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目的制备壳聚糖修饰雷公藤多苷纳米粒(LMWC-TG-NPs),并研究其体外释药行为。方法采用改良的自乳化溶剂扩散法制备LMWC-TG-NPs;正交试验设计优化雷公藤多苷纳米粒(TG-NPs)处方,单因素试验考察壳聚糖(LMWC)修饰方式;以含20%乙醇的PBS(pH 7.4)为释放介质考察LMWC-TG-NPs的体外释药行为。结果优化的处方工艺:以1.0%Poloxamer 188、80 mg PLA、12 mL有机相、丙酮-乙醇(2∶3)制备TG-NPs混悬液,以与TG-NPs混悬液等体积的10%LMWC溶液修饰TG-NPs制备LMWC-TG-NPs;根据优化条件制备的LMWC-TG-NPs,外观呈圆形或类圆形,平均粒径为(207.6±3.4)nm,多分散指数(PDI)为0.078±0.009(n=3),包封率和载药量分别为(61.83±2.43)%、(10.70±0.37)%(n=3);体外释药符合Higuchi方程。结论所制备的LMWC-TG-NPs包封率较高,粒径小,体外释药具有明显的缓释特征,为后期研究其肾脏靶向和毒性奠定了基础。
Objective To prepare chitosan-modified wilt glycoside nanoparticles (LMWC-TG-NPs) and study its in vitro release behavior. Methods LMWC-TG-NPs were prepared by a modified self-emulsifying solvent diffusion method. Orthogonal design was used to optimize the formulation of TG-NPs. Single factor experiments were conducted to investigate the modification of LMWC. % Ethanol in PBS (pH 7.4) as the release medium to investigate the in vitro release behavior of LMWC-TG-NPs. Results Optimized Prescription Processes TG-NPs suspensions were prepared with 1.0% Poloxamer 188, 80 mg PLA, 12 mL organic phase, acetone-ethanol (2: 3) LMWC-TG-NPs were prepared by modifying TG-NPs with LMWC solution. The morphology of LMWC-TG-NPs was round or round with average diameter of 207.6 ± 3.4 nm and polydispersity index (PDI) The encapsulation efficiency and drug loading were (61.83 ± 2.43)% and (10.70 ± 0.37)% (n = 3), respectively. The in vitro drug release conformed to the Higuchi equation. CONCLUSION: The prepared LMWC-TG-NPs have high entrapment efficiency, small particle size and obvious sustained release characteristics in vitro, which lays a foundation for further studies on the targeting and toxicity of LMWC-TG-NPs.