Shantha K L, Harding D R
Chemistry, Institute of Fundamental Sciences, Massey University, Palmerston North, New Zealand.
Int J Pharm. 2000 Oct 10;207(1-2):65-70. doi: 10.1016/s0378-5173(00)00533-0.
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.
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。
