of Ca pectinate beads would be effective for protection against gastric ulcers because of Nonsteroidal anti-inflammatory drugs (NSAID) administration.
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Ibrahim M, Sarhan HA, Naguib YW, Abdelkader H. Design, characterization and in vivo evaluation of modified release baclofen floating coated beads. Int J Pharm 2020; 582:119344. [DOI: 10.1016/j.ijpharm.2020.119344] [Citation(s) in RCA: 5] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/26/2019] [Revised: 04/13/2020] [Accepted: 04/15/2020] [Indexed: 11/16/2022]
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Kevadiya BD, Chen L, Zhang L, Thomas MB, Davé RN. Fenofibrate Nanocrystal Composite Microparticles for Intestine-Specific Oral Drug Delivery System. Pharmaceuticals (Basel) 2019; 12:E109. [PMID: 31315263 PMCID: PMC6789785 DOI: 10.3390/ph12030109] [Citation(s) in RCA: 7] [Impact Index Per Article: 1.2] [Reference Citation Analysis] [Abstract] [Key Words] [Grants] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/16/2019] [Revised: 07/09/2019] [Accepted: 07/10/2019] [Indexed: 11/16/2022] Open
Abstract
Hydrophobic drug nanocrystals (NCs) manufactured by particle engineering have been extensively investigated for enhanced oral bioavailability and therapeutic effectiveness. However, there are significant drawbacks, including fast dissolution of the nanocrystals in the gastric environment, leading to physicochemical instability. To solves this issue, we developed an innovative technique that involves the encapsulation of nanocrystals in composite spherical microparticles (NCSMs). Fenofibrate (FNB) NCs (FNB-NCs) manufactured by a wet stirred media milling (WSMM) technique and an ionotropic crosslinking method were used for FNB-NC encapsulation within gastroresistant NCSMs. Various solid-state methods were used for characterizing NCSMs. The pH-sensitive NCSMs showed a site-specific release pattern at alkaline pH and nearly 0% release at low pH (gastric environment). This phenomenon was confirmed by a real-time in situ UV-imaging system known as the surface dissolution imager (SDI), which was used to monitor drug release events by measuring the color intensity and concentration gradient formation. All these results proved that our NCSM approach is an innovative idea in oral drug delivery systems, as it resolves significant challenges in the intestine-specific release of hydrophobic drugs while avoiding fast dissolution or burst release.
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Affiliation(s)
- Bhavesh D Kevadiya
- New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Warren Street, Newark, NJ 07102, USA.
| | - Liang Chen
- New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Warren Street, Newark, NJ 07102, USA
| | - Lu Zhang
- New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Warren Street, Newark, NJ 07102, USA
| | - Midhun B Thomas
- Pandorum Technologies Pvt Ltd, Bangalore Bioinnovation Centre, Helix Biotech Park, Electronic City Phase 1, Bangalore, Karnataka 560100, India
| | - Rajesh N Davé
- New Jersey Center for Engineered Particulates, New Jersey Institute of Technology, Warren Street, Newark, NJ 07102, USA.
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Treesinchai S, Puttipipatkhachorn S, Pitaksuteepong T, Sungthongjeen S. Development of curcumin floating beads with low density materials and solubilizers. J Drug Deliv Sci Technol 2019. [DOI: 10.1016/j.jddst.2019.03.002] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.2] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/11/2023]
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Devi P, Rathor S, Sharma P, Sen J, Kaur H, Singh J. Development of novel gastroretentive salbutamol sulfate-loaded sodium alginate-pectin bubble beads prepared by co-axial needle air-injection method and in vivo clinical evaluation by ultrasound studies. Eur J Pharm Sci 2018; 122:359-373. [PMID: 30017846 DOI: 10.1016/j.ejps.2018.07.019] [Citation(s) in RCA: 4] [Impact Index Per Article: 0.6] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/28/2018] [Revised: 06/22/2018] [Accepted: 07/06/2018] [Indexed: 11/28/2022]
Abstract
In the present study, the salbutamol sulfate-loaded sodium alginate-pectin (SS-loaded SA-PEC) bubble beads have been optimized and evaluated for drug loading, in vitro drug release, in vivo floating behavior in the stomach, etc. Nine batches (F1-F9) of bubble beads with different SA and PEC contents were prepared by novel co-axial needle air-injection method and related to their percent drug loading efficiency (%DLE) and percent drug release at 4 h (%R4h) as response factors. The multivariate analysis has shown the effect of SA/PEC ratio, total polymer content, as well as their interaction on %DLE and %R4h. In the quantitative modeling, the satisfactory adjustment of the linear models (along with interaction terms) with the experimental data for both %DLE and %R4h has confirmed the findings of the multivariate analysis. The optimized SS-loaded SA-PEC bubble beads based on 2D (contours), 3D, desirability, and overlay plots has exhibited %DLE of 87.35 ± 2.48% (n = 3 and error = 2.94%) and %R4h of 85.79 ± 2.98% (n = 3 and error = 0.25%). The in vitro drug release studies have shown almost complete (≥85%) SS release from all the batches within 4-6 h in simulated gastric fluid (SGF) pH 1.2. The in vivo clinical findings by ultrasound studies have shown excellent floatation (>6 h) behavior of bubble beads in the upper gastrointestinal tract (GIT) and efficient stomach-specific gastroretention.
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Affiliation(s)
- Pooja Devi
- College of Pharmacy, PGIMS, University of Health Sciences, Rohtak 124001, Haryana, India
| | - Sandeep Rathor
- College of Pharmacy, PGIMS, University of Health Sciences, Rohtak 124001, Haryana, India
| | - Pratibha Sharma
- College of Pharmacy, PGIMS, University of Health Sciences, Rohtak 124001, Haryana, India
| | - Jyotsna Sen
- Department of Radiodiagnosis, PGIMS, University of Health Sciences, Rohtak 124001, Haryana, India
| | - Harmeet Kaur
- Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak 124001, Haryana, India
| | - Jasbir Singh
- College of Pharmacy, PGIMS, University of Health Sciences, Rohtak 124001, Haryana, India.
