新型智能聚合物水凝胶的制备及胰岛素载药性能研究
Preparation and characterization of a novel smart polymeric hydrogel for drug delivery of insulin.
机构信息
Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran ; Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
出版信息
Bioimpacts. 2011;1(2):135-43. doi: 10.5681/bi.2011.018. Epub 2011 Aug 10.
INTRODUCTION
Over the past years, temperature and pH-sensitive hydrogels was developed as suitable carriers for drug delivery. In this study temperature and pH-sensitive hydrogels was designed for an oral insulin delivery modeling.
METHODS
NIPAAm-MAA -HEM copolymers were synthesized by radical chain reaction with 86:4:10 (5% w/v) ratios respectively. Reaction was carried out in 1,4-Dioxane under Nitrogen gas-flow. The copolymers were characterized with FT-IR, 1H-NMR and DSC. Copolymers were loaded with regular insulin by modified double emulsion method with ratio of 1:10. Release study carried out in two different pH (pH=2 and 7.4 for stomach and intestine simulation respectively) at 37ºC. For each pH, a 5 mL suspension of the insulin containing hydrogel was taken in to a cellulose acetate dialysis membrane, and the dialysis membrane was allowed to float in a beaker containing 15 mL of buffer solution. The beakers were placed in a shaker incubator maintained at 37ºC. Phosphate buffer (0.1 M, pH 3)/ acetonitrile (60/40) was used as the mobile phase in HPLC assay.
RESULTS
Yield of reaction was 86% with an optimum Lower Critical Solution Temperature point (30ºC). In-vitro studies showed a control release behavior via pH changes which the amount of insulin releases was 80% and 20% at pH=2 and 7.4 respectively.
CONCLUSION
Results showed that by optimizing polymerization and loading method we could achieve a suitable nano system for oral delivery of insulin.
简介
在过去的几年中，温度和 pH 敏感水凝胶已被开发为适合药物输送的载体。本研究设计了温度和 pH 敏感水凝胶，用于模拟口服胰岛素输送。
方法
采用自由基链反应，以 86:4:10（5%w/v）的比例分别合成 NIPAAm-MAA-HEM 共聚物。反应在氮气气流下于 1,4-二恶烷中进行。共聚物用 FT-IR、1H-NMR 和 DSC 进行表征。共聚物通过改良的双乳液法用 1:10 的比例负载普通胰岛素。在 37°C 下在两种不同的 pH（分别为 pH=2 和 7.4，模拟胃和肠）下进行释放研究。对于每种 pH，将含有胰岛素的水凝胶的 5 mL 悬浮液置于纤维素乙酸酯透析膜中，并允许透析膜漂浮在装有 15 mL 缓冲溶液的烧杯中。将烧杯放置在保持在 37°C 的摇床孵育器中。HPLC 测定中使用磷酸盐缓冲液（0.1 M，pH 3）/乙腈（60/40）作为流动相。
结果
反应收率为 86%，最佳下临界溶液温度点（30°C）。体外研究表明，通过 pH 值的变化可以实现控制释放行为，在 pH=2 和 7.4 时胰岛素的释放量分别为 80%和 20%。
结论
结果表明，通过优化聚合和负载方法，我们可以为口服胰岛素输送开发出合适的纳米系统。
Zotero 插件