El Maghraby G M, Williams A C, Barry B W
School of Pharmacy, University of Bradford, West Yorkshire, UK.
J Pharm Pharmacol. 2001 Aug;53(8):1069-77. doi: 10.1211/0022357011776450.
The potential use of ultradeformable and standard liposomes as skin drug delivery systems was investigated in-vitro. An improved experimental design gave a good measure for skin deposition of drug. This avoided the contamination that can occur due to incomplete washing of the donor before direct determination of the amount of drug in the skin. The design used aqueous ethanolic receptor which is believed to diffuse into skin, disrupting deposited liposomes (if any) and thus releasing both bound and free drug. The receptor fluid was refined by testing different concentrations of ethanol. The applied dose was also optimized. Using the improved design and the optimum dose, an ultradeformable formulation was compared with four traditional liposomes for skin delivery of 5-fluorouracil (5-FU). The best receptor was 50% aqueous ethanol and the optimum dose was 20 microL. The ultradeformable formulation was superior to standard liposomes in the skin delivery of 5-FU. Of the traditional liposomes, the non-rigid preparation was the best. However, stabilization of the liposome membrane with cholesterol abolished the benefit of this non-rigid preparation. It was concluded that ultradeformable vesicles are promising agents for skin delivery of drugs.
在体外研究了超可变形脂质体和标准脂质体作为皮肤给药系统的潜在用途。一种改进的实验设计为药物在皮肤中的沉积提供了很好的测量方法。这避免了在直接测定皮肤中药物量之前由于供体洗涤不完全而可能发生的污染。该设计使用乙醇水溶液受体，据信其可扩散到皮肤中，破坏沉积的脂质体（如果有的话），从而释放结合的和游离的药物。通过测试不同浓度的乙醇对受体液进行了优化。给药剂量也进行了优化。使用改进的设计和最佳剂量，将一种超可变形制剂与四种传统脂质体用于5-氟尿嘧啶（5-FU）的皮肤给药进行了比较。最佳受体是50%乙醇水溶液，最佳剂量是20微升。在5-FU的皮肤给药方面，超可变形制剂优于标准脂质体。在传统脂质体中，非刚性制剂是最好的。然而，用胆固醇稳定脂质体膜消除了这种非刚性制剂的优势。得出的结论是，超可变形囊泡是有前途的皮肤给药药物载体。