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Bera H, Kumar S. Diethanolamine-modified pectin based core-shell composites as dual working gastroretentive drug-cargo. Int J Biol Macromol 2018; 108:1053-1062. [DOI: 10.1016/j.ijbiomac.2017.11.019] [Citation(s) in RCA: 7] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 09/07/2017] [Revised: 11/03/2017] [Accepted: 11/05/2017] [Indexed: 10/18/2022]
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13
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Cheewatanakornkool K, Niratisai S, Manchun S, Dass CR, Sriamornsak P. Characterization and in vitro release studies of oral microbeads containing thiolated pectin-doxorubicin conjugates for colorectal cancer treatment. Asian J Pharm Sci 2017; 12:509-520. [PMID: 32104364 PMCID: PMC7032137 DOI: 10.1016/j.ajps.2017.07.005] [Citation(s) in RCA: 31] [Impact Index Per Article: 3.9] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/15/2017] [Accepted: 07/06/2017] [Indexed: 12/20/2022] Open
Abstract
Novel oral microbeads were developed based on a biopolymer-drug conjugate of doxorubicin (DOX) conjugated with thiolated pectin via reducible disulfide bonds. The microbeads were fabricated by ionotropic gelation with cations such as Al3+, Ca2+ and Zn2+. The results showed that using zinc acetate can produce the strongest microbeads with spherical shape. However, the microbeads prepared from thiolated pectin-DOX conjugate were very soft and irregular in shape. To produce more spherical microbeads with suitable strength, the native pectin was then added to the formulations. The particle size of the microbeads ranged from 0.87 to 1.14 mm. The morphology of the microbeads was characterized by optical and scanning electron microscopy. DOX was still in crystalline form when used in preparing the microbeads, as confirmed by powder X-ray diffractometry. Drug release profiles showed that the microbeads containing thiolated pectin-DOX conjugate exhibited reduction-responsive character; in reducing environments, the thiolated pectin-DOX conjugate could uncouple resulting from a cleavage of the disulfide linkers and consequently release the DOX. The best-fit release kinetics of the microbeads containing thiolated pectin-DOX conjugate, in the medium without reducing agent, fit the Korsmeyer-Peppas model while those in the medium with reducing agent fit a zero-order release model. These results suggested that the microbeads containing thiolated pectin-DOX conjugate may be a promising platform for cancer-targeted delivery of DOX, exploiting the reducing environment typically found in tumors.
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Affiliation(s)
- Kamonrak Cheewatanakornkool
- Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand
- Pharmaceutical Biopolymer Group (PBiG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand
| | - Sathit Niratisai
- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand
| | - Somkamol Manchun
- Pharmaceutical Biopolymer Group (PBiG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand
- Thailand Institute of Scientific and Technological Research, Klong Luang, Pathum Thani 12120, Thailand
| | - Crispin R. Dass
- School of Pharmacy, Faculty of Health Sciences, Curtin University, Perth, WA 6845, Australia
- Curtin Health Institute for Research Innovation, Curtin University, Perth, WA 6845, Australia
| | - Pornsak Sriamornsak
- Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand
- Pharmaceutical Biopolymer Group (PBiG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand
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Bera H, Nadimpalli J, Kumar S, Vengala P. Kondogogu gum-Zn+2-pectinate emulgel matrices reinforced with mesoporous silica for intragastric furbiprofen delivery. Int J Biol Macromol 2017; 104:1229-1237. [DOI: 10.1016/j.ijbiomac.2017.07.027] [Citation(s) in RCA: 17] [Impact Index Per Article: 2.1] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/13/2017] [Revised: 05/28/2017] [Accepted: 07/04/2017] [Indexed: 10/19/2022]
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Chitosan-glutaraldehyde activated calcium pectinate beads as a covalent immobilization support. BIOCATALYSIS AND AGRICULTURAL BIOTECHNOLOGY 2017. [DOI: 10.1016/j.bcab.2017.10.016] [Citation(s) in RCA: 13] [Impact Index Per Article: 1.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/17/2022]
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16
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Çakır B, Gülseren İ. Dissolution kinetics of polyphenol bearing calcium pectate hydrogels in simulated gastric or intestinal media and their anti-carcinogenic capacities. Food Hydrocoll 2017. [DOI: 10.1016/j.foodhyd.2017.03.026] [Citation(s) in RCA: 5] [Impact Index Per Article: 0.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/26/2022]
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17
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Xing P, Shi Y, Dong C, Liu H, Cheng Y, Sun J, Li D, Li M, Sun K, Feng D. Colon-Targeted Delivery of IgY Against Clostridium difficile Toxin A and B by Encapsulation in Chitosan-Ca Pectinate Microbeads. AAPS PharmSciTech 2017; 18:1095-1103. [PMID: 27826799 DOI: 10.1208/s12249-016-0656-2] [Citation(s) in RCA: 17] [Impact Index Per Article: 2.1] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/14/2016] [Accepted: 10/26/2016] [Indexed: 12/18/2022] Open
Abstract
This study investigated the use of a newly developed chitosan-Ca pectinate microbead formulation for the colon-targeted delivery of anti-A/B toxin immunoglobulin of egg yolk (IgY) to inhibit toxin binding to colon mucosa cells. The effect of the three components (pectinate, calcium chloride, and chitosan) used for the microbead production was examined with the aim of identifying the optimal levels to improve drug encapsulation efficiency, swelling ratio, and cumulative IgY release rate. The optimized IgY-loaded bead component was pectin 5% (w/v), CaCl2 3% (w/v), and chitosan 0.5% (w/v). Formulated beads were spherical with 1.2-mm diameter, and the drug loading was 45%. An in vitro release study revealed that chitosan-Ca pectinate microbeads inhibited IgY release in the upper gastrointestinal tract and significantly improved the site-specific release of IgY in the colon. An in vivo rat study demonstrated that 72.6% of biologically active IgY was released specifically in the colon. These results demonstrated that anti-A/B toxin IgY-loaded chitosan-Ca pectinate oral microbeads improved IgY release behavior in vivo, which could be used as an effective oral delivery platform for the biological treatment of Clostridium difficile infection (CDI).
