环糊精修饰的氟苯尼考PLGA纳米粒的制备及其体外释放评价

Preparation of Cyclodextrin-modified Florfenicol PLGA Nanoparticles and Its Release Evaluation in vitro

制备了环糊精修饰的氟苯尼考PLGA纳米粒(FF-2-HP-β-CD-PLGA NPs),筛选出其最优处方并进行评价。采用乳化溶剂挥发法制备FF-2-HP-β-CD-PLGA NPs,通过单因素考察,以乳化剂浓度、药脂比、药物浓度和2-HP-β-CD浓度为考察因素,包封率为考察指标,正交试验筛选最优处方,并对其进行体外释放试验。结果表明,制备FF-2-HP-β-CD-PLGA NPs的最佳工艺为PVA浓度2%,药物与PLGA用量比1∶15,药物浓度2.0 mg·mL-1,2-HP-β-CD浓度为1.5%。测得平均包封率为(82.02±0.82)%,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-2-HP-β-CD-PLGA NPs释放速率明显较FF慢且平稳(P<0.05),后期可持续平稳释放至72 h,累积释放率为(82.08±1.71)%。结论表明,制备的FF-2-HP-β-CD-PLGA NPs具有较高的包封率,体外释药具有缓释行为。

The cyclodextrin-modified florfenicol PLGA nanoparticles(FF-2-HP-β-CD-PLGANPs)were prepared,and their optimal formulations were selected and evaluated.FF-2-HP-β-CD-PLGANPs were prepared by emulsifying solvent evaporation.The optimal formulation was screened by orthogonal test with emulsifier concentration,drug-to-lipid ratio,drug concentration and 2-HP-β-CD concentration as factors,and the encapsulation index was investigated.The optimal formulation was selected by orthogonal test,and its in vitro release test was performed.In results,the optimum preparation process of FF-2-HP-β-CD-PLGA NPs were as follows:PVA concentration 2%,drug to PLGA dosage ratio 1∶15,drug concentration 2.0 mg·mL-1,2-HP-β-CD concentration 1.5%.The average encapsulation was(82.02±0.82)%,and the reproducibility of the formulation was good and the process was stable and feasible.In the in vitro drug release assay,the release rate of FF-2-HP-β-CD-PLGA NPs was significantly slower and more stable than that of FF(P<0.05),and the release could continue and be stable until 72 hours at a later stage,with a cumulative release of(82.08±1.71)%.The results show that the prepared FF-2-HP-β-CD-PLGA NPs have high entrapment efficiency and sustained release behavior in vitro.