盐酸利多卡因跨膜肽纳米高分子脂质体的制备与体外透皮实验研究  

Preparation of Lidocaine Hydrochloride-Loaded Transactivation Transcriptional Activator Conjugated Polymeric Liposomes and Its in Vitro Skin Permeation in Mice

作　　者：曹岩[1] 李雨辰[1] 王悦[1] 王汉杰[2] 李芹[3] 李长义[1] 张连云[1] 

机构地区：[1]天津医科大学口腔医院,300070 [2]天津大学材料科学与工程学院纳米生物技术研究所 [3]天津医科大学基础医学院药理学教研室

出　　处：《天津医药》2013年第3期227-229,共3页Tianjin Medical Journal

基　　金：国家自然科学基金资助项目(项目编号:81070871);天津市自然科学基金重点项目(项目编号:11JCZDJC20400)

摘　　要：目的采用赖氨酸壳聚糖十八烷基季铵盐(OQLCS)组装跨膜肽(TAT)包载盐酸利多卡因制备纳米高分子脂质体,并研究其体外透皮渗透情况。方法采用反相蒸发法制备盐酸利多卡因跨膜肽纳米高分子脂质体(LID-TAT-PLs),使用离体小鼠皮和Franz扩散池进行体外透皮实验,HPLC法测定接收液中盐酸利多卡因的浓度,评价LID-TAT-PLs、未组装跨膜肽的盐酸利多卡因纳米高分子脂质体(LID-PLs)和盐酸利多卡因注射液(LID-IJ)的体外透皮渗透情况。结果 LID-TAT-PLs的体外透皮速度和累积透过量均明显高于LID-PLs和LID-IJ。LID-TAT-PLs组的24h累积透过量达(88.15±11.11)%,明显高于LID-PLs的(73.91±12.13)%和LID-IJ的(26.31±5.43)%,差异有统计学意义(P<0.05)。结论 TAT可以明显促进药物的透皮渗透,LID-TAT-PLs制备简单,具有良好的透皮释放行为。Objective To prepare the lidocaine hydrochloride-loaded transactivation （TAT） conjugated octadecyl quaternized lysine modified chitosan polymeric liposomes （LID-TAT-PLs） and to study its in vitro skin permeation characters in mice. Methods LID-TAT-PLs were prepared by reverse-phase evaporation method. The concentrations of lidocaine hy- drochloride were determined by HPLC. The isolated mouse skin and Franz diffusion cell were used to evaluate the characters of permeation of LID-TAT-PLs, LID-PLs and lidocaine hydrochloride injection （LID-IJ）. Results The permeation rate and cumulative permeation amount were significantly higher in LID-TAT-PLs group than those of LID-PLs and LID-IJ groups （P〈 0.05）. Conclusion TAT can significantly enhance the transdermal permeation of drugs in mice. The LID-TAT-PLs can be prepared via a relatively simple method.

关 键 词：利多卡因 赖氨酸壳聚糖十八烷基季铵盐 跨膜肽 纳米高分子脂质体 皮肤试验 透皮实验 

分 类 号：R[医药卫生]