脂质体及脂质体凝胶对尼美舒利透皮吸收的比较研究

Comparative Study of Liposomes and Liposomes-in-hydrogel for Transdermal Absorption of Nimesulide

目的:比较脂质体及脂质体凝胶作为载体对尼美舒利(NIM)透皮吸收的影响。方法:采用薄膜-超声分散法制备NIM脂质体,并以泊洛沙姆-407为亲水性凝胶基质,制备NIM脂质体凝胶。对其形态、粒径、Zeta电位、包封率、体外释药等体外主要性质进行考察,并探究NIM脂质体凝胶的粘附性;以大鼠腹部皮肤为屏障,对其体外透皮吸收特性及其机制进行了研究。结果:与NIM脂质体相比,凝胶基质中NIM脂质体的形态、粒径及Zeta电位、包封率差异无统计学意义(P>0.05),却呈现优良的粘附特性及更显著的缓释性;NIM脂质体、NIM脂质体凝胶体外透皮特性符合Higuchi函数方程;两者均可使皮肤的相变温度下降,且以NIM脂质体凝胶作用下降更为明显(P<0.05)。结论:与脂质体相比,脂质体凝胶作为载体可增加NIM的皮肤粘附性、缓释性,并使NIM更易透皮吸收。

Objective:To compare the effects of liposomes and liposomes-in-hydrogel as carriers on transdermal absorption of nimesulide(NIM).Methods:NIM-loaded liposomes were prepared with a film-ultrasonic dispersion method,and dispersed into hydrogel with Poloxmar-407 as the matrix to obtain NIM-loaded liposomes-in-hydrogel.The morphology,size and size distribution,zeta potential,encapsulation efficiency and drug release in vitro were studied for the two preparations,and the adhesion properties of NIM-loaded liposomes-in-hydrogel were also investigated.Rat’s abdominal skin as the barrier,the in vitro percutaneous permeability and underlying mechanism were explored.Results:Compared to those of NIM-loaded liposomes,the morphology,size and size distribution,zeta potential and encapsulation efficiency of NIM-loaded liposomes-in-hydrogel showed no significant changes(P>0.05),while the adhesion properties and sustained release were both more notable.The in vitro percutaneous permeability of NIM-loaded liposomes and NIM-loaded liposomes-in-hydrogel both conformed to the characteristics of Higuchi release equation model.After the treatment with the two preparations,the phase transition temperature of skin was lowered,and the effect of NIM-loaded liposomes-in-hydrogel was more significant(P<0.05).Conclusion:Compared to liposomes,liposomes-in-hydrogel can enhance the adhesion and sustained release of NIM,and make NIM penerate through skin easier.