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脑源性神经营养因子缓释注射纳米粒的制备及其释药特性评价
史国栋1,贾连顺1,袁文1,史建刚1*,谭俊铭1,储藏2
0
(1.第二军医大学长征医院骨科,上海 200003;2.第二军医大学药学院药剂学教研室,上海 200433)
摘要:
目的:制备稳定性高、粒径小的脑源性神经营养因子(BDNF)缓释注射纳米粒,并评价其释药过程。方法:采用乳酸-羟基乙酸共聚物(PLGA)为载体材料,复乳化溶剂挥干法制备载有BDNF的PLGA纳米粒。优化纳米粒处方和制备工艺,观察纳米粒的形态、大小和粒径分布,评价其回收率、精密度、重复性、包封率以及体外释药特性。结果:优选处方选择理论载药量1%、聚合物浓度3.3 mg/ml、超声时间为40 s,甘露醇为支架剂。BDNF纳米粒呈圆形,大小均匀,平均粒径为156.7 nm。制备的纳米粒回收率、精密度、重复性和包封率较高,缓慢溶蚀释放为其主释药过程,时间达30 d。结论:成功制备的BDNF缓释注射纳米粒具有稳定性好、包封率高的特点。
关键词:  脑源性神经营养因子  缓释制剂  纳米粒
DOI:10.3724/SP.J.1008.2008.00538
投稿时间:2007-10-08修订日期:2008-01-25
基金项目:国家自然科学基金(30300359),上海市自然科学基金(07JC14072).
Preparation of injectable sustained-release nanoparticles carrying brain-derived neurotrophic factor and evaluation of their drug releasing characteristics
SHI Guo-dong1,JIA Lian-shun1,YUAN Wen1,SHI Jian-gang1*,TAN Jun-ming1,CHU Cang2
(1.Department of Orthopedics,Changzheng Hospital,Second Military Medical University,Shanghai 200003,China;2.Department of Pharmacy,School of Pharmacy,Second Military Medical University,Shanghai 200433)
Abstract:
Objective:To prepare stable, small-sized injectable sustained-release nanoparticles harboring brain-derived neurotrophic factor (BDNF) and to evaluate its drug releasing process.Methods: The nanoparticles were prepared using poly(D,L-lactic-co-glycolic acid) (PLGA) as the carrier by w/o/w double emulsion-solvent evaporation method.The formula and technique were optimized; the shape,size and the distribution of the diameters of the particles were observed; and recovery rate,precision,repeatability,encapsulation efficiency,and drug releasing characteristics were assessed.Results: With the optimized formula,the drug loading rate was 1%,the polymer concentration was 3.3 mg/ml, and the ultrasound time was 40 s; mannitol was used as the supporting agent.BDNF nanoparticles were round,homogenous in size,with a mean diameter of 156.7 nm.The prepared particles had high recovery rate,precision,repeatability,and encapsulation efficiency.The drug release was characterized by slow corrosion and the process lasted for 30 days.Conclusion: We have successfully prepared slow-release nanoparticles harboring BDNF,which are stable and have high encapsulation efficiency.
Key words:  brain-derived neurotrophic factor  sustained-release preparations  nanoparticles