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目的:制备具有靶向性的雷公藤甲素叶酸-壳聚糖纳米粒,并考察其体外释药性能。方法:以粒径和PDI为指标,采用单因素试验和正交试验法,考察溶液pH值、反应温度、壳聚糖和多聚磷酸钠的比例及质量浓度对壳聚糖纳米粒的制备工艺的影响;通过雷公藤甲素与壳聚糖的偶联比及雷公藤甲素、叶酸活性酯和壳聚糖上的氨基反应确定最佳制备工艺,采用离子交联法制备雷公藤甲素叶酸-壳聚糖纳米粒。采用HPLC考察其体外释药特性。结果:最佳制备工艺为反应温度25℃,溶液pH 3.5,壳聚糖-多聚磷酸3∶1,壳聚糖与多聚磷酸钠的质量分数均为0.3%,制得的纳米粒平均粒径约170 nm,粒子分散指数(PDI)约0.21。载药纳米粒的释放率于4 h后达平衡,最大释药率约68%。结论:按优选工艺制备的雷公藤甲素叶酸-壳聚糖纳米粒质量稳定可靠,优选的工艺简便易行。
OBJECTIVE: To prepare targeting triptolide-loaded chitosan nanoparticles and study its in vitro drug release properties. Methods: The particle size and PDI as an indicator, the single factor test and the orthogonal test method, investigated the solution pH value, reaction temperature, the proportion of chitosan and sodium polyphosphate and the concentration of mass concentration of chitosan nanoparticles preparation process The optimal preparation process was determined by the coupling ratio between triptolide and chitosan and the amino groups on triptolide, folate active ester and chitosan. The triptolide folic acid Chitosan Nanoparticles. Using HPLC to investigate its in vitro release characteristics. Results: The optimum preparation conditions were as follows: the reaction temperature was 25 ℃, the pH was 3.5, the mass ratio of chitosan to polyphosphate 3:1, chitosan and sodium polyphosphate were both 0.3% Diameter of about 170 nm, particle dispersion index (PDI) of about 0.21. The release rate of drug-loaded nanoparticles reached equilibrium after 4 h, and the maximum release rate was about 68%. Conclusion: The triptolide-chitosan nanoparticles prepared by the optimized process are stable and reliable, and the preferred process is simple and easy.