Fang J Y, Hong C T, Chiu W T, Wang Y Y
Graduate Institute of Pharmaceutical Sciences, Taipei Medical University, 250 Wu-Hsing Street, Taipei, Taiwan.
Int J Pharm. 2001 May 21;219(1-2):61-72. doi: 10.1016/s0378-5173(01)00627-5.
The skin permeation and partitioning of a fluorinated quinolone antibacterial agent, enoxacin, in liposomes and niosomes, after topical application, were elucidated in the present study. In vitro percutaneous absorption experiments were performed on nude mouse skin with Franz diffusion cells. The influence of vesicles on the physicochemical property and stability of the formulations were measured. The enhanced delivery across the skin of liposome and niosome encapsulated enoxacin had been observed after selecting the appropriate formulations. The optimized formulations could also reserve a large amount of enoxacin in the skin. A significant relationship between skin permeation and the cumulative amount of enoxacin in the skin was observed. Both permeation enhancer effect and direct vesicle fusion with stratum corneum may contribute to the permeation of enoxacin across skin. Formulation with niosomes demonstrated a higher stability after 48 h incubation compared to liposomes. The inclusion of cholesterol improved the stability of enoxacin liposomes according to the results from encapsulation and turbidity. However, adding negative charges reduced the stability of niosomes. The ability of liposomes and niosomes to modulate drug delivery without significant toxicity makes the two vesicles useful to formulate topical enoxacin.
本研究阐明了一种氟化喹诺酮抗菌剂依诺沙星在局部应用后在脂质体和非离子表面活性剂泡囊中的皮肤渗透和分配情况。采用Franz扩散池对裸鼠皮肤进行体外经皮吸收实验。测定了泡囊对制剂物理化学性质和稳定性的影响。在选择合适的制剂后，观察到脂质体和非离子表面活性剂泡囊包裹的依诺沙星经皮递送增强。优化后的制剂还能在皮肤中保留大量依诺沙星。观察到皮肤渗透与皮肤中依诺沙星累积量之间存在显著关系。渗透促进剂效应和泡囊与角质层的直接融合都可能有助于依诺沙星透过皮肤。与脂质体相比，非离子表面活性剂泡囊制剂在孵育48小时后表现出更高的稳定性。根据包封和浊度结果，加入胆固醇可提高依诺沙星脂质体的稳定性。然而，添加负电荷会降低非离子表面活性剂泡囊的稳定性。脂质体和非离子表面活性剂泡囊在不产生明显毒性的情况下调节药物递送的能力使得这两种泡囊可用于配制局部用依诺沙星。
