注射用姜黄色素纳米脂质载体的制备及其质量评价  

Preparation and in vitro characterization of curcuminoids-loaded nanostructured lipid carriers for intravenous injection

作　　者：肖衍宇[1,2] 陈曦[1] 邹浪[3] 陈志鹏[4] 平其能[1,2] 

机构地区：[1]中国药科大学药剂学教研室,南京210009 [2]中国药科大学天然药物活性组分与功效国家重点实验室,南京210009 [3]江西中医学院附属医院,南昌330006 [4]南京中医药大学药学院,南京210046

出　　处：《中国新药杂志》2013年第9期1088-1093,1099,共7页Chinese Journal of New Drugs

基　　金：中央高校基本科研业务费专项资金(JKP2011005);国家基础科学人才培养基金(J0630858);天然药物活性组分与功效国家重点实验室(中国药科大学)资助项目(SKLNMKF201204)

摘　　要：目的:制备适用于静脉注射给药的姜黄色素纳米脂质载体(curcuminoids-loaded nanostructured lipid carriers,Cur-NLC)用于脑胶质瘤的治疗,并对其理化性质和体内安全性进行初步研究。方法:采用熔融-乳化法制备Cur-NLC,以姜黄素(Cur I)的含量为代表,以包封率为指标,通过正交试验设计优化处方。考察Cur-NLC的形态、粒径、电位、包封率、体外释药行为以及体外溶血性,为进一步的研究奠定基础。结果:优化条件下制备的Cur-NLC多为类球形粒子,平均粒径(187.5±4.7)nm,Zeta电位(-23.7±2.9)mV,包封率、载药量分别为(98.3±0.4)%和(4.6±0.2)%。Cur-NLC体外释放具有明显的缓释特征,36 h累积释放百分数为19.2%,释药行为符合一级方程。溶血性研究表明,Cur-NLC具有较高的安全性。结论:制备的Cur-NLC粒径小,药物包封率高,安全性好,有望实现药物在体内的缓慢释药,提高药物的生物利用度,增加在脑胶质瘤部位的浓集。Objective： To develop an appropriate nanostructured lipid carrier of eurcuminoids （Cur-NLC） for intravenous injection to target brain, and investigate its in vitro physicochemical properties and injection safety. Methods： The melt-emulsification method was chosen to prepare Cur-NLC. The formulation was optimized by orthogonal design. The morphology, the mean particle size, zeta potential, encapsulation efficiency and in vitro release of Cur-NLC were observed, and the hemolytic experiment of the optimal formulation was carried out. Results ： The obtained Cur-NLC was approximately spherical in shape with average particle size of （187.5± 4.7） nm and zeta potential of （ - 23.7 ±2.9） mV. The drug loading and encapsulation efficiency were （4.6 ±0.2） % and （98.3 ±0.4） % , respectively. The in vitro release of the drug from Cur-NLC was slowed down and the drug release behavior conformed to well fit the first order equation. Cur-NLC injection did not induce hemolysis. Conclusion： Cur-NLC has advantages of small particle sizes, high encapsulation efficiency, slow release and good safety.Thus, it would be a promising nanocarrier for intravenous injection to achieve the slow release of the drug in the body, improve the bioavailability of the drug and increase the concentration of the drug at the brain tumor site.

关 键 词：姜黄色素 纳米脂质载体 静脉注射 理化性质 溶血性 

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