β-环糊精交联聚丙烯酸水凝胶的合成及其药物控制释放研究

采用1,3-二环己基碳化二亚胺(DCC)为缩合剂,通过β环糊精与丙烯酸的酯化反应合成了不同取代度的丙烯酸β环糊精酯(βCD6A),以此为单体与丙烯酸通过氧化还原自由基引发聚合,合成出了不同交联密度和不同环糊精含量的新型水凝胶(AAβCD6A).溶胀实验表明,该类水凝胶均具有pH敏感性,溶胀动力学实验进一步对其机理进行了探讨.选择苯丁酸氮芥(CHL)作为模型药物,考察了不同pH下AAβCD6A水凝胶对药物释放行为的影响.结果表明,pH=6.8时药物释放率均大于pH=2.0时药物释放率,环糊精的存在表现出促释作用.

STUDY ON HYDROGELS OF β-CYCLODEXTRIN-CROSSLINKED ACRYLIC ACID AND THEIR CONTROLLED DRUG RELEASE BEHAVIOR

β-cyclodextrin(β-CD)-containing acrylic monomers (β-CD-6-A) with different substitution degree were prepared by using dicyclohexylcarbodiimide (DCC) as condensation agent,and a functional hydrogel was synthesized by copolymerization of β-CD-6-A with acrylic acid (AA) using a redox initiator system in aqueous solutions.The nuclear magnetic resonance ( 1H-NMR),infrared spectroscopy (IR) and swelling experiments were employed to characterize the β-CD modified monomers and their copolymers.The results show that the resin's equilibrium swelling ratio (ESR) possesses pH-sensitivities.The mechanisms of controlled drug release were investigated by using an anti-cancer drug,chlorambucil (CHL),as the model medicines at different medium.The release behavior of CHL from the hydrogels β-CD-AA indicated that the release ratio of CHL is affected by the pH value,and the cumulative release at pH=6.8 was higher than that at pH=2.0. In addition,the release efficiency of CHL from the hydrogels with β-CD is higher than that of the hydrogels without β-CD.