脑用表阿霉素壳聚糖微球的制备及其特性考察

Study on preparation and properties of epirubicin-loaded chitosan microspheres for the cerebral administration

目的:以壳聚糖为载体材料,表阿霉素为模型药物,制备脑内局部给药缓释微球。方法:以液体石蜡为油相,L-抗坏血酸棕榈酸酯为交联剂,司盘-80为乳化剂,采用乳化化学交联技术制备表阿霉素脑用微球。用动态透析法研究微球的体外释放特性。结果:盐酸表阿霉素/壳聚糖的质量比为1∶9的载药微球形态良好,粒径分布较为均匀,平均粒径为(9.3±2.6)μm、载药量为(8.01±0.23)%、包封率为(72.9±2.2)%。体外释放具有良好的缓释效果。结论:所优化的制备工艺稳定,适用于脑用表阿霉素壳聚糖微球的制备。

OBJECTIVE To study the preparation technique and release characteristic of epirubicin-loaded chitosan microspheres for the cerebral administration. METHODS Using the liquid paraffin as oil phase,L-ascorbyl palmitate as cross linking agent,and span-80 as the emulsifier; epirubiein-loaded chitosan microspheres were achieved by emulsion-chemical cross link technique. Dynamic dialysis method was used to determine the releasing characteristic of microspheres in vitro. RESULTS Microspheres （epirubicin/chitosan 1： 9） with a good shape and narrow size distribution were prepared. The average diameter was （9. 3±2. 6）/μm. The ratio of drug loading was （8. 01 ± 0. 23）%. The ratio of entrapment was （72.9 ± 2.2）%. The drug release profile in vitro had a characteristic of good delayed release. CONCLUSION The optimized preparation technique is stable and has a high entrapment efficiency. So it could be used to prepare epirubicin-loaded chitosan microspheres for the cerebral administration.