title: Lipid-based microtubes for topical delivery of amphotericin B.
abstract: The self-assembly process is a valuable tool for constructing nano and microstructures. Microtubes (MTs) self-assembled from amphiphiles are novel promising nanomaterials as they have easy self-assembly in aqueous solutions, reproducibility and biocompatibility. The incorporation of amphotericin B (AmB) into lipid microtubes formed from 12-hydroxystearic acid (12HSA) when mixed with ethanolamine in aqueous media was investigated. MTs of several concentrations of lipid material and AmB were prepared. The structure was characterized by phase-contrast microscopy, TEM and SEM. The type of interaction was analyzed by FTIR and DSC. Stability studies were carried out at room temperature and at 4 °C. Loading efficiency of the system was found to be much higher than the drug solubility in water. MTs with 1% of 12HSA and 1 mg/ml of AmB showed to be the most stable formulation. In vitro skin penetration assay showed a flux of 18.20±3.35 μg/cm(2). Amb-loaded MTs in vitro antifungal activity was evaluated and formulation showed similar results to that of AmB deoxycholate showing that AmB retained its antifungal activity in the MTs formulation.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires. Buenos Aires, Argentina. salernoclaudia@hotmail.com
authors.forename: Claudia
authors.initials: C
authors.lastname: Salerno
authors.forename: Diego A
authors.initials: DA
authors.lastname: Chiappetta
authors.forename: Alicia
authors.initials: A
authors.lastname: Arechavala
authors.forename: Susana
authors.initials: S
authors.lastname: Gorzalczany
authors.forename: Silvia L
authors.initials: SL
authors.lastname: Scioscia
authors.forename: Carlos
authors.initials: C
authors.lastname: Bregni
mesh_terms: D000287:Administration, Topical; D000666:Amphotericin B / Q000008:administration & dosage* / Q000494:pharmacology*; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D004355:Drug Stability; D005374:Filtration; D005658:Fungi / Q000187:drug effects; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D008858:Microscopy, Phase-Contrast; D011817:Rabbits; D012869:Skin Absorption / Q000187:drug effects; D023422:Skin Irritancy Tests; D017550:Spectroscopy, Fourier Transform Infrared; D055672:Static Electricity; D034421:Sus scrofa; D013696:Temperature
chemical_list: D004337:Drug Carriers; D008055:Lipids; D000666:Amphotericin B