尼古丁二元醇脂质体温敏凝胶的制备及体外评价  

Preparation and in vitro evaluation of nicotine diol liposome thermo sensitive gels

作　　者：王慧[1] 邵青 张燕[1] 杨苗苗[1] 胡婕雯 龚阳泽 WANG Hui;SHAO Qing;ZHANG Yan;YANG Miaomiao;HU Jiewen;GONG Yangze(Mental Health Center,Xi an 710061,China)

机构地区：[1]西安市精神卫生中心,西安710061

出　　处：《西北药学杂志》2022年第6期100-104,共5页Northwest Pharmaceutical Journal

基　　金：国家自然科学基金项目(编号:81202938);西安市科学技术局项目(编号:201805051ZD2CG35)。

摘　　要：目的 制备尼古丁二元醇脂质体温敏凝胶,并对其进行处方筛选,优化药物的经皮转运。方法 选用温敏材料泊洛沙姆407(P407)及泊洛沙姆188(P188)为基质,尼古丁二元醇脂质体温敏凝胶用冷溶法制备,以胶凝温度为考察指标,采用单因素实验对尼古丁二元醇脂质体温敏凝胶进行处方优化;考察尼古丁乙醇溶液、二元醇脂质体及含P407/P188二元醇脂质体温敏凝胶的体外释放性质;Franz扩散池对比尼古丁二元醇脂质体和二元醇脂质体凝胶透皮量及皮内滞留量。结果 制备的温敏凝胶在室温以液体状态存在,在32℃形成凝胶。体外释放实验显示,24 h二元醇脂质体和二元醇脂质体凝胶的释放率分别是(78.60%±0.43%)、(56.36%±0.26%)。与二元醇脂质体相比,二元醇脂质体凝胶有明显的缓释作用。12 h透皮实验表明,二元醇脂质体凝胶可以增大皮内滞留量,而二元醇脂质体可以增加透皮深度。结论 与二元醇脂质体相比,二元醇脂质体温敏凝胶有明显的缓释作用,且显著增加药物的皮内滞留量。Objective Nicotine diol liposome thermosensitive gels were prepared and the prescription was screened to optimize the drug transdermal transportation.Methods Poloxam 407(P407) and Poloxam 188(P188) were selected as the thermo sensitive materials, and nicotine-diol liposome thermo sensitive gels were prepared by cold solution method. The gelation temperature was used as the index. The formulation of nicotine diol liposome thermo sensitive gels were optimized by single factor experiment. The release properties of nicotine ethanol solution, diol liposome and thermosensitive gels containing P407/P188 diol liposome in vitro were investigated. Franz diffusion cell was used to compare the transdermal volume and intradermal retention of nicotine diol liposomes and diol liposomes gels.Results The thermosensitive gels were prepared in liquid state at room temperature and formed at 32 ℃. The release rate of diol liposome and diol liposome gels at 24 hours was(78.60%±0.43%) and(56.36%±0.26%), respectively. Compared with diol liposome, diol liposome gels had obvious slow-release effect. 12 hours transdermal experiment showed that the diol liposome gel could increase the retention amount in skin, and the diol liposome could increase the transdermal depth.Conclusion Compared with diol liposomes, the thermosensitive gels of diol liposomes had a significant slow-release effect and significantly increased the intradermal retention of drugs.

关 键 词：尼古丁 二元醇脂质体 泊洛沙姆407 泊洛沙姆188 经皮转运 温敏凝胶 

分 类 号：R94[医药卫生—药剂学]