5-氟尿嘧啶乙醇脂质体的改性及其透皮吸收研究

Modification and Transdermal Absorption of 5-Fluorouracil Ethosomes

目的:研究胆固醇对5-氟尿嘧啶(5-FU)乙醇脂质体的改性及其体外透皮扩散的影响。方法:制备不同胆固醇含量的5-FU乙醇脂质体,并考察胆固醇含量对脂质体粒径、Zeta电位、分散指数、包封率、皮内药物滞留量等指标的影响。结果:加入胆固醇后粒径和Zeta电位变化不大,分散指数从0.584降至0.143,5-FU包封率从28.6%增至48.8%,皮内残留5-FU量从40%增至80%以上。结论:胆固醇不会改变乙醇脂质体的粒径大小及Zeta电位,但可提高其分散性和稳定性;加入适量的胆固醇可提高乙醇脂质体中5-FU的包封率及皮内药物滞留量。

OBJECTIVE： To study the effects of cholesterol on the modification the transdermal permeation in vitro of 5- fluorouracil （5-FU） ethosomes. METHODS： 5-FU ethosomes containing different cholesterol amounts were prepared, and the effect of the content of cholesterol on the mean particle size of liposome, Zeta potentials, polydispersity index, entrapment efficiency, and residual amount of drug in local skin were measured. RESULTS： The mean diameters of the 5- FU ethosomes and the Zeta potentials experienced no significant change, but the polydispersity index of the 5-FU ethosomes decreased from 0. 584 to 0.143, the entrapment efficiency of 5-FU increased from 28.6% to 48.8%, and the residual amount of 5-FU were dramatically increased from 40% to 80% after modified with cholesterol. CONCLUSIONS： Cholesterol does no effect on mean diameters and the Zeta potentials of the 5- FU ethosomes, but it can change their polydispersity and stability. The entrapment efficiency and the residual amount of 5- FU can be enhanced after being modified with vis quantum cholesterol.