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

作　　者：王小娟 杨宝乐 马川 何蕾 景临林 黄琼 马慧萍 WANG Xiaojuan;YANG Baole;MA Chuan;HE Lei;JING Linlin;HUANG Qiong;MA Huiping(College of Pharmacy,Gansu University of Chinese Medicine,Lanzhou730000,China;Department of Pharmacy,the 940th Hospital of Joint Logistics Support force of PLA,Lanzhou 730050,China;Department of Pharmacy,the First Affiliated Hospital of Xi’an Jiaotong University,Xi’an 710061,China)

机构地区：[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

出　　处：《浙江大学学报（医学版）》2024年第1期116-125,共10页Journal of Zhejiang University(Medical Sciences)

基　　金：国家自然科学基金(81571847,81872796);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)。

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。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 

分 类 号：R944[医药卫生—药剂学]