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目的:以两亲性β-环糊精衍生物(β-CD-[P(AA-co-MMA)-b-PNVP]4,β-CD-PPP)为药物载体制备长春西汀嵌段共聚物胶束,探究其作为药物载体的可行性和稳定性。方法:采用溶剂挥发法制备长春西汀胶束,考察处方因素及工艺条件对载药量和包封率的影响后,以正交设计试验优化制备工艺条件;并对制得胶束的包封率、载药量、粒径、红外图谱、体外释放度以及胶束材料的临界胶束浓度(CMC)进行了研究。结果:以最优处方所制备的长春西汀胶束包封率为(56.42±0.28)%,载药量为(12.36±0.05)%,平均粒径为48.1 nm;红外光谱图表明β-环糊精衍生物载药胶束将药物包裹在胶束里面;体外释放度测定结果显示长春西汀胶束具有pH敏感性和缓释能力;胶束材料β-CD-PPP的CMC为0.554 6×10-4 mg·ml-1。结论:两亲性β-环糊精聚合物β-CD-PPP可用作疏水性药物的缓释给药载体。
OBJECTIVE: To prepare vinpocetine block copolymer with amphipathic β-cyclodextrin derivative (β-CD- [P (AA-co-MMA) -b-PNVP] 4 and β-CD-PPP as drug carrier Micelles to explore its feasibility and stability as a drug carrier. Methods: The vinpocetine micelles were prepared by solvent evaporation method. The effects of prescription factors and process conditions on drug loading and entrapment efficiency were investigated. The orthogonal design test was used to optimize the preparation conditions. The encapsulation of micelles Rate, drug loading, particle size, infrared spectrum, in vitro release and the critical micelle concentration (CMC) of micelles were studied. RESULTS: The encapsulation efficiency of vinpocetine micelles was (56.42 ± 0.28)%, the drug loading was (12.36 ± 0.05)% and the average particle diameter was 48.1 nm. The IR spectra showed that the β- The drug-loaded micelles of dextrin derivatives encapsulated the drug in micelles. The in vitro release assay showed that vinpocetine micelles had pH-sensitive and sustained-release ability. The CMC of micellar β-CD-PPP was 0.554 6 × 10-4 mg · ml-1. Conclusion: β-CD-PPP amphiphilic β-cyclodextrin polymer can be used as a sustained-release drug delivery carrier for hydrophobic drugs.