title: Itraconazole-hydroxypropyl-β-cyclodextrin loaded deformable liposomes: in vitro skin penetration studies and antifungal efficacy using Candida albicans as model.
abstract: 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.
authors.affiliation: 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.
authors.forename: Abdullah H
authors.initials: AH
authors.lastname: Alomrani
authors.affiliation: 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.
authors.forename: Gamal A
authors.initials: GA
authors.lastname: Shazly
authors.affiliation: Department of Protein Research, Genetic Engineering and Biotechnology Research Institute, Mubarak City for Scientific Research and Technology Applications, Alexandria, Egypt.
authors.forename: Amro A
authors.initials: AA
authors.lastname: Amara
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; Department of Pharmaceutics, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt. Electronic address: mbadran75@gmail.com.
authors.forename: Mohamed M
authors.initials: MM
authors.lastname: Badran
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000818:Animals; D000935:Antifungal Agents / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects*; D004355:Drug Stability; D066298:In Vitro Techniques; D017964:Itraconazole / Q000494:pharmacology*; D008081:Liposomes / Q000737:chemistry* / Q000648:ultrastructure; D008826:Microbial Sensitivity Tests; D008954:Models, Biological; D010316:Particle Size; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects*; D055672:Static Electricity; D053835:Unilamellar Liposomes / Q000737:chemistry; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000935:Antifungal Agents; D008081:Liposomes; D053835:Unilamellar Liposomes; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D017964:Itraconazole
keywords: Antifungal activity; Deformable liposomes; Ex vivo penetration; HPβCD; Itraconazole (ITZ)