PEG修饰的氟苯尼考PLGA纳米粒制备及其体外释放性能研究  

Preparation of PEG-modified florfenicol PLGA nanoparticles and the study on their in vitro release properties

作　　者：陈媛 李姝琪 高崇凯 易军 李晓芳 吴芳 郭波红 CHEN Yuan;LI Shuqi;GAO Chongkai;YI Jun;LI Xiaofang;WU Fang;GUO Bohoiig(School of Pliannaiy,Guangdong Pharmaceutical University,Guangzhou 510006,China;Guangdong Runhua Phamiacriitical Co.Ltd.,Jieyang 515500,China)

机构地区：[1]广东药科大学药学院,广州510006 [2]广东润华药业有限公司,广东揭阳515500

出　　处：《黑龙江畜牧兽医》2022年第5期109-114,共6页Heilongjiang Animal Science And veterinary Medicine

基　　金：广东省“扬帆计划”引进创新创业团队项目(2017YT05S137)。

摘　　要：为了制备具有亲水段聚乙二醇(PEG)修饰的氟苯尼考聚乳酸-羟基乙酸共聚物(PLGA)纳米粒,筛选出其最优处方并对其进行评价,试验采用乳化-溶剂挥发法,以PEG_(4000)-PLGA作为载体材料制备PEG修饰的氟苯尼考PLGA纳米粒(FF-PEG_(4000)-PLGA NPs),通过单因素考察,以乳化剂聚乙烯醇(PVA)浓度、药脂比、油/水相体积比和氟苯尼考浓度为考察因素,包封率为考察指标,采用L_(9)(3^(4))正交试验设计选出最优处方,以葡聚糖凝胶法测定包封率,并进行体外释放试验。结果表明:制备FF-PEG_(4000)-PLGA NPs的最佳工艺为PVA浓度1.5%,氟苯尼考浓度0.8 mg/mL,药脂比(氟苯尼考∶PEG_(4000)-PLGA)1∶5,油水相体积比1∶8,此时包封率为(81.04±1.04)%,处方的重现性较好且工艺稳定可行。在体外药物释放试验中,FF-PEG_(4000)-PLGA NPs释放速率明显较氟苯尼考慢且平稳,后期可持续平稳释放至96小时,累计释放率约94%。说明制备的FF-PEG_(4000)-PLGA NPs具有较高的包封率和良好的缓释作用,重现性好。In order to prepare florfenicol poly lactic acid glycolic acid(PLGA)nanoparticles with hydrophilic polyethylene glycol(PEG)modification,the optimal prescription was screened and evaluated.In the experiment,the emulsification-solvent evaporation method was used to prepare PEG-modified florfenicol PLGA nanoparticles(FF-PEG_(4000)-PLGA NPs)with PEG_(4000)-PLGA as the carrier material.Through single-factor investigation,taking emulsifier concentration,drug-lipid ratio,oil/water phase volume ratio and drug concentration as the investigating factors,the encapsulation rate was the investigating index,and the optimal prescription was selected by the L_(9)(3^(4))orthogonal test design;the encapsulation efficiency was determined by the sephadex gel method,and the in vitro release test was carried out.The results showed that the best process for preparing FF-PEG_(4000)-PLGA NPs was that the concentration of polyvinyl alcohol(PVA)was 1.5%;the concentration of florfenicol was 0.8 mg/mL,and the drug-to-lipid ratio(florfenicol∶PEG_(4000)-PLGA)was 1∶5,the volume ratio of oil-water phase was 1∶8,and the encapsulation rate was(81.04±1.04)%.The reproducibility of the prescription was good and the process was stable and feasible.In the in vitro drug release test,the release rate of FF-PEG_(4000)-PLGA NPs was significantly slower and more stable than that of florfenicol.In the later stage,it could continue to be released steadily for 96 hours,and the cumulative release amount was about 94%.The results suggested that FF-PEG_(4000)-PLGA NPs had high encapsulation rate,good sustained release and good reproducibility.

关 键 词：氟苯尼考 正交试验 体外释放 聚乙二醇(PEG)修饰 纳米粒 

分 类 号：S859.53[农业科学—临床兽医学] S859.796[农业科学—兽医学]