天津医药 ›› 2015, Vol. 43 ›› Issue (4): 353-355.doi: 10.11958/j.issn.0253-9896.2015.04.005

• 实验研究 • 上一篇    下一篇

盐酸利多卡因葡聚糖基纳米类脂质体的透皮研究

牛娇1,曾东1,李芹2,王生3,常津3,王悦1,张连云1△   

  1. 1天津医科大学口腔医院(邮编300070);2天津医科大学基础学院药理学教研室;3天津大学材料科学与工程学院纳米生物技术研究所
  • 收稿日期:2014-10-23 修回日期:2015-01-09 出版日期:2015-04-15 发布日期:2015-04-13
  • 通讯作者: 张连云 E-mail:qianniuhuahua321@163.com
  • 作者简介:牛娇(1988),女,硕士在读,主要从事表面麻醉剂研究
  • 基金资助:
    国家自然科学基金资助项目(81070871);天津市自然科学基金重点项目(11JCZDJC20400)

Percutaneous permeability of lidocaine hydrochloride loaded destran-based niosomes

NIU Jiao1, ZENG Dong1, LI Qin2, WANG Sheng3, CHANG Jin3,WANG Yue1, ZHANG Lianyun1△   

  1. The Stomatological Hospital of Tianjin Medical University, Tianjin 300070,China
  • Received:2014-10-23 Revised:2015-01-09 Published:2015-04-15 Online:2015-04-13
  • Contact: ZHANG Lianyun E-mail:qianniuhuahua321@163.com

摘要: 摘要:目的探讨采用葡聚糖基纳米类脂质体为载体包载利多卡因(LID-HLD-BNs)的表面麻醉剂的体外透皮性能及在体透皮特征。方法以包载利多卡因的传统脂质体(LID-CLs)和盐酸利多卡因注射液(LID-IJ)为对照,使用离体小鼠腹部皮肤,采用Franz 扩散池,高效液相色谱法进行体外透皮实验,观察LID-HLD-BNs 的透皮性能。以钙黄绿素为探针,运用激光共聚焦显微镜(CLSM),以载钙黄绿素的传统脂质体(钙黄绿素-CLs)和游离钙黄绿素为对照,观察该类脂质体制剂(钙黄绿素-HLD-BNs)在活体小鼠腹部的荧光透皮情况。结果LID-HLD-BNs 单位面积累积透皮量和透皮速率高于LID-CLs 和LID-IJ。LID-IJ、LID-CLs、LID-HLD-BNs 的透皮速率分别为39.15、 79.04 和142.86 μg/(cm2·h),差异有统计学意义(P<0.01)。在体荧光透皮实验中,钙黄绿素-HLD-BNs 组的透皮速度和透皮深度均明显大于钙黄绿素-CLs 组和游离钙黄绿素组。结论葡聚糖基纳米类脂质体具有良好的经皮渗透性能。

关键词: 投药, 皮肤, 脂质体, 利多卡因, 色谱法, 液相, 药物利用, 体外研究

Abstract: Abstract:Objective To study the percutaneous permeability through mouse skin of lidocaine hydrochloride-loaded destran-based niosomes(LID-HLD-BNs)in vitro and in vivo. Methods HPLC was employed to exam lidocaine hydrochlo⁃ ride. Lidocaine hydro-chloride-loaded conventional liposomes (LID-CLs) and lidocaine hydrochloride injection (LID-IJ) were used as control. Isolated mouse skin was added into Franz diffusion cell to evaluate the permeability of LID-HLD-BNs in vitro. Confocal Laser Scanning Microscopy(CLSM)was used to observe the permeation depth of mouse skin in vivo. Re⁃ sults The permeation rate and cumulative permeation amount were significantly higher in LID-HLD-BNs group than those of LID-CLs and LID-IJ groups (P<0.05). CLSM studies also confirmed that HLD-BNs reached deeper layers of the skin. Conclusion LID-HLD-BNs has good transdermal ability.

Key words: administration, cutaneous;liposomes;lidocaine;chromatography, liquid;drug utilization, in vitro