姜黄素固体脂质纳米粒制备及质量评价.doc

姜黄素固体脂质纳米粒制备及理化性质研究 邓睿园 1，宋金春2,吕桦1（1.武汉大学药学院，湖北 武汉 430072；2.武汉大学人民医院药学部，湖北 武汉430060） 摘 要 目的: 以姜黄素为模型药物，山嵛酸甘油酯为载体材料制备姜黄素固体脂质纳米粒，并考察其质量和性质。方法：用乳化蒸发一低温固化技术制得了姜黄素固体脂质纳米拉，以单因素考察和正交设计法筛选处方和工艺, 并对其形态、粒径、表面电位、包封率、体外释药特等进行了研究。结果: 所得脂质纳米粒为类圆球状,粒径分布较均匀。样品粒径为(134±5)nm,包封率为(67.4±1.3)%,平均Zeta电位值为(-23.5±1.5)mV。药物体外释放符合Higuchi方程。结论: 选择乳化蒸发—低温固化法制备姜黄素固体脂质纳米粒方法可行,为开发姜黄素新型注射制剂提供了实验依据。 关键词 姜黄素；固体脂质纳米粒；乳化蒸发—低温固法；理化性质 Preparation and Physico-chemical Property of Curcumin solid lipid nanoparticles DENG rui-yuan1,SONG Jin-chun2, LV hua 1 (1.College of pharmacy, Wuhan university, Wuhan 430072, China ；2.Department of pharmacy, Renmin Hospital of Wuhan university, Wuhan 430060,china) ABSTRACT：OBJECTIVE To prepare the Curcumin solid lipid nanoparticles with docosanoic acid glycerol ester and investigate their quality and characteris .METHODS The method of emulsification evaporation- solidification at low temperature was used to the solid lipid nanoparticles (SLN) containing curcumin. the formula and technology were optimized by the single factor exploration and orthogonal design. Its morphology and particle size were examined by transmission electron microscope. Entrapment efficiency, Zeta potential, and the release of curcumin in vitro were studied. RESULTS The Cur -SLN assumed spherical shape.Its distribution of diameter was even with average particle size (134±5) nm. Entrapment efficiency was (67.4±1.3)%. The Zeta potential was(-23.5±1.5)mV . The release of curcumin in vitro conformed to Higuchi Equation. CONCLUSION: The selected preparation technique of Cur-SLN is rational and practicable. It provides experimental evidence for developing a new curcumin injection. KEY WORDS :curcumin; solid lipid nanoparticles; emulsion evaporation-solidification at low temperature; Physico-chemical property 姜黄素(Curcumin)是我国传统中药姜黄(Curcumin long L.)的主要活性成分，近年来，对姜黄素抗癌作用的实验研究表明,姜黄素可抑制肿瘤细胞的生长[1]，且抗癌谱广,毒副作用小,是一种具有良好应用前景的抗癌新药。但姜黄素水溶性差，在机体内难吸收，易代谢（口服生物利用度低,大部分以原形排出体外约89%)在体外也容易被氧化[2]，由于上述原因，为姜黄素的临床应用带来了一定的难