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聚(N-乙烯基己内酰胺-共-甲基丙烯酸)水凝胶微球用于口服胰岛素传递。

Poly(N-vinylcaprolactam-co-methacrylic acid) hydrogel microparticles for oral insulin delivery.

机构信息

Industrial Biotechnology Group, Reliance Life Sciences Pvt. Ltd., Dhirubhai Ambani Life Sciences Centre, Thane Belapur Road, Rabale, Navi Mumbai 400701, India.

出版信息

J Microencapsul. 2011;28(5):384-94. doi: 10.3109/02652048.2011.576782.

Abstract

pH-sensitive copolymeric hydrogels prepared from N-vinylcaprolactam and methacrylic acid monomers by free radical polymerization offered 52% encapsulation efficiency and evaluated for oral delivery of human insulin. The in vitro experiments performed on insulin-loaded microparticles in pH 1.2 media (stomach condition) demonstrated no release of insulin in the first 2 h, but almost 100% insulin was released in pH 7.4 media (intestinal condition) in 6 h. The carrier was characterized by Fourier transform infrared, differential scanning calorimeter, thermogravimetry and nuclear magnetic resonance techniques to confirm the formation of copolymer, while scanning electron microscopy was used to assess the morphology of hydrogel microparticles. The in vivo experiments on alloxan-induced diabetic rats showed the biological inhibition up to 50% and glucose tolerance tests exhibited 44% inhibition. The formulations of this study are the promising carriers for oral delivery of insulin.

摘要

通过自由基聚合由 N-乙烯基己内酰胺和甲基丙烯酸单体制备的 pH 敏感共聚水凝胶提供了 52%的包封效率,并评估了其用于口服递送人胰岛素的效果。在 pH 1.2 介质(胃条件)中进行的载有胰岛素的微球的体外实验表明,在最初的 2 小时内没有胰岛素释放,但在 pH 7.4 介质(肠条件)中在 6 小时内几乎 100%释放胰岛素。通过傅里叶变换红外、差示扫描量热法、热重分析和核磁共振技术对载体进行了表征,以确认共聚物的形成,而扫描电子显微镜则用于评估水凝胶微球的形态。在链脲佐菌素诱导的糖尿病大鼠的体内实验中,生物抑制率高达 50%,葡萄糖耐量试验显示抑制率为 44%。本研究的制剂是胰岛素口服递送的有前途的载体。

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