Guo MQ, Hu P, Huang ZW. Cyclodextrin host-guest complex to facilitate sinomenine-based osteoporosis therapy. World J Stem Cells 2025; 17(3): 101376 [PMID: 40160693 DOI: 10.4252/wjsc.v17.i3.101376]
Corresponding Author of This Article
Zheng-Wei Huang, PhD, Associate Professor, College of Pharmacy, Jinan University, No. 855 East Xingye Dadao, Panyu District, Guangzhou 511443, Guangdong Province, China. huangzhengw@jnu.edu.cn
Research Domain of This Article
Pharmacology & Pharmacy
Article-Type of This Article
Letter to the Editor
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World J Stem Cells. Mar 26, 2025; 17(3): 101376 Published online Mar 26, 2025. doi: 10.4252/wjsc.v17.i3.101376
Cyclodextrin host-guest complex to facilitate sinomenine-based osteoporosis therapy
Meng-Qin Guo, Ping Hu, Zheng-Wei Huang
Meng-Qin Guo, Ping Hu, Zheng-Wei Huang, College of Pharmacy, Jinan University, Guangzhou 511443, Guangdong Province, China
Co-corresponding authors: Ping Hu and Zheng-Wei Huang.
Author contributions: Guo MQ contributed to the manuscript writing and artwork preparation; Hu P and Huang ZW participated in the conceptualisation, supervision, and proofreading of this manuscript, and they contributed equally to this manuscript as co-corresponding authors. All authors have read and agreed to the published version of the manuscript.
Supported by Guangdong Basic and Applied Basic Research Foundation, No. 2024A1515011236; and General Program of Administration of Traditional Chinese Medicine of Guangdong Province, No. 20241071.
Conflict-of-interest statement: All the authors report no relevant conflicts of interest for this article.
Corresponding author: Zheng-Wei Huang, PhD, Associate Professor, College of Pharmacy, Jinan University, No. 855 East Xingye Dadao, Panyu District, Guangzhou 511443, Guangdong Province, China. huangzhengw@jnu.edu.cn
Received: September 12, 2024 Revised: December 9, 2024 Accepted: March 6, 2025 Published online: March 26, 2025 Processing time: 189 Days and 21.5 Hours
Abstract
Xiao et al reported on the natural product sinomenine (SIN), which is a traditional Chinese medicine for treating osteoporosis via its modulation of autophagy; however, SIN was dissolved in dimethyl sulfoxide prior to administration, which is not conducive to the development of clinical injectables. By comparing solubilization techniques, including amorphisation, emulsification, micellisation, nano-crystallisation and host-guest inclusion, we found that the solubilization of SIN by host-guest inclusion can enhance solubility and improve stability and has an increased release rate and enhanced bioavailability. Therefore, we conclude that host-guest inclusion holds promise for SIN solubilization. To solubilise SIN, we selected β-cyclodextrin as the host agent considering its excellent biocompatibility, efficient encapsulation ability, mature preparation process and adequate drug stability. If the prerequisites of SIN-β-cyclodextrin complexes in terms of safety, efficacy, stability and the relevant laws and regulations are met, its clinical application for the treatment of osteoporosis may be achieved.
Core Tip: Sinomenine (SIN) inhibits phosphorylation processes in the phosphatidylinositol 3-kinase/protein kinase B/mammalian target of the rapamycin pathway, increases autophagic capacity and promotes osteogenic differentiation, hence effectively treating osteoporosis. Nevertheless, the insolubility of SIN is a limitation to its clinical application. Here, we proposed the use of host-guest inclusion instead of dimethyl sulfoxide (DMSO) to solubilise SIN by preparing SIN-β-cyclodextrin complexes. Compared with direct dissolution in DMSO, the SIN-β-cyclodextrin complexes circumvent the safety concerns associated with DMSO, providing higher water solubility, improved drug stability, lower toxicity and side effects and optimal drug release properties. We conclude the clinical application of SIN-β-cyclodextrin complexes to treat osteoporosis may be achieved.
