首页|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

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

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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。
Preparation of copolymer 7-hydroxyethyl chrysin loaded PLGA nanoparticles and the in vitro release
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.

7-hydroxyethyl chrysinPoly(lactic-co-glyconlic acid)nanoparticlesEmulsion solvent evaporation methodFormulation optimizationIn vitro release

王小娟、杨宝乐、马川、何蕾、景临林、黄琼、马慧萍

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甘肃中医药大学药学院,甘肃 兰州 730000

联勤保障部队第九四○医院药剂科,甘肃 兰州 730050

西安交通大学第一附属医院药学部,陕西 西安 710061

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

国家自然科学基金国家自然科学基金军队卫勤保障能力创新与生成专项计划甘肃省自然科学基金联勤保障部队第九四〇医院专项培育项目

815718478187279621WQ04522JR11RA0112021yxky015

2024

10.3724/zdxbyxb-2023-0233

浙江大学学报(医学版)
浙江大学

浙江大学学报(医学版)

CSTPCD北大核心
影响因子：0.926
ISSN：1008-9292
年,卷(期)：2024.53(1)
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