Sustained release of ibuprofen from polymeric micelles with a high loading capacity of ibuprofen in media simulating gastrointestinal tract fluids

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• 作者：Yong Zhang^a ; Jiajia Chen^a ; Genghui Zhang^a ; Jiawei Lu^a ; Husheng Yan^a ; ^{yanhs@nankai.edu.cn} ; Keliang Liu^b ; ^{keliangliu@yahoo.com}
• 关键词：Drug delivery ; Polymeric micelles ; Ibuprofen ; Sustained release ; pH-responsive
• 刊名：Reactive and Functional Polymers
• 出版年：2012
• 期刊代码：92_13815148
• 类别：ch
• 出版时间：June, 2012
• 卷：72
• 期：6
• 页码：359-364
• 文件大小：495 K

摘要

Amphiphilic diblock copolymers with poly(ethylene glycol) as the hydrophilic block and a random copolymer of n-butyl methacrylate or styrene and (N,N-diethylamino)ethyl methacrylate as the hydrophobic block were prepared by atom transfer radical polymerization (ATRP). Ibuprofen, a model drug that contains a carboxylic group and hydrophobic moiety, was loaded into micelles formed from the amphiphilic diblock copolymers by a combination of ionic interaction and hydrophobic effect. The loading capacity of ibuprofen in the micelles reached 60%. Loaded ibuprofen was released in a sustained fashion into media simulating gastric fluid (pH 1.6, 2 h), small intestinal fluid (pH 7.4, 4 h), and colon fluid (pH 6.7, 18 h). Simulating the case of oral administration at 2 doses per day, loaded ibuprofen was released almost linearly against time after the second dose in media simulating human gastrointestinal tract fluids.