Original Articles
Copyright ©The Author(s) 1999. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Gastroenterol. Feb 15, 1999; 5(1): 57-60
Published online Feb 15, 1999. doi: 10.3748/wjg.v5.i1.57
Preparation and distribution of 5-fluorouracil 125I sodium alginate-bovine serum albumin nanoparticles
Yi-Mu Yi, Tang-Yu Yang, Wei-Min Pan
Yi-Mu Yi, Pharmaceutics Department of School of Pharmacy, Tongji Medical U-niversity, Wuhan 430030, Hubei Province, China
Tang-Yu Yang, Materia Medica Department of School of Pharmacy, Tongji Medical U-niversity, Wuhan 430030, Hubei Province, China
Wei-Min Pan, Nuclear Medicine Department of Medical Experimental Research Cen-ter, Tongji Medical University, Wuhan 430030, Hubei Province, China
Yi-Mu Yi, born on January 15, 1954 in Huanggang County, Hubei Province, graduated from School of Pharmacy of Tongji Medical University in 1975, now working in the Pharmaceutics Department of the same university, mainly engaged in researches in new dosage forms of drugs and new drug-products, having 3 papers published and ten papers presented at international and national academic conferences.
Author contributions: All authors contributed equally to the work.
Supported by the National Natural Science Foundation of China, No.39270809
Correspondence to: Yi-Mu Yi, Pharmaceutics Department of School of Pharmacy, Tongji Medical University, Wuhan 430030, Hubei Province, China
Received: November 9, 1998
Revised: November 30, 1998
Accepted: December 18, 1998
Published online: February 15, 1999
Abstract

AIM: To prepare 5-FU sodium alginate 125I bovine serum albumin nanoparticles (BSA NP), to de-termine the radioactive count in different organs of rats at different time points after oral adminis-tration of 5-FU 125I sodium alginate-BSA NP and to calculate the kinetic parameters of its metabolism.

METHODS: Emulsion solidification method was used to prepare 5-FU 125I sodium alginate-BSA NP, and to determine its diameter under trans-mission electronic microscope (TEM). Then the rate of NP and external drug releasing velocity were measured. Radioactive counting in different organs of rats wa s made after oral adminis-tration of the NP by GAMA Counter, and the ki-netic para meters of drug metabolism were calcu-lated by handling the data with the two-depart-ment model.

RESULTS: The average arithmatic diameter of the NP was 166 nm ± 34 nm, the rate of 5-FU was 32.8% and the cumulative external releasing ra-tio amounted to 84.0% within 72 hours. The NP was mainly distributed in the liver, spleen, lungs and kidneys after NP oral administration to rats. The mic ro-radioautographic experiment showed that NP was distributed in the Kupffers cells of liver, liver parenchymal cells and the phagocytes of spleen and lungs. The kinetic pa-rameters of matabolism were: T1/2 = 9.42 h, Cmax =2.45 × 107 Bq, Tmax = 2.18 h, AUC = 148 × 109 Bq.

CONCLUSION: NP is difficult to pass through the blood-cerebral barrier,and 125I sodium alginate-BSA NP enters the body circulation by gastroin testinal passage.

Keywords: 5-fluorouracil (5-FU); sodi-um alginate-al bumin; preparation of nanoparticle (NP); distribution