Preparation of insulin loaded PLGA-Hp55 nanoparticles for oral delivery
Preparation of insulin loaded PLGA-Hp55 nanoparticles for oral delivery
复制标题
DOI：
10.1002/jps.20750
复制
发表时间：
2007-02-01
影响因子：
3.8
通讯作者：
Shi, Kai
中科院分区：
文献类型：
--
作者：
Cui, Fu-De;Tao, An-Jin;Shi, Kai
本研究旨在探讨聚乳酸 - 羟基乙酸共聚物纳米粒（PNP）和聚乳酸 - 羟基乙酸共聚物 - Hp55纳米粒（PHNP）作为口服胰岛素递送的潜在药物载体的制备。通过改良的水包油乳液溶剂扩散法制备纳米粒，并对其理化特性、体外药物释放以及在糖尿病大鼠中的降血糖效果进行了评估。PNP和PHNP的粒径分别为150 ± 17和169 ± 16纳米，纳米粒的药物回收率分别为50.30 ± 3.1%和65.41 ± 2.3%。在模拟胃液中1小时内胰岛素从纳米粒中的初始释放分别为50.46 ± 6.31%和19.77 ± 3.15%。在糖尿病大鼠中，与皮下注射（1 IU/kg）相比，PNP和PHNP的相对生物利用度分别为3.68 ± 0.29%和6.27 ± 0.42%。结果表明，使用载胰岛素的PHNP是一种降低血糖水平的有效方法。（c）2006威利 - 利斯公司
The aim of the present work was to investigate the preparation of PLGA nanoparticles (PNP) and PLGA-Hp55 nanoparticles (PHNP) as potential drug carriers for oral insulin delivery. The nanoparticles were prepared by a modified emulsion solvent diffusion method in water, and their physicochemical characteristics, drug release in vitro and hypoglycemic effects in diabetic rats were evaluated. The particle sizes of the PNP and PHNP were 150 +/- 17 and 169 +/- 16 nm, respectively, and the drug recoveries of the nanoparticles were 50.30 +/- 3.1 and 65.41 +/- 2.3%, respectively. The initial release of insulin from the nanoparticles in simulated gastric fluid over 1 h was 50.46 +/- 6.31 and 19.77 +/- 3.15%, respectively. The relative bioavailability of PNP and PHNP compared with subcutaneous (s.c.) injection (1 IU/kg) in diabetic rats was 3.68 +/- 0.29 and 6.27 +/- 0.42%, respectively. The results show that the use of insulin-loaded PHNP is an effective method of reducing serum glucose levels. (c) 2006 Wiley-Liss, Inc.