脒修饰的包载荧光探针香豆素-6脂质体的制备  

Preparation of amidine modified fluorescent probe coumarin-6-loaded liposome

作　　者：樊梅[1,2] 袁志翔[2] 宋联强 高媛[1,2] 徐超群[2] 

机构地区：[1]成都中医药大学药学院,四川成都610075 [2]四川省中医药科学院,四川成都610041

出　　处：《华西药学杂志》2015年第2期146-148,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的研究3,5-二-十五烷氧基苯甲脒(DBH)修饰的香豆素-6脂质体的制备工艺,并初步考察该脂质体的体外释放性能和肾小球靶向性。方法首先合成DBH。再以其为配基,胆固醇、大豆磷脂为载体材料,采用薄膜分散-超声法制备脒修饰的载香豆素-6荧光探针脂质体,考察其粒径分布、Zeta电位、包封率及体外累积释药率。结果脒基修饰的香豆素-6脂质体形态圆整,粒径分布为120.7±2.4 nm,Zeta电位为12.6±1.6 m V,包封率为99.7%±1.8%,体外的48 h累积释药量小于2%。结论脒基修饰的香豆素-6脂质体的制备工艺简便易操作,包封率高,性质稳定。OBJECTIVE To prepare the 3,5 - dipentadecyloxybenzamidine hydrochloride （DBH） modified coumarin - 6 liposome, and evaluate its release preliminarily in vitro, leading to further study the DBH modified liposome potential targeting of Glomerular Mesangial cells. METHODS DBH was synthesized, and eoumarin -6 liposome modified with DBH as ligand was prepared by cholesterol and soybean lecithin. Coumarin - 6 - loaded amidine modified liposome was prepared by film - ultrasonic and then particle size distribution, Zeta potential , encapsulation efficiency and the cumulative release rate were measured. RESULTS The structure of amidine was confirmed by nuclear magnetic resonance. The modified liposome was spherical with a mean diameter of 120.7 ± 2.4 nm and a potential of 12.6±1.6 mV, and the encapsulation efficiency was 99.7%±1.8%. Cumulative release percentage was less than 2% within 48 hours. CONCLUSION The preparation process of modified coumarin - 6 liposome is reliable and simple, and the liposome has a high encapsulation efficiency and perfect stability.

关 键 词：3 5-二-十五烷氧基苯甲脒 香豆素-6 脂质体 包封率 释放率 薄膜分散-超声法 荧光探针 

分 类 号：R94[医药卫生—药剂学]