多柔比星聚羟基丁酸酯微球的制备和体外性质

Preparation of Doxorubicin-loaded Poly(β-hydroxybutyrate) Microspheres and Its Properties in vitro

目的制备具有缓释特性和可生物降解性的多柔比星聚β-羟基丁酸酯微球。方法以生物可降解性材料聚β-羟基丁酸酯为载体,液中干燥法制备多柔比星微球,并对其表面特征、载药量、包封率、粒径、跨距、体外释放、灭菌的影响进行考察。结果所得微球呈桔红色,外观圆整,分散性好;载药量为1.01%,包封率为16.79%,平均粒径为43.13μm,跨距为1.45;微球体外释放呈现3个不同阶段,60d累计释放率达65%;灭菌剂量低于6kGy时,灭菌后仍有菌落检出,当灭菌剂量>12kGy时材料和药物的性质有改变,剂量以9kGy为宜。结论微球具有缓释长效作用,是一类有前途的治疗增殖性视网膜病变的制剂。

Purpose To prepare biodegradable poly-β-hydroxybutyrate(PHB) microspheres containing doxorubicin with long release. Methods Doxorubicin microspheres were prepared by an in-liquid drying method,using PHB as their device.And its properties were tested,including drug loading,loading efficiency,mean diameter,span of dispersity,accumulative release and an influence of the irradiation. Results Microspheres prepared were orange,smooth and spherical.Drug loading,loading efficiency,mean diameter and span of dispersity were 1.01%,16.79%,43.13 μm and 1.45.The release in vitro appeared as there different periods and the accumulative release of the microspheres reached 65% during 60 days.When the dosage of irradiation was below 6 kGy,the virus could still be tested,but when the dosage was above 12 kGy,the pro-perties of doxorubicin and PHB changed,the most proper dosage was 9 kGy. Conclusions The microspheres obtained can release in a long time in vitro,leading to a prosperity in curing proliferative vitreous retinopathy in clinical use.