摘要
背景:普通滴眼液由于泪液冲刷与鼻泪管吸收等因素,在眼表停留时间短,生物利用度低。目的:以壳聚糖、明胶为载体材料,左氧氟沙星为模型药物,制备应用于眼表的缓控释微球并考察其理化性质与体外释放。方法:采用喷雾干燥法制备左氧氟沙星壳聚糖/明胶微球,通过扫描电镜观察微球的表面形态,激光粒度仪测量微球粒径分布与zeta电位,高效液相色谱法检测微球的载药率与包封率,动态透析法研究微球体外药物释放情况。结果与结论:所得微球形态良好,粒径分布窄,平均粒径为(1267.4±115.3)nm,zeta电位为+(32.19±0.85)mV,载药量为(18.31±0.22)%,包封率为(91.53±1.12)%。载药微球体外释放符合一级释药方程Ln(1-Q)=-0.6991t-0.0864,r2=0.9451。说明壳聚糖/明胶载药微球对左氧氟沙星具有缓释作用。实验采用喷雾干燥法成功制备了粒径及分布适宜、释放周期较理想、药物稳定性好的载左氧氟沙星壳聚糖明胶缓释微球。
BACKGROUND： The bioavailability of ordinary eye drops is generally low due to short pre-corneal residence time related to tear turnover and nasolachrymal absorption. OBJECTIVE： To prepare controlled release microspheres of chitosan-gelatin containing levofloxacin for ophthalmic delivery, and to investigate their physiochemical properties and release profiles in vitro. METHODS： Chitosan-gelatin microspheres containing levofloxacin were prepared by spray drying method. The surface morphology, particle size distribution and zeta potential, drug-loading rate and encapsulation efficiency, and drug release profiles in vitro of the microspheres were detected by scanning electron microscopy, laser particle size analyzer, high performance liquid chromatography and dynamic dialysis respectively. RESULTS AND CONCLUSION： The results showed that the prepared microspheres had a regular shape and narrow particle size distribution with the average particle size of （126 7.4±115.3） nm, the drug loading rate of （18.31±0.22）% and the encapsulation efficiency of （91.53±1.12）%. The release profile in vitro was in line with the first order equation of [Ln （1-Q）= -0.699 1t-0.086 4, r2=0.945 1]. Chitosan-gelatin microspheres containing levofloxacin were successfully prepared by spray drying method with acceptable particle size distribution, suitable release period, and high drug stability.
出处
《中国组织工程研究》
CAS
CSCD
2012年第16期2917-2921,共5页
Chinese Journal of Tissue Engineering Research
基金
浙江省自然科学基金项目(Y2090914)
浙江省新苗人才计划(2010R413044)~~
