论文部分内容阅读
目的:制备去甲斑蝥素壳聚糖-丝素蛋白栓塞微球(Norcantharidin-loaded chitosan-fibroin micro-spheres for embolization,NCTD-CS-SF-MS),考察其包封率,载药量及外观形态,并对其体外释放特性进行考察。方法:采用乳化-交联固化法制备NCTD-CS-SF-MS,其中以液体石蜡为油相,壳聚糖(chitosan CS)与丝素蛋白(silk fibroin SF)的物理混合溶液为水相,Span-80为乳化剂,戊二醛为交联剂。星点设计-效应面法优化制备工艺,扫描电镜观察微球表面形态及X-射线衍射(XRD)、差示量热扫描(DSC)表征微球特性。采用体外动态透析法测定微球在不同介质条件下的释药性能。结果:制备的微球形态圆整,大小均匀,平均粒径约(184±5)μm,载药量(15.08±2.85)%,包封率(27.46±1.25)%。微球在0.1 mol.L-1 HCl、PBS(pH=7.4)和生理盐水中的释放均遵循Weibull方程。结论:所优化的制备工艺简单易行,缓释作用显著。
OBJECTIVE: To prepare norcantharidin-loaded chitosan-fibroin micro-spheres for embolization (NCTD-CS-SF-MS) and study its encapsulation efficiency, drug loading and appearance Morphology, and its in vitro release characteristics were investigated. Methods: NCTD-CS-SF-MS was prepared by emulsion-crosslinking method. The liquid phase was composed of liquid paraffin oil, chitosan CS and silk fibroin SF. Span-80 as emulsifier, glutaraldehyde as crosslinking agent. The design of star spots-response surface methodology was used to optimize the preparation process. The surface morphology, X-ray diffraction (XRD) and differential scanning calorimetry (DSC) of the microspheres were characterized by scanning electron microscopy. The in vitro dynamic dialysis method was used to determine the release properties of microspheres under different media conditions. Results: The prepared microspheres were round and uniform in size. The average diameter of the microspheres was about (184 ± 5) μm. The drug loading was 15.08 ± 2.85% and the encapsulation efficiency was 27.46 ± 1.25%. The release of microspheres in 0.1 mol·L-1 HCl, PBS (pH = 7.4) and saline followed the Weibull equation. Conclusion: The optimized preparation process is simple and easy, slow-release effect is significant.