盐酸维拉帕米PLGA纳米粒的成型工艺及制剂学性质研究  

Preparation and characterization of Verapamil hydrochloride loaded PLGA nanoparticles

作　　者：龚道琼[1] 尹宗宁[1] 宋相容[2] 何治尧[1] 侯世祥[1] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]四川大学生物治疗国家重点实验室,四川成都610041

出　　处：《华西药学杂志》2009年第6期583-586,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金(批准号:30772668);863高新技术研究发展计划重点项目(2007AA021810)

摘　　要：目的优化影响盐酸维拉帕米乳酸/羟基乙酸共聚物(PLGA)纳米粒成型工艺的参数,并评价优化工艺后所制纳米粒的制剂学性质。方法采用O/W超声乳化-溶剂挥发法制备盐酸维拉帕米PLGA纳米粒(VRP-PLGANP),以粒径、包封率和载药量为评价指标,采用单因素试验系统考察PLGA浓度、PLGA/VRP质量比、PVA浓度、有机相中丙酮浓度、外水相pH、内外相(O/W)体积比、探头超声时间、旋蒸时间共8个参数对纳米粒成型工艺的作用规律。结果用优化处方工艺制备的纳米粒的包封率和载药量分别为65.78%±6.32%和22.75%±1.48%、平均粒径为150.4±6.9nm、PDI=0.070±0.018(n=3),体外释放规律符合Weibull方程,具有一定的缓释特性。结论所用方法可用于制备载两亲性药物的PLGA纳米粒。OBJECTIVE To optimize the processing parameters of Verapamil hydrochloride loaded PLGA nanopartieles （ VRP - PL- GANP） and study the characterization of the optimal VRP - PLGANP. METHODS Eight processing parameters were assessed systematically to enhance the VRP incorporation into PLGA nanoparticles and minimize the particle size, including PLGA concentration in the organic phase, PLGA/VRP mass ratio, PVA concentration in the aqueous phase, acetone concentration in the organic phase, aqueous phase pH, aqueous to organic phase volume ratio, sonication time, removal time of organic solvents. RESULTS The VRP - PLGANP produced by optimal formulation were submicron size 150.4±6.9 ran, n = 3 and of low polydispersity （ 0. 070 ±0. 018, n = 3 ） ,with the entrapment efficiency （EE） and drug loading （DL） of 65.78% ±6, 32% and 22.75 % ±1.48% respectively. The in vitro releasing curves with sustained - release properties could be simulated by Weibull equation. CONCLUSION Amphiphilie drug loaded PLGA nanopartieles could be prepared by O/W emulsion solvent evaporation.

关 键 词：维拉帕米 乳酸/羟基乙酸共聚物 纳米粒 乳化-溶剂挥发法 

分 类 号：R94[医药卫生—药剂学]