Alomrani Abdullah H, Shazly Gamal A, Amara Amro A, Badran Mohamed M
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; Nanomedicine Unit (NMU-KSU), College of Pharmacy, King Saud University, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Colloids Surf B Biointerfaces. 2014 Sep 1;121:74-81. doi: 10.1016/j.colsurfb.2014.05.030. Epub 2014 Jun 2.
The study aimed to develop novel ITZ-loaded deformable liposomes (DL) in presence of hydroxypropyl-β-cyclodextrin (HPβCD) (DL-CD) to enhance antifungal activity. These formulations have been reported as conceivable vesicles to deliver drug molecules to the skin layers. The efficiency of the prepared systems was compared with conventional liposomes (CL) and ITZ solution. The developed liposomes were characterized for particle size, entrapment efficiency (EE %), deformability, stability, and morphology of the vesicles. In addition, ex vivo penetration and antifungal activity were evaluated. It was found that the presence of HPβCD played a significant role in reducing the vesicle size to nano range. The deformability study and TEM images revealed that membrane deformability of DL and DL-CD was much higher than that of CL. Moreover, DL-CD enhanced the amount of ITZ in SC and deeper skin layers compared to DL and CL. The antifungal activity of ITZ-loaded deformable liposomes remained intact compared to ITZ solution. It can be concluded that deformable liposomes in the presence of HPβCD may be a promising carrier for effective cutaneous delivery of ITZ.
该研究旨在开发在羟丙基-β-环糊精（HPβCD）存在下的新型载伊曲康唑（ITZ）可变形脂质体（DL）（DL-CD），以增强抗真菌活性。这些制剂已被报道为可将药物分子递送至皮肤层的理想囊泡。将所制备体系的效率与常规脂质体（CL）和ITZ溶液进行比较。对所开发的脂质体进行粒径、包封率（EE%）、可变形性、稳定性和囊泡形态表征。此外，还评估了体外渗透和抗真菌活性。发现HPβCD的存在在将囊泡尺寸减小至纳米范围方面发挥了重要作用。可变形性研究和透射电镜图像显示，DL和DL-CD的膜可变形性远高于CL。此外，与DL和CL相比，DL-CD增加了伊曲康唑在角质层（SC）和更深皮肤层中的含量。与ITZ溶液相比，载ITZ可变形脂质体的抗真菌活性保持不变。可以得出结论，在HPβCD存在下的可变形脂质体可能是伊曲康唑有效经皮递送的有前景的载体。