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Kim ES, Lee JS, Lee HG. Calcium-alginate microparticles for sustained release of catechin prepared via an emulsion gelation technique. Food Sci Biotechnol 2016; 25:1337-1343. [PMID: 30263414 DOI: 10.1007/s10068-016-0210-8] [Citation(s) in RCA: 25] [Impact Index Per Article: 2.8] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/30/2015] [Revised: 08/07/2016] [Accepted: 08/08/2016] [Indexed: 11/29/2022] Open
Abstract
Catechin-loaded Ca-alginate beads and microparticles were prepared by an emulsion gelation method using sunflower oil for efficient sustained release of catechin. The emulsion was prepared by sequential mixing of alginate, oil, and oleic acid ester as an emulsifier. Encapsulation efficiency (EE) and inhibition of catechin release of the beads were significantly increased approximately to 453.83 and 148.71% by the emulsion gelation technique, respectively (p<0.05). For the microparticles, the highest inhibition of catechin release after 1 h of incubation (78.82%) was observed at the microparticles prepared by 5% (w/w) oil, 3% (w/w) alginate, 4% (w/v) CaCl2, and 200 mg catechin with the most hydrophilic emulsifier, decaglycerol mono-ester. Moreover, the catechin release was sustained at acidic conditions and increased with increase in pH of release medium. These results suggest that catechin encapsulation within Ca-alginate particles by emulsion gelation method can be an effective delivery system for catechin.
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Affiliation(s)
- Eun Suh Kim
- Department of Food and Nutrition, Hanyang University, Seoul, 04763 Korea
| | - Ji-Soo Lee
- Department of Food and Nutrition, Hanyang University, Seoul, 04763 Korea
| | - Hyeon Gyu Lee
- Department of Food and Nutrition, Hanyang University, Seoul, 04763 Korea
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Wahba MI. Treated calcium pectinate beads for the covalent immobilization of β- d -galactosidase. Int J Biol Macromol 2016; 91:877-86. [DOI: 10.1016/j.ijbiomac.2016.06.044] [Citation(s) in RCA: 29] [Impact Index Per Article: 3.2] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/28/2016] [Revised: 06/09/2016] [Accepted: 06/13/2016] [Indexed: 10/21/2022]
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Dey SK, De PK, De A, Ojha S, De R, Mukhopadhyay AK, Samanta A. Floating mucoadhesive alginate beads of amoxicillin trihydrate: A facile approach for H. pylori eradication. Int J Biol Macromol 2016; 89:622-31. [PMID: 27177460 DOI: 10.1016/j.ijbiomac.2016.05.027] [Citation(s) in RCA: 24] [Impact Index Per Article: 2.7] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/25/2016] [Revised: 05/03/2016] [Accepted: 05/08/2016] [Indexed: 12/13/2022]
Abstract
This study investigates the design of sunflower oil entrapped floating and mucoadhesive beads of amoxicillin trihydrate using sodium alginate and hydroxypropyl methylcellulose as matrix polymers and chitosan as coating polymer to localize the antibiotic at the stomach site against Helicobacter pylori. Beads prepared by ionotropic gellation technique were evaluated for different physicochemical, in-vitro and in-vivo properties. Beads of all batches were floated for >24h with a maximum lag time of 46.3±3.2s. Scanning electron microscopy revealed that the beads were spherical in shape with few oil filled channels distributed throughout the surfaces and small pocket structures inside the matrix confirming oil entrapment. Prepared beads showed good mucoadhesiveness of 75.7±3.0% to 85.0±5.5%. The drug release profile was best fitted to Higuchi model with non fickian driven mechanism. The optimized batch showed 100% Helicobacter pylori growth inhibition in 15h in in-vitro culture. Furthermore, X-ray study in rabbit stomach confirmed the gastric retention of optimized formulation. The results exhibited that formulated beads may be preferred to localize the antibiotic in the gastric region to allow more availability of antibiotic at gastric mucus layer acting on Helicobacter pylori, thereby improving the therapeutic efficacy.
