褪黑素载药纳米粒的优化设计及研制

Preparation and design of nanoparticles loaded with melatonin

目的 :探讨采用复合乳液 -溶剂挥发法制备褪黑素载药纳米粒的最佳工艺条件。方法 :以聚乳酸、壳聚糖可降解生物材料为载体 ,明胶为分散剂 ,span - 80和tween - 80混合液为微乳液 ,根据微粒的表面形态、粒径大小分布、包封率、载药量选择最佳工艺条件 ,制备褪黑素载药纳米粒。结果与结论 :原子力显微镜下可见纳米粒表面圆滑 ,分布均匀。正交设计效应曲线图直观分析和方差分析结果显示 ,搅拌速度、溶剂挥发温度、聚乳酸与褪黑素投药比、壳聚糖浓度是影响制备工艺的主要因素。在 30℃ ,10 0 0r/min搅拌速度 ,搅拌时间 4 5min ,m(褪黑素 ) :m(聚乳酸 )为 1:5 ,V(Tween - 80 ) :V(Span - 80 )为 5 :1,壳聚糖质量浓度为 1%条件下 ,可制备成平均粒径为 4 5 .84nm ,包封率为 38.33% ,载药量为 8.35

Aim: To select the best method to prepare nanoparticles loaded with melatonin by co-emulsification-solvent evaporation technique. Methods: Based on the poly-lactic acid and chitosan as biodegradable carrier, glutin was used as dispersion, microemulsion was preparated by mixing Span-80 with Tween-80. According to shapes, sizes of particles, dispersion, rate of drug loading, entrapment efficiency, and character of nanoarticles, the best technique to prepare nanoparticles loaded with melatonin was selected. Results and Conclusion: AFM(atomic force microscope probe) showed glaze of nanoparticles and uniformity of dispersion. Effective curve and analysis of variance showed that stirring speed, reaction temperature, ratio of poly-lactic acid and melatonin, concentration of chitosan were the main factors. MT-NPs could be prepared according to optimum factors described below as reaction temperature at 30 ℃, stirring speed at 1 000 r/min, stirring time for 45 min, ratio of MT and PLA to 1:5, ratio of Tween-80 and Span-80 to 5:1, concentration of CS 1% with the average particle sizes 45.84 nm, entrapment efficiency of 38.33%, and drug loading of 8.35%.