郭健新, 平其能, 吴涛. 环孢素脂质微粒经小鼠皮肤给药的渗透机理研究J. 药学学报, 2000, 35(10): 782-785.
引用本文: 郭健新, 平其能, 吴涛. 环孢素脂质微粒经小鼠皮肤给药的渗透机理研究J. 药学学报, 2000, 35(10): 782-785.
GUO Jian-xin PING Qi-neng WU Tao, . TRANSDERMAL DELIVERY MECHANISMS OF LECITHIN NANOPARTICLES WITH CYCLOSPORIN A THROUGH MICE SKINJ. Acta Pharmaceutica Sinica, 2000, 35(10): 782-785.
Citation: GUO Jian-xin PING Qi-neng WU Tao, . TRANSDERMAL DELIVERY MECHANISMS OF LECITHIN NANOPARTICLES WITH CYCLOSPORIN A THROUGH MICE SKINJ. Acta Pharmaceutica Sinica, 2000, 35(10): 782-785.

环孢素脂质微粒经小鼠皮肤给药的渗透机理研究

TRANSDERMAL DELIVERY MECHANISMS OF LECITHIN NANOPARTICLES WITH CYCLOSPORIN A THROUGH MICE SKIN

  • 摘要: 目的 研究普通纳米脂质体、柔性纳米脂质体及胆酸钠-磷脂混合胶团对环孢素经小鼠皮肤给药的渗透机理。方法 将含药载体非封闭性应用于离体或在体小鼠皮肤,测定了皮肤、接收介质和血液中环孢素含量。结果 离体条件下,应用柔性纳米脂质体和混和胶团后均能在接收液中检测到药物,但普通脂质体却不能。在体条件下,应用柔性纳米脂质体后8 h血药浓度到达峰值,而应用普通脂质体和混合胶团后在血中几乎未检测到药物。结论 柔性纳米脂质体在皮肤水合压力下发生变形,携药透过皮肤;普通脂质体主要与皮肤发生融合产生蓄积作用;混合胶团在水溶液状态下发挥其渗透促进作用。

     

    Abstract: AIM To investigate the transdermal delivery mechanisms of the flexible nano-liposomes, conventional nano-liposomes and lecithin-cholate mixed micelles through mouse skin. METHODS Liposomes and micelles were applied onto the mouse skin non-occlusively in vitro and in vivo, then the drug concentrations in the skin, receiver and blood were determined. RESULTS In vitro permeation studies showed that flexible nano-liposomes and mixed micelles transported measurable amount of cyclosporin A through the skin. Conventional liposomes precluded drugs permeate through the skin while deposited it in the skin. In vivo studies indicated that blood concentration reached peak value at 8 h after the application of flexible nano-liposomes. Both conventional nano-liposomes and mixed micelles failed to deliver measurable amount of drug into the blood. CONCLUSION Liposomes fuse with the skin. Flexible nano-liposomes penetrate through the skin under the pressure of hydration force. Mixed micelles promote transfer in state of solution.

     

/

返回文章
返回