通过羧甲基壳聚糖接枝二甲基十八烷基环氧丙基氯化铵,合成水油两溶性的羧甲基壳聚糖十八烷基季铵盐(OQCMC);并将其作为乳化剂与乳酸-羟基乙酸(PLGA)和羟乙基纤维素(HEC)复合,利用溶剂挥发法,构建一种多功能的药物载体缓释系统,并尝试包裹脂溶性药物盐酸米诺环素.利用透射电子显微镜(TEM),激光光散射仪,Zeta电位仪,FTIR,1HNMR等对OQCMC及载药微球进行表征,并进行药物的体外释放实验.结果表明:OQCMC可作为一种优良的乳化剂对PLGA微球进行修饰;并可使复合微球体系带正电,在提高微球载药率(9.4%)的同时减小微球粒径[(166.4±0.8)nm];复合微球体系对盐酸米诺环素具有较好的物理包裹能力,并有长效缓释作用(PBS,pH=7.9).
Octadecyl quaternized carboxymethyl chitosan (OQCMC) was synthesized through carboxymethyl chitosan grafting with glycidyl octadecyl dimethylammonium chloride. By a solvent evaporation method, the drug delivery system was prepared based on poly(lactic-co-glycolic acid) (PLGA) block copolymers, hydroxyethyl cellulose and OQCMC, which was tried to load minocycline hydrochloride. The microspheres were characterized by transmission electron microscopy (TEM), quasielastic laser light scattering with a Malvern Zetaslzer, 1H NMR and PTIR. The results showed that the complex delivery system was good to load the minocycline hydrochloride and could provide long-term release behaviour through drug release experiment in vitro. The drug loading efficiency of minocycline hydrochloride could reach 9.4% by using the polymer surfactant OQCMC. It is good to decrease the particle size [(166.4±0.8) nm], increase the Zeta potential and keep the stabilization of the microspheres.