生物降解多功能缓释微球的制备与表征

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Transmission electron microscopy, Quasielastic laser light scattering, Zeta电位仪, FTIR, 1H NMR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).

Preparation and Characterization of Novel Biodegradable Multifunctional Microspheres

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 TEM, quasielastic laser light scattering with a Malvern Zetasizer, 1H NMR and FTIR. 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.