7-羟乙基白杨素聚乳酸-羟基乙酸共聚物纳米粒的制备及体外释放评价
Preparation of copolymer 7-hydroxyethyl chrysin loaded PLGA nanoparticles and the in vitro release
王小娟 1杨宝乐 1马川 1何蕾 2景临林 3黄琼 2马慧萍2
作者信息
- 1. 甘肃中医药大学药学院,甘肃 兰州 730000
- 2. 联勤保障部队第九四○医院药剂科,甘肃 兰州 730050
- 3. 西安交通大学第一附属医院药学部,陕西 西安 710061
- 折叠
摘要
目的:制备和评价7-羟乙基白杨素(7-HEC)聚乳酸-羟基乙酸共聚物(PLGA)纳米粒.方法:采用乳化溶剂挥发法制备7-HEC/PLGA纳米粒,以粒径、多分散系数(PDI)、包封率、载药量及Zeta电位为评价指标,通过单因素考察结合Box-Behnken响应面法优化处方.采用甘露醇作为冻干保护剂制备冻干粉,对最优处方制备的7-HEC/PLGA纳米粒进行表征及体外释放研究.结果:经Box-Behnken响应面法优化后的最优处方为:药载比2.12∶20,油水体积比1∶14.7,乳化剂为2.72%大豆磷脂.最优处方条件制备的 7-HEC/PLGA纳米粒的平均粒径为(240.28±0.96)nm、PDI为 0.25±0.69、包封率为(75.74±0.80)%、载药量为(6.98±0.83)%、电位为(-18.17±0.17)mV.体外释放48 h内累积释放度达到50%以上.结论:优化所得处方工艺稳定、操作简便.所得7-HEC/PLGA纳米粒粒度均匀,包封率较高.相对于7-HEC原料药,7-HEC/PLGA纳米粒的溶出度显著提高.
Abstract
Objective:To prepare 7-hydroxyethyl chrysin(7-HEC)loaded poly(lactic-co-glycolic acid)(PLGA)nanoparticles and to detect the in vitro release.Methods:The 7-HEC/PLGA nanoparticles were prepared by emulsification solvent volatilization method.The particle size,polydispersity index(PDI),encapsulation rate,drug loading and zeta potential were measured.The prescription was optimized by single factor investigation combined with Box-Behnken response surface method.Mannitol was used as protectant to prepare lyophilized powder,and the optimal formulation was characterized and studied for the in vitro release.Results:The optimal formulation of 7-HEC/PLGA nanoparticles was as follows:drug loading ratio of 2.12∶20,oil-water volume ratio of 1∶14.7,and 2.72%soybean phospholipid as emulsifier.With the optimal formulation,the average particle size of 7-HEC/PLGA nanoparticles was(240.28±0.96)nm,the PDI was 0.25±0.69,the encapsulation rate was(75.74±0.80)%,the drug loading capacity was(6.98±0.83)%,and the potentiostatic potential was(-18.17±0.17)mV.The cumulative in vitro release reached more than 50%within 48 h.Conclusions:The optimized formulation is stable and easy to operate.The prepared 7-HEC/PLGA nanoparticles have uniform particle size,high encapsulation rate and significantly higher dissolution rate than 7-HEC.
关键词
7-羟乙基白杨素/聚乳酸-羟基乙酸共聚物纳米粒/乳化溶剂挥发法/处方优化/体外释放Key words
7-hydroxyethyl chrysin/Poly(lactic-co-glyconlic acid)nanoparticles/Emulsion solvent evaporation method/Formulation optimization/In vitro release引用本文复制引用
基金项目
国家自然科学基金(81571847)
国家自然科学基金(81872796)
军队卫勤保障能力创新与生成专项计划(21WQ045)
甘肃省自然科学基金(22JR11RA011)
联勤保障部队第九四〇医院专项培育项目(2021yxky015)
出版年
2024
NETL
NSTL
维普
万方数据