天津医药

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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*

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   

  1. 1. 天津医科大学口腔医院
    2. 天津大学材料科学与工程学院纳米生物技术研究所
    3. 天津医科大学药理教研室
  • 收稿日期:2012-07-13 修回日期:2012-10-28 出版日期:2013-03-15 发布日期:2013-03-15
  • 通讯作者: 李长义

Preparation of lidocaine hydrochloride-loaded transactivation transcriptional activator conjugated polymetric liposomes and permeation through mouse skin in vitro

  • Received:2012-07-13 Revised:2012-10-28 Published:2013-03-15 Online:2013-03-15

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摘要：

【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24 h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。

关键词: 盐酸利多卡因, 赖氨酸壳聚糖十八烷基季铵盐, 跨膜肽, 纳米高分子脂质体, 透皮实验

Abstract:

[Abstract] 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 hydrochloride 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.

Key words: lidocaine hydrochloride, octadecyl quaternized lysine modi?ed chitosan, transactivation, polymetric liposomes, permeation through skin