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用于胰岛素口服递送的多功能聚合物水凝胶的辐射合成

Radiation synthesis of multifunctional polymeric hydrogels for oral delivery of insulin.

作者信息

Abou Taleb Manal F

机构信息

Chemistry Department, Faculty of Science and Humanities, Salman bin Abdulaziz University, Alkharj, Saudi Arabia; Polymer Chemistry Department, National Center for Radiation Research and Technology, P. O. Box No. 29, Nasr city, Cairo 11731 Egypt.

出版信息

Int J Biol Macromol. 2013 Nov;62:341-7. doi: 10.1016/j.ijbiomac.2013.09.004. Epub 2013 Sep 19.

DOI:10.1016/j.ijbiomac.2013.09.004
PMID:24055698
Abstract

Polyelectrolyte crosslinked hydrogel was synthesized using gamma radiation-induced copolymerization of methacrylic acid (MAA), N,N-dimethyl aminoethyl methacrylate (DMAEMA) in aqueous solution to utilize for oral delivery of insulin. The influence of copolymer composition and pH value of the surrounding medium on the type of water diffusion in the glassy polymer was discussed. In addition, the swelling kinetics tests on MAA/DMAEMA (90/10) reveal that the swelling kinetics of the proposed hydrogel follows a Fickian diffusion process in media of pH 5, and an anomalous diffusion process in media of pH 1.5 and 7.2. The cross-linked three-dimensional polymers were characterized by scanning electron microscopy and FT-IR. In the matrices with increase in the content of MAA had shown increased bioadhesivity. Insulin was entrapped in these gels and the in vitro release profiles were established separately in both (SGF, pH 1.5) and (SIF, pH 7.2). The release profile of insulin showed negligible release in acidic media (SGF, pH 1.5) and sustained release in simulated intestinal fluid (SIF, pH 7.2). Drug release studies showed that the increasing content of MAA in the copolymer enhances release in SIF to design and improve insulin release behavior from these carriers.

摘要

采用γ射线引发甲基丙烯酸(MAA)、甲基丙烯酸N,N - 二甲氨基乙酯(DMAEMA)在水溶液中共聚的方法合成了聚电解质交联水凝胶,用于胰岛素的口服给药。讨论了共聚物组成和周围介质pH值对玻璃态聚合物中水扩散类型的影响。此外,对MAA/DMAEMA(90/10)进行的溶胀动力学测试表明,所提出的水凝胶在pH值为5的介质中的溶胀动力学遵循菲克扩散过程,而在pH值为1.5和7.2的介质中则遵循反常扩散过程。通过扫描电子显微镜和傅里叶变换红外光谱对交联的三维聚合物进行了表征。在基质中,随着MAA含量的增加,生物粘附性增强。将胰岛素包封在这些凝胶中,并分别在(模拟胃液,pH 1.5)和(模拟肠液,pH 7.2)中建立了体外释放曲线。胰岛素的释放曲线显示在酸性介质(模拟胃液,pH 1.5)中释放可忽略不计,而在模拟肠液(pH 7.2)中持续释放。药物释放研究表明,共聚物中MAA含量的增加会增强在模拟肠液中的释放,从而设计并改善这些载体的胰岛素释放行为。

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