盐酸丁卡因脂质体凝胶剂的经皮渗透性

Transcutaneous permeation of hydrochloride tetracaine formulated in liposome gel

目的 :比较盐酸丁卡因脂质体凝胶与盐酸丁卡因游离药物凝胶的离体皮肤渗透性 ,探讨脂质体作为盐酸丁卡因的载体对皮肤渗透的影响。方法 :采用体外双室渗透池作为离体皮肤的渗透试验装置 ,测定盐酸丁卡因在接受液内的累计透过百分率和在皮肤内的滞留百分率。结果 :盐酸丁卡因脂质体凝胶和游离药物凝胶相比 ,药物透过皮肤的速度明显减慢 ,累计透过百分率与时间之间均符合Hihuchi方程 ;以卡波普为基质的盐酸丁卡因脂质体凝胶涂于皮肤 2 4h后 ,在皮肤内滞留量为 36 .7% ,而游离药物凝胶皮肤内滞留量为 9.7%。结论 :脂质体有促进药物进入皮肤的能力 。

Objective:To compare the transcutaneous permeation of hydrochloride tetracaine formulated in liposome gel with the free drug in gel.And discuss the permeation mechanism of liposome as the carrier of hydrochloride tetracaine. Methods: The drug accumulated permeation percentage through the skin into the receptor cells and the drug resident percentage in the skin were determined, using the double permeation cells in vitro. Results: The drug accumulated permeation percentage into the receptor cells of hydrochloride tetracaine formulated in liposome gel was smaller than that of the free drug in gel. The drug resident percentage in the skin formulated in liposome gel was larger than that of the free drug in gel. The transcutaneous permeation of the drug in both formulations fitted in with Higuchi equation. Conclusion: The hydrochloride tetracaine liposome gel has the ability to enhance the transcutaneous permeation of the drug, and the drug in receptor cells does not increase.