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Affiliation(s)
- Sanjoy Kumar Dey
- Division of Microbiology, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India
| | - Pintu Kumar De
- Department of Pharmaceutics, Dr. B. C. Roy College of Pharmacy and Allied Health Sciences, Bidhan Nagar, Durgapur 713206, India
| | - Arnab De
- Division of Microbiology, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India
| | - Souvik Ojha
- Department of Pharmaceutics, Dr. B. C. Roy College of Pharmacy and Allied Health Sciences, Bidhan Nagar, Durgapur 713206, India
| | - Ronita De
- Division of Bacteriology, National Institute of Cholera and Enteric Diseases, Beleghata, Kolkata 700010, India
| | - Asish Kumar Mukhopadhyay
- Division of Bacteriology, National Institute of Cholera and Enteric Diseases, Beleghata, Kolkata 700010, India
| | - Amalesh Samanta
- Division of Microbiology, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
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Soradech S, Petchtubtim I, Thongdon-A J, Muangman T. Development of Wax-Incorporated Emulsion Gel Beads for the Encapsulation and Intragastric Floating Delivery of the Active Antioxidant from Tamarindus indica L. Molecules 2016; 21:380. [PMID: 27011162 PMCID: PMC6273378 DOI: 10.3390/molecules21030380] [Citation(s) in RCA: 5] [Impact Index Per Article: 0.6] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/12/2016] [Revised: 03/03/2016] [Accepted: 03/16/2016] [Indexed: 12/05/2022] Open
Abstract
In this study, tamarind (Tamarindus indica L.) seed extracts with potential antioxidant activity and toxicity to cancer cells were developed as functional foods and nutraceutical ingredients in the form of emulsion gel beads. Three extracts were obtained from ethanol and water: TSCH50, TSCH95 and TSCH. All extracts exhibited high potential for superoxide anion scavenging activity over the IC50 range < 5–11 µg/mL and had no toxic effects on normal cells, however, the water extract (TSCH) was the most effective due to its free radical scavenging activity and toxicity in mitochondrial membranes of cancer cells. Next a study was designed to develop a new formulation for encapsulation and intragastric floating delivery of tamarind seed extract (TSCH) using wax-incorporated emulsion gel beads, which were prepared using a modified ionotropic gelation technique. Tamarind seed extract at 1% (w/w) was used as the active ingredient in all formulations. The effect of the types and amounts of wax on the encapsulation efficiency and percentage of the active release of alginate gel beads was also investigated. The results demonstrated that the incorporation of both waxes into the gel beads had an effect on the percentage of encapsulation efficiency (%) and the percentage of the active ingredient release. Furthermore, the addition of water insoluble waxes (carnauba and bee wax) significantly retarded the release of the active ingredient. The addition of both waxes had a slight effect on drug release behavior. Nevertheless, the increase in incorporated waxes in all formulations could sustain the percentage of active ingredient release. In conclusion, wax-incorporated emulsion gel beads using a modified ionotropic gelation technique could be applied for the intragastric floating delivery and controlled release of functional food and nutraceutical products for their antioxidant and anticancer capacity.
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Affiliation(s)
- Sitthiphong Soradech
- Department of Pharmaceuticals and Natural Products, Thailand Institute of Scientific and Technological Research, Pathum Thani 12120, Thailand.
| | - Intira Petchtubtim
- Department of Pharmaceuticals and Natural Products, Thailand Institute of Scientific and Technological Research, Pathum Thani 12120, Thailand.
| | - Jeerayu Thongdon-A
- Department of Pharmaceuticals and Natural Products, Thailand Institute of Scientific and Technological Research, Pathum Thani 12120, Thailand.
| | - Thanchanok Muangman
- Department of Pharmaceuticals and Natural Products, Thailand Institute of Scientific and Technological Research, Pathum Thani 12120, Thailand.
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Soltani S, Madadlou A. Two-step sequential cross-linking of sugar beet pectin for transforming zein nanoparticle-based Pickering emulsions to emulgels. Carbohydr Polym 2016; 136:738-43. [DOI: 10.1016/j.carbpol.2015.09.100] [Citation(s) in RCA: 57] [Impact Index Per Article: 6.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 06/24/2015] [Revised: 08/31/2015] [Accepted: 09/26/2015] [Indexed: 11/25/2022]
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Gupta A, Tiwari G, Tiwari R, Srivastava R. Factorial designed 5-fluorouracil-loaded microsponges and calcium pectinate beads plugged in hydroxypropyl methylcellulose capsules for colorectal cancer. Int J Pharm Investig 2015; 5:234-46. [PMID: 26682194 PMCID: PMC4675005 DOI: 10.4103/2230-973x.167688] [Citation(s) in RCA: 18] [Impact Index Per Article: 1.8] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/04/2022] Open
Abstract
INTRODUCTION The work was aimed to develop an enteric-coated hydroxypropyl methylcellulose (HPMC) capsules (ECHC) plugged with 5-fluorouracil (5-FU)-loaded microsponges in combination with calcium pectinate beads. MATERIALS AND METHODS The modified quasi-emulsion solvent diffusion method was used to prepare microsponges. A 3(2) factorial design was employed to study the formulation and the effects of independent variables (volume of organic solvent and Eudragit-RS100 content) on dependent variables (particle size, %entrapment efficiency, and %cumulative drug release). The optimized microsponge (F4) was characterized by scanning electron microscopy, powder X-ray diffraction, and thermogravimetric analysis. F4 was plugged along with the calcium pectinate beads in HPMC capsules coated with enteric polymer Eudragit-L100 (Ed-L100) and/or Eudragit-S100 (Ed-S100) in different proportions. An in vitro release study of ECHC was performed in simulated gastric fluid for 2 h, followed by simulated intestinal fluid for next 6 h and then in simulated colonic fluid (in the presence and absence of pectinase enzyme for further 16 h). The optimized formulation was subjected to in vivo roentgenographic and pharmacokinetic studies in New Zealand white rabbits to analyze the in vivo behavior of the developed colon-targeted capsules. RESULTS Drug release was retarded on coating with Ed-S100 in comparison to a blend of Ed-S100:Ed-L100 coating. The percentage of 5-FU released at the end of 24 h from ECHC3 was 97.83 ± 0.12% in the presence of pectinase whereas in the control study, it was 40.08 ± 0.02%. CONCLUSION Thus, enteric-coated HPMC capsules plugged with 5-FU-loaded microsponges and calcium pectinate beads proved to be a promising dosage form for colon targeting.
