尼古丁乙醇脂质体的制备与体外透皮特性研究  

Study on the Preparation of Nicotine Ethosome and Its Transdermal Permeability in vitro

作　　者：王慧[1] 张晓红[1] 张燕[1] 杨苗苗[1] 权伟[1] 戴尊孝[1] 

机构地区：[1]西安市精神卫生中心,西安710061

出　　处：《中国药房》2015年第19期2717-2720,共4页China Pharmacy

摘　　要：目的:制备尼古丁乙醇脂质体,并对其体外透皮特性进行研究。方法:采用注入法制备尼古丁乙醇脂质体。采用单因素法考察乙醇和磷脂用量对脂质体粒径和包封率的影响。采用Franz扩散池进行小鼠离体皮肤渗透实验以比较尼古丁乙醇脂质体、尼古丁脂质体和尼古丁乙醇溶液中尼古丁的累积渗透量。采用共聚焦激光扫描电镜,观察含有罗丹明B的尼古丁乙醇脂质体、尼古丁脂质体和尼古丁乙醇溶液在小鼠离体皮肤上的渗透深度。结果:当处方中含3%(m/V)磷脂和35%(V/V)乙醇时制得的尼古丁乙醇脂质体的粒径最小[(105±11.5)nm]、包封率最高[(89.13±6.12)%];与尼古丁脂质体及尼古丁乙醇溶液比较,尼古丁乙醇脂质体12 h时的体外累积渗透量最高,且3种制剂均在12 h时渗透达饱和,其渗透深度依次为80、156、175μm。结论:成功制得能增加尼古丁皮肤渗透性的尼古丁乙醇脂质体。OBJECTIVE：To prepare nicotine ethosome and study its transdermal permeability in vitro.METHODS：Injection method was adopted to prepare nicotine ethosome.Single-factor test was conducted to study the effects of the amounts of ethanol and phospholipid on the particle size and encapsulation efficiency of the ethosome.Franz diffusion cell was employed to conduct permeability test on excised rat skin to compare cumulative permeating quantities of the nicotine in nicotine ethosome,nicotine liposome and nicotine ethanol solution.Confocal laser scanning electron microscope was applied to observe the penetration depths of rhodamine B-containing nicotine ethosome,nicotine liposome and the solution of nicotine ethanol solution in the in vitro rat skin.RESULTS：When the formulation contained 3%（m/V）phospholipid and 35%（V/V）ethanol,the obtained nicotine ethosome had the smallest particle size [（105 ± 11.5） nm] and the highest encapsulation efficiency [（89.13 ± 6.12）% ].Compared with nicotine ethosome and the nicotine ethanol solution,nicotine ethosome had the largest cumulative permeating quantity in vitro at 12 h.Furthermore,the above-mentioned 3 preparations all became saturated in permeability at 12 h with the penetration depths of 80 μm,156 μm and 175 μm,respectively.CONCLUSIONS：The nicotine ethosome that can increase the transdermal permeability of nicotine has been prepared successfully.

关 键 词：尼古丁 乙醇脂质体 包封率 渗透性 

分 类 号：R943[医药卫生—药剂学]