槲皮素PLGA-TPGS纳米粒处方筛选及体外稳定性  

Formulation Screening and in vitro Stability of Quercetin-loaded PLGA-TPGS Nanoparticles

作　　者：徐红[1] 高萌[2] 关欣[2] 董浩[2] 董仁超 丛中笑 张成鸿[1] 田燕[2] 

机构地区：[1]大连医科大学基础医学院,大连116044 [2]大连医科大学药学院,大连116044 [3]大连医科大学2013级临床药学专业,大连116044

出　　处：《医药导报》2018年第3期345-350,共6页Herald of Medicine

基　　金：辽宁省自然科学基金资助项目(2015020308)

摘　　要：目的采用正交实验法筛选制备槲皮素乳酸羟基乙酸共聚物-维生素E聚乙二醇1000琥珀酸酯(PLGATPGS)纳米粒(QPTN)的最佳处方和制备工艺,并对QPTN进行体外稳定性考察。方法采用单一因素方法分别考察主药槲皮素与载体比例、乳化剂TPGS溶液浓度、超声功率、超声时间对QPTN粒径、载药量、包封率的影响。在单一因素实验基础上通过正交实验筛选制备QPTN的最佳处方和工艺,并制备6批QPTN。通过影响因素、加速、长期实验考察其中3批QPTN的体外稳定性。结果制备QPTN的最佳处方及工艺是槲皮素与载体比例为3∶10,TPGS溶液的浓度为0.05%,超声功率为200 W时超声6 min。在该条件下制备6批QPTN的平均粒径、载药量和包封率分别为(155.4±2.7)nm、(21.6±1.5)%和(93.7±2.9)%。体外稳定性实验中,QPTN在影响因素、加速、长期实验条件下稳定性良好。结论确定了制备QPTN的最佳处方和工艺,自制QPTN粒径较小,载药量和包封率较高,体外显示具有良好的稳定性。Objective To study the best formulation and technology of quercetin-loaded polylactic-co-glycolic acid-D-α-tocopheryl polyethylene glycol 1000 succinate( PLGA-TPGS) nanoparticles( QPTN) with QT as model drug and PLGA-TPGS as polymer materials by orthogonal tests,and to investigate the in vitro stability of QPTN. Methods To ensure the best formulation and technology for preparing QPTN,single-factor test was established to determine the influence of the ratio of quercetin to PLGA-TPGS,the concentration of TPGS as emulsifiers,the ultrasonic power and ultrasonic time to the particle size,drug loading( DL) and entrapment efficiency( EE).According to single-factor test,the factor levels of nanoparticles were set to select the best prescription and technology of QPTN by orthogonal test.The stability of QPTN was examined using the effecting factor test,acceleration test and long-term test. Results The best formulation and technology of QPTN was that the ratio of quercetin to PLGATPGS was 3∶10( W∶W) with 0. 05% TPGS as emulsifier,the mixed solution was sonicated for 6 min at 200 W. The average particle size,DL and EE of QPTN prepared under the conditions described above were( 155. 4 ± 2. 7) nm,( 21. 6 ± 1. 5) % and( 93.7±2.9) %( n= 6),respectively.In the in vitro stability test,QPTN showed a good stability at high temperature,high humidity and strong light condition. Conclusion The best formulation and preparation technology of QPTN was selected.QPTN got small particle size,high DL and EE,and good in vitro stability.

关 键 词：槲皮素 纳米粒 乳酸羟基乙酸共聚物-维生素E聚乙二醇1000琥珀酸酯 稳定性 

分 类 号：R979[医药卫生—药品] TQ460.1[医药卫生—药学]