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Affiliation(s)
- Ankita Gupta
- Department of Pharmaceutics, Pranveer Singh Institute of Technology, Bhauti, Kanpur, Uttar Pradesh, India
| | - Gaurav Tiwari
- Department of Pharmaceutics, Pranveer Singh Institute of Technology, Bhauti, Kanpur, Uttar Pradesh, India
| | - Ruchi Tiwari
- Department of Pharmaceutics, Pranveer Singh Institute of Technology, Bhauti, Kanpur, Uttar Pradesh, India
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Gupta A, Tiwari G, Tiwari R, Srivastava R, Rai AK. Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer. BRAZ J PHARM SCI 2015. [DOI: 10.1590/s1984-82502015000300011] [Citation(s) in RCA: 13] [Impact Index Per Article: 1.3] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/21/2022] Open
Abstract
The work was aimed at developing novel enteric coated HPMC capsules (ECHC) plugged with 5 Florouracil (5-FU) loaded Microsponges in combination with calcium pectinate beads. Modified quasi-emulsion solvent diffusion method was used to formulate microsponges based on 32 factorial design and the effects of independent variables (volume of organic solvent and Eudragit RS100 content) on the dependent variables (Particle size, %EE & % CDR) were determined. The optimized microsponges (F4) were characterized by SEM, PXRD, TGA and were plugged along with calcium pectinate beads in HPMC capsules and the HPMC capsules were further coated with enteric polymer Eudragit L 100 (Ed-L100) and/ or Eudrgit S 100 (Ed-S 100) in different proportions. In vitro release study of ECHC was performed in various release media sequentially SGF for 2 h, followed by SIF for the next 6 h and then in SCF (in the presence and absence of pectinase enzyme for further 16 h). Drug release was retarded on coating with EdS-100 in comparison to blend of EdS-100: EdL-100 coating. The percentage of 5-FU released at the end of 24 h from ECHC 3 was 97.83 ± 0.12% in the presence of pectinase whereas in control study it was 40.08 ± 0.02% drug. The optimized formulation was subjected to in vivo Roentgenographic studies in New Zealand white rabbits to analyze the in vivo behavior of the developed colon targeted capsules. Pharmacokinetic studies in New Zealand white rabbits were conducted to determine the extent of systemic exposure provided by the developed formulation in comparison to 5-FU aqueous solutions. Thus, enteric coated HPMC capsules plugged with 5-FU loaded microsponges and calcium pectinate beads proved to be promising dosage form for colon targeted drug delivery to treat colorectal cancer.
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Affiliation(s)
| | | | | | | | - A. K. Rai
- Pranveer Singh Institute of Technology, India
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Aoki H, Iwao Y, Mizoguchi M, Noguchi S, Itai S. Clarithromycin highly-loaded gastro-floating fine granules prepared by high-shear melt granulation can enhance the efficacy of Helicobacter pylori eradication. Eur J Pharm Biopharm 2015; 92:22-7. [DOI: 10.1016/j.ejpb.2015.02.012] [Citation(s) in RCA: 13] [Impact Index Per Article: 1.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 12/24/2014] [Revised: 02/05/2015] [Accepted: 02/09/2015] [Indexed: 11/30/2022]
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Abourehab MAS, Khaled KA, Sarhan HAA, Ahmed OAA. Evaluation of combined famotidine with quercetin for the treatment of peptic ulcer: in vivo animal study. DRUG DESIGN DEVELOPMENT AND THERAPY 2015; 9:2159-69. [PMID: 25926722 PMCID: PMC4403742 DOI: 10.2147/dddt.s81109] [Citation(s) in RCA: 13] [Impact Index Per Article: 1.3] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Subscribe] [Scholar Register] [Indexed: 01/11/2023]
Abstract
The aim of this work was to prepare a combined drug dosage form of famotidine (FAM) and quercetin (QRT) to augment treatment of gastric ulcer. FAM was prepared as freeze-dried floating alginate beads using ion gelation method and then coated with Eudragit RL100 to sustain FAM release. QRT was prepared as solid dispersion with polyvinyl pyrrolidone K30 to improve its solubility. Photo images and scanning electron microscope images of the prepared beads were carried out to detect floating behavior and to reveal surface and core shape of the prepared beads. Anti-ulcerogenic effect and histopathological examination of gastric tissues were carried out to investigate the effect of the combined drug formulation compared with commercial FAM tablets and FAM beads. Gastric glutathione (GSH), superoxide dismutase, catalase, tissue myeloperoxidase, and lipid peroxidation enzyme activities and levels in rat stomach tissues were also determined. Results revealed that spherical beads were formed with an average diameter of 1.64±0.33 mm. They floated immediately with no lag time before floating, and remained buoyant throughout the test period. Treatment with a combination of FAM beads plus QRT showed the absence of any signs of inflammation or hemorrhage, and significantly prevented the indomethacin-induced decrease in GSH levels (P<0.05) with regain of normal GSH gastric tissue levels. Also, there was a significant difference in the decrease of malondialdehyde level compared to FAM commercial tablets or beads alone (P<0.05). The combined formula significantly improved the myeloperoxidase level compared to both the disease control group and commercial FAM tablet-treated group (P<0.05). Formulation of FAM as floating beads in combination with solid dispersion of QRT improved the anti-ulcer activity compared to commercially available tablets, which reveals a promising application for treatment of peptic ulcer.
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Affiliation(s)
- Mohammed A S Abourehab
- Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt ; Department of Pharmaceutics, Faculty of Pharmacy, Umm Al-Qura University, Makkah, Saudi Arabia
| | - Khaled A Khaled
- Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt
| | - Hatem A A Sarhan
- Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt
| | - Osama A A Ahmed
- Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, Egypt ; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia
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Kaushik AY, Tiwari AK, Gaur A. Role of excipients and polymeric advancements in preparation of floating drug delivery systems. Int J Pharm Investig 2015; 5:1-12. [PMID: 25599027 PMCID: PMC4286829 DOI: 10.4103/2230-973x.147219] [Citation(s) in RCA: 27] [Impact Index Per Article: 2.7] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 01/08/2023] Open
Abstract
Since decade or two, the development of floating drug delivery systems becomes a significant and novel tool as having low density than gastric content. There are various advanced polymers including chitosan, eudragit, etc., and excipients such as; pore forming agent, surfactants, etc. All of them are discussed briefly, and results are concluded from various reputed researches. We have discussed all natural and synthetic systems with their effect on the release and other parameters which are essential for the floating formulation development.
