聚(2-甲基丙烯酸二甲胺乙酯-co-二烯丙基二甲基氯化铵)水凝胶调控Notoginsenoside药物释放效应

摘要

Aim To investigate the effects of Poly [(dimethylaminoethyl methacrylate)-co-(diallyldimethyl ammonium chloride)]i.e. poly(DMAEMA-co-DADMAC) hydrogel on the controlled drug delivery system for releasing notoginsenoside as a model drug. MethodsNovel pH/temperature sensitive [poly(DMAEMA-co-DADMAC)] hydrogels was synthesized by radiation induced copolymerization and cross-linking of dimethylaminoethyl methacrylate (DMAEMA) and diallyldimethyl ammonium chloride (DADMAC). The copolymer structure and gel fractions were confirmed by PT-IR, UV-Vis, and releasing analysis of notoginsenoside, in order to achieve a controlled drug delivery system for notoginsenoside and evaluating the reseasing properties in three rats. ResultsThe results show that the copolymerization of DMAEMA and DADMAC is an azeotropic compound. The charge of polyDADMAC (polyelectrolyte) could distribute uniformly along the macromolecular chains in poly(DMAEMA-co-DADMAC) hydrogels. The equilibrium degree of swelling (EDS) of the gels had a maximum at 3% of charge density and temperature sensitivity would not exist when charge density was approximately higher than 5%. The animal experiments show that the gels saturated with Panax notoginsen(PANS) have relatively good biological compatibility and could be of function in cicatrizing the wound of rat due to the release of notoginsenoside. ConclusionTarget-oriented drug delivery system of Chinese herbs, the release of notoginsenoside can be controlled by adjusting the pH, ionic strength, temperature of solution as well as the composition and structure of the gel.%目的 研究共聚物2-甲基丙烯酸二甲胺乙酯-co-二烯丙基二甲基氯化铵水凝胶对中草药notoginsenoside为模型药物的调控给药释放效应.方法 以辐射共聚和交联法合成的新颖温度/酸度敏感性水溶胶,注入3只大鼠体内以研究中药notoginsenoside在其体内受控释放性能.共聚物结构和凝胶片断经红外、紫外以及释放药效分析确证.结果 2-甲基丙烯酸二甲胺乙酯(DMAEMA)和二烯丙基二甲基氯化铵(DADMAC)为共沸化合物.在标题聚合物中,聚DADMAC电解质的电荷能沿大分子链均匀分布.凝胶的平衡溶胀度(EDS)在载体电荷密度3%摩尔时最大,而载体电荷密度接近5%摩尔及其以上时温度敏感性消失.溶液温度、酸度和盐浓度以及凝胶组成和结构能调控notoginsenoside给药释放;用三七(Panax notoginsen,PANS)饱和的水凝胶能有效释放notoginsenoside而呈现出相当好的生物兼容性和具有愈合大鼠伤口的功能.结论 靶向药物释放可以通过调节pH, 离子强度,溶液温度以及凝胶的组成和结构而有效实现.