长春西汀β-环糊精衍生物胶束的制备及表征

Preparation and characterization of vinpocetine in-loadedβ-CD derivatives micelles

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 （VP） micelles by using an amphiphilic β-CD derivative, β-CD-[P（AA-co- MMA） -b PNVP]4 （β-CD-PPP） ; and to explore its potential application in drug delivery system. METHODS VP micelles were prepared by solvent evaporation methods and the preparation process of VP micelles was optimized by single factor analy- sis and orthogonal test. The drug loading capacity, entrapment efficiency, particle size, the in vitro release of VP micelles, and the critical micelle concentration （CMC） of β-CD-PPP were determined. RESULTS The encapsulation efficiency and drug loading of micelles were （30. 21 ± 0. 51 ）% and （12.36± 0. 20）%, the mean size of VP-loaded mieelles was 48. 1 nm, infrared spectrogram indicated VP was packaged in micelles. VP micelles showed pH sensibility and sustained release in vitro release. The CMC of β-CDPPP was 0. 5546 × 10^-4 mg·ml^-1. CONCLUSION β-CD-PPP could be considered as a novel polymer carrier in drug delivery system for hydrophobic drugs.