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Affiliation(s)
- Avinash Y Kaushik
- Department of Pharmaceutics, School of Pharmaceutical Sciences, Jaipur National University, Jaipur, India
| | - Ajay K Tiwari
- Department of Pharmaceutics, School of Pharmaceutical Sciences, Jaipur National University, Jaipur, India
| | - Ajay Gaur
- Department of Pharmaceutics, Lachoo Memorial College of Science and Technology, Jodhpur, Rajasthan, India
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Zhao S, Lv Y, Zhang JB, Wang B, Lv GJ, Ma XJ. Gastroretentive drug delivery systems for the treatment of Helicobacter pylori. World J Gastroenterol 2014; 20:9321-9. [PMID: 25071326 PMCID: PMC4110563 DOI: 10.3748/wjg.v20.i28.9321] [Citation(s) in RCA: 5] [Impact Index Per Article: 0.5] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 11/01/2013] [Revised: 03/04/2014] [Accepted: 04/15/2014] [Indexed: 02/07/2023] Open
Abstract
Helicobacter pylori (H. pylori) is one of the most common pathogenic bacterial infections and is found in the stomachs of approximately half of the world's population. It is the primary known cause of gastritis, gastroduodenal ulcer disease and gastric cancer. However, combined drug therapy as the general treatment in the clinic, the rise of antibiotic-resistant bacteria, adverse reactions and poor patient compliance are major obstacles to the eradication of H. pylori. Oral site-specific drug delivery systems that could increase the longevity of the treatment agent at the target site might improve the therapeutic effect and avoid side effects. Gastroretentive drug delivery systems potentially prolong the gastric retention time and controlled/sustained release of a drug, thereby increasing the concentration of the drug at the application site, potentially improving its bioavailability and reducing the necessary dosage. Recommended gastroretentive drug delivery systems for enhancing local drug delivery include floating systems, bioadhesive systems and expandable systems. In this review, we summarize the important physiological parameters of the gastrointestinal tract that affect the gastric residence time. We then focus on various aspects useful in the development of gastroretentive drug delivery systems, including current trends and the progress of novel forms, especially with respect to their application for the treatment of H. pylori infections.
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Taranalli SS, Dandagi PM, Mastiholimath VS. Development of hollow/porous floating beads of metoprolol for pulsatile drug delivery. Eur J Drug Metab Pharmacokinet 2014; 40:225-33. [DOI: 10.1007/s13318-014-0194-9] [Citation(s) in RCA: 5] [Impact Index Per Article: 0.5] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/24/2013] [Accepted: 03/25/2014] [Indexed: 02/03/2023]
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Ketorolac tromethamine floating beads for oral application: Characterization and in vitro/in vivo evaluation. Saudi Pharm J 2013; 22:349-59. [PMID: 25161380 DOI: 10.1016/j.jsps.2013.06.006] [Citation(s) in RCA: 12] [Impact Index Per Article: 1.0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 05/29/2013] [Accepted: 06/23/2013] [Indexed: 11/21/2022] Open
Abstract
The floating beads have been employed to make a sustained release of the drug in the stomach and to decrease the dose of the drug and hence overcome its side effects. The common benefits of the floating beads were it is easy preparation, without the need of a high temperature, and high percentage of the drug entrapment. In the present work, the Ketorolac tromethamine (KT) floating beads were prepared by extrusion congealing method utilizing calcium carbonate as a gas forming agent. The physical characters of the produced beads were investigated such as KT yield, KT loading, and entrapment efficiency of the drug. In addition, floating behavior, swelling, particle size, morphology and KT stability were also evaluated. In vitro drug release study was carried out, and the kinetics of the release was evaluated using the linear regression method. Furthermore, the in vivo analgesic effect of KT after oral administration of the selected formula of floating beads (F10) was carried out using hot plate and tail flick methods. Oral commercial KT tablets and KT solution were used for the comparison. The prepared beads remained floated for more than 8 h. The optimized formulation (F10) exhibited prolonged drug release (more than 8 h) and the drug release follows the Higuchi kinetic model, with a Fickian diffusion mechanism according to Korsmeyer-Peppas (n = 0.466). Moreover, F10 showed a sustained analgesic effect as compared to the commercial tablet.
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Awasthi R, Kulkarni GT. Development of novel gastroretentive drug delivery system of gliclazide: hollow beads. Drug Dev Ind Pharm 2013; 40:398-408. [DOI: 10.3109/03639045.2013.763817] [Citation(s) in RCA: 26] [Impact Index Per Article: 2.2] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 02/01/2023]
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32
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Formulation and statistical optimization of multiple-unit ibuprofen-loaded buoyant system using 23-factorial design. Chem Eng Res Des 2012. [DOI: 10.1016/j.cherd.2012.02.010] [Citation(s) in RCA: 69] [Impact Index Per Article: 5.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/23/2022]
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Kshirsagar SJ, Patil SV, Bhalekar MR. Statistical optimization of floating pulsatile drug delivery system for chronotherapy of hypertension. Int J Pharm Investig 2012; 1:207-13. [PMID: 23071945 PMCID: PMC3465146 DOI: 10.4103/2230-973x.93005] [Citation(s) in RCA: 5] [Impact Index Per Article: 0.4] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/04/2022] Open
Abstract
INTRODUCTION A pulsatile drug delivery system is characterized by a lag time that is an interval of no drug release followed by rapid drug release. The purpose of this work was to develop hollow calcium alginate beads for floating pulsatile release of valsartan intended for chronopharmacotherapy. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. MATERIALS AND METHODS To overcome the limitations of various approaches for imparting buoyancy, hollow/porous beads were prepared by simple process of acid-base reaction during ionotropic crosslinking by low viscosity sodium alginate and calcium chloride as a crosslinking agent. In this study, investigation of the functionality of the sodium alginate to predict lag time and drug release was statistically analyzed using the response surface methodology (RSM). RSM was employed for designing of the experiment, generation of mathematical models and optimization study. The chosen independent variables, i.e. sodium alginate and potassium bicarbonate were optimized with a 3(2) full factorial design. Floating time and cumulative percentage drug release in 6 h were selected as responses. RESULTS Results revealed that both the independent variables are significant factors affecting drug release profile. A second-order polynomial equation fitted to the data was used to predict the responses in the optimal region. The optimized formulation prepared according to computer-determined levels provided a release profile, which was close to the predicted values. The floating beads obtained were porous (21-28% porosity), hollow with bulk density <1 and had Ft(70) of 2-11 h. The floating beads provided expected two-phase release pattern with initial lag time during floating in acidic medium followed by rapid pulse release in phosphate buffer. CONCLUSION The proposed mathematical model is found to be robust and accurate for optimization of time-lagged formulations for programmable pulsatile release of valsartan.
