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用于口服给药的聚[N-乙烯基-2-吡咯烷酮-聚乙二醇二丙烯酸酯]-壳聚糖互聚物pH响应水凝胶的制备及体外评价

Preparation and in-vitro evaluation of poly[N-vinyl-2-pyrrolidone-polyethylene glycol diacrylate]-chitosan interpolymeric pH-responsive hydrogels for oral drug delivery.

作者信息

Shantha K L, Harding D R

机构信息

Chemistry, Institute of Fundamental Sciences, Massey University, Palmerston North, New Zealand.

出版信息

Int J Pharm. 2000 Oct 10;207(1-2):65-70. doi: 10.1016/s0378-5173(00)00533-0.

Abstract

Biocompatible and biodegradable pH-responsive hydrogels based on N-vinyl pyrrolidone (NVP), polyethylene glycol diacrylate (PAC) and chitosan were prepared for controlled drug delivery. These interpolymeric hydrogels were synthesized by a free radical polymerization technique using azobisisobutyronitrile (AIBN) as initiator and N,N'-methylenebisacrylamide (BIS) as crosslinker. These hydrogels were subjected to equilibrium swelling studies in enzyme-free simulated gastric and intestinal fluids (SGF and SIF). These swelling studies clearly indicated that these hydrogels were swollen more in SGF when compared to SIF. Theophylline and 5-fluorouracil (5-FU) were entrapped into these hydrogels and equilibrium-swelling studies were carried out for the drug-entrapped gels in enzyme-free SGF and SIF. The in-vitro release profiles of the drugs were established in enzyme-free SGF. More than 50% of the entrapped drugs were released in the first 2 h at gastric pH and the rest of the drug release was slower.

摘要

制备了基于N-乙烯基吡咯烷酮(NVP)、聚乙二醇二丙烯酸酯(PAC)和壳聚糖的生物相容性和可生物降解的pH响应水凝胶用于药物控释。这些聚合物间水凝胶通过自由基聚合技术合成,使用偶氮二异丁腈(AIBN)作为引发剂,N,N'-亚甲基双丙烯酰胺(BIS)作为交联剂。这些水凝胶在无酶模拟胃液和肠液(SGF和SIF)中进行平衡溶胀研究。这些溶胀研究清楚地表明,与SIF相比,这些水凝胶在SGF中溶胀得更多。将茶碱和5-氟尿嘧啶(5-FU)包裹在这些水凝胶中,并对包裹药物的凝胶在无酶SGF和SIF中进行平衡溶胀研究。在无酶SGF中建立了药物的体外释放曲线。在胃pH值下,超过50%的包裹药物在最初2小时内释放,其余药物释放较慢。

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