含RGD修饰的丹参酮ⅡA多级靶向纳米粒的质量评价

Preparation and characterization of TSⅡA-loaded mPEG-PLGA-PLL-cRGD nanoparticles

目的探讨丹参酮ⅡA多级靶向纳米粒的制备及其质量评价。方法采用乳化溶剂蒸发法制备丹参酮ⅡA多级纳米粒;测定丹参酮ⅡA多级靶向纳米粒的粒径分布及纳米微粒表面结构;并检测丹参酮ⅡA多级靶向纳米粒的载药量、包封率及体外药物释放规律。结果课题组制备的丹参酮ⅡA多级靶向纳米粒,大小均匀,载药纳米粒的平均粒径为190nm,Zeta电位为4.3mV,包封率(94.12±5.20)%,载药量(2.05±0.12)%。与游离的丹参酮ⅡA单体相比,丹参酮ⅡA多级靶向纳米粒释放速度明显减慢,在120h累积释放量为72.59%。结论采用乳化溶剂蒸发法成功制备了含RGD修饰的丹参酮ⅡA多级靶向纳米粒。与丹参酮ⅡA单体相比,制备成纳米制剂后,多级靶向载药纳米粒能随着时间的延长将药物逐步释放出来,具有良好的缓释特征。

Objective To prepare and evaluate the novel polymeric nanoparticles containing Tanshinon Ⅱ A （TS Ⅱ A-mPEG-PLGA-PLL-cRGD NPs, TNP）. Methods TNP was prepared by using a emulsion/solvent evaporation method. The size, shape, zeta, drug loading, encapsulation efficiency, and release of these nanoparticles were studied in vitro. Results TNP were of uniform size with an average particle size of 190nm and zeta potential of 4.3mV.The encapsulation efficiency was （94.12 ±5.20）% and the drug load was （2.05 ±0.12）%. It showed that the release curve of TNP was prolonged. Conclusion TNP was stable and had a slow-releasing and tumor targeting effect.