载姜黄素甲氧基聚乙二醇-聚谷氨酸-胆固醇共聚物纳米粒的制备及表征  

Preparation and characterization of curcumin-loaded methoxy poly(ethylene glycol)-block-poly(γ-cholesterol-l-glutamate) nanoparticles

作　　者：樊春梅[1] 李慧莉[2] 何黎黎[3] 贺英菊[1] 何谷[2] 宋相容[2] 

机构地区：[1]四川大学华西药学院,成都610041 [2]四川大学华西医院生物治疗国家重点实验室,成都610041 [3]西南民族大学化学与环境保护工程学院,成都610041

出　　处：《中国新药杂志》2015年第19期2251-2256,共6页Chinese Journal of New Drugs

基　　金：国家自然科学基金(81302729);四川大学优秀青年学者基金(2013SCU04A19)

摘　　要：目的:制备载姜黄素(curcumin,Cur)的甲氧基聚乙二醇-聚谷氨酸-胆固醇共聚物(m PEGPCLG)纳米粒(Cur-NP),并评价其制剂学相关性质。方法:采用O/W乳化-溶剂挥发法制备Cur-NP,以粒径、包封率和载药量为综合评价指标,通过单因素试验法优化Cur-NP的处方及制备工艺;利用透射电镜和动态透析法考察最优处方制得的Cur-NP的形态和体外释放特性。结果:用最优处方工艺制备的Cur-NP呈球形或类球形,平均粒径、Zeta电位、包封率和载药量分别为(171±11)nm,(-1.68±0.34)m V,(95.51±2.30)%和(48.85±0.60)%;体外释放速率在p H 5.5条件下较p H 7.4略快,96 h累积释放率分别为63.91%和51.68%。结论:由O/W乳化-溶剂挥发法制得的Cur-NP粒径小,包封率和载药量高;体外释药缓慢并具有一定的p H依赖性;m PEG-PCLG可作为包载难溶性药物姜黄素的一种新型理想纳米载体材料,值得进一步深入研究。Objective： To prepare curcumin-loaded methoxy poly（ ethylene glycol）-block-poly（ γ-cholesterol-l-glutamate） copolymer（ m PEG-PCLG） nanoparticles（ Cur-NP） and study the related pharmaceutical properties. Methods： Cur-NP was prepared by O/W single emulsion-solvent evaporation method and the processing parameters were optimized by single-factor test using particle size,entrapment efficiency and drug loading as indicators. The optimal Cur-NP was observed by TEM and the in vitro release behavior was investigated through dynamic dialysis method. Results： The optimal Cur-NP was approximately spherical,with the average size of（ 171 ± 11） nm and zeta potential of（- 1. 68 ± 0. 34） m V. The entrapment efficiency and drug loading were（ 95. 51 ± 2. 30） %and（ 48. 85 ± 0. 60） %,respectively. Curcumin was released out of nanoparticles slightly faster at p H 5. 5 than p H7. 4,and the accumulated release rates reached 63. 91% and 51. 68% at 96 h,respectively. Conclusion： The prepared Cur-NP has small particle size and high entrapment efficiency and loading rate. It can release curumin slowlyin a p H-dependent manner. Thus,m PEG-PCLG may be one novel and promising biomaterial as Cur-NP carrier and is worthy of further investigation.

关 键 词：姜黄素 纳米粒 甲氧基聚乙二醇-聚谷氨酸-胆固醇 

分 类 号：R943.42[医药卫生—药剂学] R979.1[医药卫生—药学]