盐酸多柔比星脂质体的制备及体外释放研究  

Preparation and in vitro Release of Doxorubicin Hydro chloride Liposome

作　　者：王秋云 岳占国 潘颖彬 WANG Qiu-yun;YUE Zhan-guo;PAN Ying-bin(Bostal Drug Delivery Co.,Ltd.,Guangzhou 510530,China)

机构地区：[1]广州玻思韬控释药业有限公司,广东广州510530

出　　处：《海峡药学》2024年第2期9-13,共5页Strait Pharmaceutical Journal

摘　　要：目的制备盐酸多柔比星脂质体(DOX-Lip),并研究其体外释放行为。方法采用硫酸铵梯度法制备DOX-Lip,通过单因素考察硫酸铵溶液pH、油水比、挤出次数、超滤次数、孵育温度和时间对DOX-Lip包封率的影响。再以包封率为评价指标,采用正交试验进行处方工艺优化,并评价其体外释放行为。结果经最优处方工艺制备的DOX-Lip为类圆球形,分布均匀。平均粒径为85 nm~87 nm(PDI=0.052~0.078),Zeta电位为-15 mV~-16 mV,包封率为96%~97%。体外释放与市售参比制剂相似,具有明显的缓释性。结论采用最优处方工艺制备DOX-Lip稳定可行,具有明显的缓释特征,体外释放与参比制剂相似,为该产品的生物等效性评价提供研究基础。OBJECTIVE To prepare doxorubicin hydrochloride liposome(DOX-Lip)and investigate its in vitro release behavior.METHODS DOX-Lip was prepared by ammonium sulfate gradient methods.The encapsulation efficiency of doxorubicin were investigated by a single factor of ammonium sulfate pH,oil to water ratio,extrusion passes,diafiltration passes,incubation temperature and duration.Taking encapsulation efficiency as evaluation indicators,the orthogonal test was used to optimize the formulation process of DOX-Lip and investigate in vitro release behavior.RESULTS DOX-Lip which prepared by optimal formulation process was spherical with a uniform size distribution.The particle size was 85 nm-87 nm(PDI=0.052-0.078),the Zeta potential was-15 mV--16 mV and the encapsulation efficiency was 96%-97%.DOX-Lip released slowly in vitro and was similar to that of the reference listed drug(RLD).CONCLUSION DOX-Lip prepared by the optimal formulation process is stable and feasible,has obvious sustained-release characteristics and is similar to that of RLD,and provides a research basis for the bioequivalence evaluation of doxorubicin hydrochloride liposome injection.

关 键 词：盐酸多柔比星 脂质体 正交试验 体外释放 

分 类 号：R94[医药卫生—药剂学]