Itraconazole-hydroxypropyl-β-cyclodextrin loaded deformable liposomes: In vitro skin penetration studies and antifungal efficacy using Candida albicans as model

• Published in: Colloids and surfaces, B, Biointerfaces Vol. 121; pp. 74 - 81
• Main Authors: Alomrani, Abdullah H., Shazly, Gamal A., Amara, Amro A., Badran, Mohamed M.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.09.2014
• Subjects: 2-Hydroxypropyl-beta-cyclodextrin; Animals; Antifungal activity; Antifungal Agents - pharmacology; beta-Cyclodextrins - chemistry; Candida albicans; Candida albicans - drug effects; Computational efficiency; Computing time; Deformable liposomes; Deformation; Drug Stability; Ex vivo penetration; Formability; HPβCD; In Vitro Techniques; Itraconazole (ITZ); Itraconazole - pharmacology; Liposomes; Liposomes - chemistry; Liposomes - ultrastructure; Mathematical models; Microbial Sensitivity Tests; Models, Biological; Particle Size; Penetration; Rats; Skin Absorption - drug effects; Static Electricity; Unilamellar Liposomes - chemistry; Vesicles; Antifungal activity; Deformable liposomes; HPβCD; Itraconazole (ITZ); Ex vivo penetration
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2014.05.030

•Development of itraconazole loaded deformable liposomes in the presence of HPβCD.•High drug entrapped and reduced particle size was achieved by these liposomes.•The amount of itraconazole in SC, deeper skin layers and receptor fluid was enhanced.•The antifungal activity of itraconazole remained intact compared to drug solution. 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.