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Burapapadh K, Takeuchi H, Sriamornsak P. Novel pectin-based nanoparticles prepared from nanoemulsion templates for improving in vitro dissolution and in vivo absorption of poorly water-soluble drug. Eur J Pharm Biopharm 2012; 82:250-61. [DOI: 10.1016/j.ejpb.2012.07.010] [Citation(s) in RCA: 38] [Impact Index Per Article: 2.9] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/20/2012] [Revised: 06/11/2012] [Accepted: 07/16/2012] [Indexed: 11/28/2022]
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Colonic luminal surface retention of meloxicam microsponges delivered by erosion based colon-targeted matrix tablet. Int J Pharm 2012; 427:153-62. [DOI: 10.1016/j.ijpharm.2012.01.036] [Citation(s) in RCA: 45] [Impact Index Per Article: 3.5] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/08/2011] [Revised: 12/28/2011] [Accepted: 01/14/2012] [Indexed: 11/22/2022]
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Abstract
INTRODUCTION Biopolymers have been used extensively in the pharmaceutical field. Pectin, a biopolymer, has several unique properties that enable it to be used as an excipient or carrier for oral drug delivery systems. Accordingly, several investigators have identified the benefits of pectin-based delivery systems for oral drug administration. AREAS COVERED This review first describes the chemical structure, source and production, degree of esterification and gel formation properties of pectin. The application of pectin in various oral drug delivery platforms is also discussed, that is, controlled release systems, gastro-retentive systems, colon-specific delivery systems and mucoadhesive delivery systems. EXPERT OPINION Pectin from different sources provides different gelling abilities, due to variations in molecular size and chemical composition. Like other natural polymers, a major problem with pectin is inconsistency in reproducibility between samples, which may result in poor reproducibility in delivery characteristics. Scintigraphic studies and in vivo studies, in both animals and human volunteers, demonstrate the successful development of a pectin-based colon-specific drug delivery system. Pectin-based controlled release systems, gastro-retentive systems and mucoadhesive systems present promising approaches for increasing the bioavailability of drugs, but are in their infancy. A lack of direct correlation between in vitro release and in vivo absorption studies is a major concern with these systems.
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Affiliation(s)
- Pornsak Sriamornsak
- Silpakorn University, Department of Pharmaceutical Technology, Pharmaceutical Biopolymer Group (PBiG), Faculty of Pharmacy, Nakhon Pathom 73000, Thailand.
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Adibkia K, Hamedeyazdan S, Javadzadeh Y. Drug release kinetics and physicochemical characteristics of floating drug delivery systems. Expert Opin Drug Deliv 2011; 8:891-903. [DOI: 10.1517/17425247.2011.574124] [Citation(s) in RCA: 20] [Impact Index Per Article: 1.4] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/05/2022]
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38
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Flocculating and suspending properties of commercial citrus pectin and pectin extracted from pomelo (Citrus maxima) peel. Carbohydr Polym 2011. [DOI: 10.1016/j.carbpol.2010.08.018] [Citation(s) in RCA: 34] [Impact Index Per Article: 2.4] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/24/2022]
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Pawar VK, Kansal S, Garg G, Awasthi R, Singodia D, Kulkarni GT. Gastroretentive dosage forms: a review with special emphasis on floating drug delivery systems. Drug Deliv 2010; 18:97-110. [PMID: 20958237 DOI: 10.3109/10717544.2010.520354] [Citation(s) in RCA: 85] [Impact Index Per Article: 5.7] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 12/21/2022] Open
Abstract
In the present era, gastroretentive dosage forms (GRDF) receive great attention because they can improve the performance of controlled release systems. An optimum GRDF system can be defined as a system which retains in the stomach for a sufficient time interval against all the physiological barriers, releases active moiety in a controlled manner, and finally is easily metabolized in the body. Physiological barriers like gastric motility and gastric retention time (GRT) act as obstacles in developing an efficient GRDF. Gastroretention can be achieved by developing different systems like high density systems, floating drug delivery systems (FDDS), mucoadhesive systems, expandable systems, superporous systems, and magnetic systems. All these systems have their own merits and demerits. This review focused on the various aspects useful in development of GRDF including the current trends and advancements.
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Affiliation(s)
- Vivek K Pawar
- Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, NH- 58, Uttar Pradesh, 250002, India.
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40
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Kim JS, Lee JS, Chang PS, Lee HG. Optimization, in vitro release and bioavailability of γ-oryzanol-loaded calcium pectinate microparticles reinforced with chitosan. N Biotechnol 2010; 27:368-73. [DOI: 10.1016/j.nbt.2010.02.018] [Citation(s) in RCA: 12] [Impact Index Per Article: 0.8] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/17/2009] [Revised: 02/11/2010] [Accepted: 02/22/2010] [Indexed: 11/28/2022]
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Sriamornsak P, Nunthanid J, Cheewatanakornkool K, Manchun S. Effect of drug loading method on drug content and drug release from calcium pectinate gel beads. AAPS PharmSciTech 2010; 11:1315-9. [PMID: 20730576 DOI: 10.1208/s12249-010-9513-x] [Citation(s) in RCA: 42] [Impact Index Per Article: 2.8] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/15/2010] [Accepted: 08/12/2010] [Indexed: 11/30/2022] Open
Abstract
Drug-loaded calcium pectinate gel (CaPG) beads were prepared by either mixing, absorption, or swelling method. The effects of drug loading method as well as the drug loading factors (i.e., drug concentration, soaking time in drug solution, type of solvent) on drug content and drug release were investigated. The amount of drug uptake (i.e., drug content) into CaPG beads increased as the initial drug concentration increased and varied depending on the loading method. The in vitro release studies in 0.1 N hydrochloric acid (HCl) and pH 6.8 buffer indicated that the drug loading method affected drug release and release parameter, time for 50% of drug release (T(50)). The mixing method provided a faster drug release and lower T(50) than the absorption method and swelling method, respectively. This is probably due to higher drug content in CaPG beads. The increased concentration of drug in soaking solution and soaking time resulted in higher drug content and thus faster drug release (lower in T(50) values). When using 0.1 N HCl as solvent for soaking instead of water, the drug release was slower owing to the increase in molecular tortuosity of CaPG beads. The drug release was also affected by pH of the release medium in which drug release in 0.1 N HCl was faster than in pH 6.8 buffer.
