海藻酸钠基pH响应性聚合物胶束的制备及释药性能研究  

Preparation of p H-responsive Polymeric Micelles based on Sodium Alginate and Its Drug Release Property

作　　者：韩俊源 王玉珑 刘庆坚 刘艳新 HAN Junyuan;WANG Yulong;LIU Qingjian;LIU Yanxin(School of Chemistry and Food Engineering,Changsha University of Science and Technology,Changsha,Hu'nan Province,410114)

机构地区：[1]长沙理工大学化学与食品工程学院,湖南长沙410114

出　　处：《中国造纸学报》2021年第2期18-23,共6页Transactions of China Pulp and Paper

基　　金：湖南省自然科学基金项目(2015JJ2008)。

摘　　要：采用1-(3-二甲氨基丙基)-3-乙基碳二亚胺盐酸盐(EDC)和N-羟基琥珀酰亚胺(NHS)对海藻酸钠进行改性并制备了海藻酸钠基p H响应性聚合物胶束(以下简称聚合物胶束),分析了EDC/NHS改性前后海藻酸钠的红外光谱(FT-IR)、临界胶束浓度(CMC)、粒径和Zeta电位;利用反溶剂重结晶法将疏水药物金雀异黄酮包裹于聚合物胶束中,并对载药聚合物胶束的包封率、载药量和pH响应性进行了研究。结果表明,经EDC/NHS改性后的海藻酸钠可在水中形成聚合物胶束,其CMC为0.041 mg/mL;当聚合物胶束与金雀异黄酮质量比为10∶1时,聚合物胶束的包封率和载药量分别为74.4%和8.6%;体外溶出实验表明,载药聚合物胶束具有良好的pH响应性,其在酸性条件(pH值=2.0)下相对稳定,在中性条件(pH值=7.4)下能释放药物,其有望用作口服型肠吸收药物的载体,以实现药物的缓释和控释。In this study sodium alginate(SA)was modified with 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride(EDC)and N-hydroxysuccinimide(NHS),then the sodium alginate-based pH-responsive polymer micelles were prepared. The Fourier transform infrared spectroscopy(FT-IR),critical micelle concentration(CMC),particle size,and Zeta potential were analyzed for SA before and after modified by EDC/NHS. The genistein was then encapsulated in polymeric micelles based on anti-solvent recrystallization method,and the drug loading efficiency,drug loading capacity,and pH responsiveness of the polymer micelles were studied. The results showed that EDC/NHS-modified SA could form polymer micelles in water,and its CMC was 0. 041 mg/mL. The loading efficiency and drug loading capacity of polymeric micelles were 74. 4% and 8. 6%,respectively when the mass ratio of polymeric micelles to genistein was 10∶1. The in vitro release study showed that the polymeric micelles loaded with drug were pH-responsive and relatively stable under acidic conditions(pH value=2. 0),and would release drugs under neutral conditions(pH value =7. 4),enabling it to be used as a carrier for oral drugs absorbing by intestinal tract,so as to achieve controlled release and sustained release of drugs.

关 键 词：海藻酸钠 聚合物胶束 PH响应性 生物质材料 药物释放 

分 类 号：TS72[轻工技术与工程—制浆造纸工程] TQ317.4[化学工程—高聚物工业]