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

关键词:  氟苯尼考  正交试验  纳米粒  体外释放

Key words:  florfenicol  orthogonal test  nanoparticles  in vitro release

摘要:

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。在体外药物释放实验中，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小时，累积释放率为(82 ± 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。

Abstract:

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 ± 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.