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目的:研究利用壳聚糖(chitosan,CS)和良好生物相容性的丝素蛋白(silk fibroin,SF)为载体,去甲斑蝥素(norcantharidin,NCTD)为模型药物,制备去甲斑蝥素壳聚糖-丝素蛋白微球(norcantharidin-chitosan-silk fibroin-microspheres,NCTD-CS-SF-MS)。并考察微球的载药量、包封率及微球表面形态以及微球的体外释放特性。方法:以液体石蜡为油相,壳聚糖与丝素蛋白的物理混合溶液为水相,Span-80为乳化剂,戊二醛为交联剂;采用乳化-交联固化法制备NCTD-CS-SF-MS。星点设计优化制备工艺,扫描电镜,观察微球表面形态及X-射线粉末衍射法(X-ray power diffraction,X-RD)和差示扫描量热法(differential scanning calorimetry,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NCTD-CS-SF-MS形态圆整,粒径分布较为均匀,平均粒径约(184.0±5.0)μm,载药量(15.08±2.85)%,包封率(27.46±1.25)%。NCTD-CS-SF-MS在0.1mol/L HCl,PBS(pH=7.4)和9.0mg/mL氯化钠溶液的3种介质中的释放均遵循Weibull方程。结论:优化的NCTD-CS-SF-MS制备工艺简单易行,载药量高,缓释作用良好。
OBJECTIVE: To study the effects of chitosan (CS) and silk fibroin (SF) with good biocompatibility as carrier and norcantharidin (NCTD) as model drug to prepare norcantharidin shell Norcantharidin-chitosan-silk fibroin-microspheres (NCTD-CS-SF-MS). The drug loading, entrapment efficiency, surface morphology of microspheres and in vitro release characteristics of microspheres were investigated. Methods: Liquid paraffin as the oil phase, the chitosan and silk fibroin physical mixing solution as the water phase, Span-80 as emulsifier, glutaraldehyde as cross-linking agent; using emulsion-crosslinking curing NCTD-CS -SF-MS. The optimized preparation process of star spots, scanning electron microscopy, surface morphology of microspheres and X-ray diffraction (X-RD) and differential scanning calorimetry (DSC) Properties; in vitro dynamic dialysis method to determine the release of microspheres in different media conditions. Results: The morphology of NCTD-CS-SF-MS was uniform and the average particle diameter was (184.0 ± 5.0) μm. The drug loading was 15.08 ± 2.85% and the encapsulation efficiency was 27.46 ± 1.25. %. The release of NCTD-CS-SF-MS in all three media of 0.1 mol / L HCl, PBS (pH = 7.4) and 9.0 mg / mL sodium chloride solution follows the Weibull equation. Conclusion: The optimized preparation process of NCTD-CS-SF-MS is simple and easy, with high drug loading and good sustained release.