紫花牡荆素壳聚糖微球的制备及体外释药性能考察

Preparation of Casticin Chitosan Microspheres and Investigation of Its in Vitro Release Properties

目的:制备紫花牡荆素壳聚糖微球,优化其制备工艺,并考察其体外释放性质。方法:以山梨糖醇酐单油酸酯和聚山梨酯-80为乳化剂,液体石蜡为油相,戊二醛作交联剂,采用乳化交联法制备紫花牡荆素壳聚糖微球。利用Design-Expert8.0.6软件优化紫花牡荆素壳聚糖微球的制备工艺,扫描电镜观察目标微球形态,动态透析法检测目标微球的体外释药性能。结果:紫花牡荆素壳聚糖微球最佳制备工艺条件为油水相比例6∶1,交联时间3 h,转速1 400 r·min^(-1);目标微球形态较圆整、粒径分布较为均匀,平均粒径7.92μm,载药量29.20%,包封率39.23%。紫花牡荆素壳聚糖微球在4 h的药物累计释放率26.75%,之后释药平缓,释放变慢,48 h的药物累计释放率95%。微球在磷酸盐缓冲溶液(pH 7.4)中的释放遵循Higuchi方程。结论:优化的制备工艺简单易行。紫花牡荆素壳聚糖微球载药量较高,具有一定的缓释作用。

Objective： To optimize preparation process of casticin chitosan microspheres and investigate its in vitro release characteristics. Method： Casticin chitosan microspheres were achieved by emulsion crosslinking method,taking liquid paraffin as oil phase, span-80 and tween-80 as emulsifier, and glutaraldehyde as crossinking agent. Design-Expert 8. 0. 6 software was applied to optimize preparation procedure. Morphology of the microspheres was observed by scanning electron microscope（ SEM）. Dynamic dialysis method was used to determine in vitro release characteristic of casticin chitosan microspheres. Result： Optimum preparation process of microspheres was as following： ratio of oil phase to water phase of 6 ∶1,crosslinking time of 3 h,rotation rate of1 400 r·min- 1. Casticin chitosan microspheres had rounded shape and uniform particle size distribution, its average diameter was 7. 92 μm,drug-loading was 29. 20% and encapsulation efficiency was 39. 23%. Release behavior of casticin chitosan microspheres was described by Higuchi model in phosphate buffer solution with pH of 7. 4. Cumulative release amounts of casticin chitosan microspheres in 4 h and 48 h were 26. 75% and 95%,respectively. Conclusion： This optimized preparation process is feasible and simple, casticin chitosan microspheres has high drug-loading with a sustained-release effect.