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Fabrication of pectin-based nanoemulsions loaded with itraconazole for pharmaceutical application. Carbohydr Polym 2010. [DOI: 10.1016/j.carbpol.2010.04.071] [Citation(s) in RCA: 51] [Impact Index Per Article: 3.4] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/19/2022]
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Javadzadeh Y, Hamedeyazdan S, Adibkia K, Kiafar F, Zarrintan MH, Barzegar-Jalali M. Evaluation of drug release kinetics and physico-chemical characteristics of metronidazole floating beads based on calcium silicate and gas-forming agents. Pharm Dev Technol 2010; 15:329-38. [DOI: 10.3109/10837450903196843] [Citation(s) in RCA: 17] [Impact Index Per Article: 1.1] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/13/2022]
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Wattanakorn N, Asavapichayont P, Nunthanid J, Limmatvapirat S, Sungthongjeen S, Chantasart D, Sriamornsak P. Pectin-based bioadhesive delivery of carbenoxolone sodium for aphthous ulcers in oral cavity. AAPS PharmSciTech 2010; 11:743-51. [PMID: 20443091 DOI: 10.1208/s12249-010-9424-x] [Citation(s) in RCA: 17] [Impact Index Per Article: 1.1] [Reference Citation Analysis] [Abstract] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 11/02/2009] [Accepted: 04/05/2010] [Indexed: 11/30/2022] Open
Abstract
The objective of this study was to prepare and evaluate the pectin-based dosage form for buccal adhesion. Carbenoxolone sodium, which is used for the treatment of aphthous ulcers in oral cavity, was used as a model drug. The pectin buccal discs were prepared by direct compression. The water uptake and erosion of pectin disc increased progressively with the swelling time. The bioadhesion of dried pectin discs decreased when either the discs were hydrated or the buccal tissue was wet with a small volume of medium. The influencing factors such as pectin type, pectin to lactose ratio, and sweetener type on the formulations were investigated. The results demonstrated that buccal discs prepared from pectin with a high degree of esterification (DE) showed a weaker and more friable characteristic than that with low DE. Decreasing pectin to lactose ratio resulted in the high dissolution rate with low bioadhesive properties. Addition of sweetener in the formulations also affected the hardness, friability, and bioadhesive properties of the discs. The pectin discs containing sweetening agent showed a higher drug release than those without sweetener. The results suggested that pectin-based bioadhesive discs could be used to deliver carbenoxolone sodium in oral cavity.
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Gaikwad M, Belgamwar V, Tekade A, Gattani S, Surana S. Formulation and evaluation of floating, pulsatile, multiparticulates using pH-dependent swellable polymers. Pharm Dev Technol 2010. [DOI: 10.3109/10837450903095334] [Citation(s) in RCA: 4] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/13/2022]
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Lee JS, Kim HW, Chung D, Lee HG. Catechin-loaded calcium pectinate microparticles reinforced with liposome and hydroxypropylmethylcellulose: Optimization and in vivo antioxidant activity. Food Hydrocoll 2009. [DOI: 10.1016/j.foodhyd.2009.05.005] [Citation(s) in RCA: 26] [Impact Index Per Article: 1.6] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 10/20/2022]
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Lee JS, Kim EJ, Chung D, Lee HG. Characteristics and antioxidant activity of catechin-loaded calcium pectinate gel beads prepared by internal gelation. Colloids Surf B Biointerfaces 2009; 74:17-22. [DOI: 10.1016/j.colsurfb.2009.06.018] [Citation(s) in RCA: 32] [Impact Index Per Article: 2.0] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 01/29/2009] [Revised: 06/11/2009] [Accepted: 06/12/2009] [Indexed: 11/26/2022]
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de Oliveira H, Tavares G, Nogueiras C, Rieumont J. Physico-chemical analysis of metronidazole encapsulation processes in Eudragit copolymers and their blending with amphiphilic block copolymers. Int J Pharm 2009; 380:55-61. [DOI: 10.1016/j.ijpharm.2009.06.028] [Citation(s) in RCA: 13] [Impact Index Per Article: 0.8] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 04/25/2009] [Revised: 06/17/2009] [Accepted: 06/24/2009] [Indexed: 11/29/2022]
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Meka L, Kesavan B, Kalamata VN, Eaga CM, Bandari S, Vobalaboina V, Yamsani MR. Design and evaluation of polymeric coated minitablets as multiple unit gastroretentive floating drug delivery systems for furosemide. J Pharm Sci 2009; 98:2122-32. [DOI: 10.1002/jps.21562] [Citation(s) in RCA: 33] [Impact Index Per Article: 2.1] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/07/2022]
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Elmowafy EM, Awad GA, Mansour S, El-Shamy AEHA. Ionotropically emulsion gelled polysaccharides beads: Preparation, in vitro and in vivo evaluation. Carbohydr Polym 2009. [DOI: 10.1016/j.carbpol.2008.07.019] [Citation(s) in RCA: 27] [Impact Index Per Article: 1.7] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/24/2022]
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