title: Topical Amphotericin B solid lipid nanoparticles: Design and development.
abstract: The present work is focused on design and development of topical Amphotericin B solid lipid nanoparticles (SLNs) to improve the therapeutic antifungal activity. Amphotericin B loaded SLNs were prepared by novel solvent diffusion method and were characterized for particle size, zeta potential, drug entrapment, surface morphology, in vitro antifungal activity, ex vivo permeation, retention and skin-irritation. Optimized SLNs were spherical with average size of 111.1±2.2nm, zeta potential of -23.98±1.36mV and 93.8±1.8% of drug entrapment. Characterization of Amphotericin B SLNs by differential scanning calorimetry, Fourier transform infrared spectroscopy and Powder X-ray diffraction studies revealed absence of interaction between Amphotericin B and lipid. Amphotericin B is well dispersed in the lipid matrix without any crystallization. The SLNs were lyophilized with and without cryoprotectants to evaluate the stability and it was observed that the particle size of the SLNs significantly increased in SLN formulations lyophilized without cryoprotectant. The optimized SLN 5 formulation exhibited 2 fold higher drug permeation as compared to plain drug dispersion and higher zone of inhibition in Trichophyton rubrum fungal species. Formulation was found to be stable at 2-8°C and 25±2°C for the period of three months. Results of present study indicate that SLNs are suitable carriers for entrapment of poorly water soluble drugs and for enhancement of therapeutic efficacy of antifungal drug.
authors.affiliation: Pharmacy Department, Faculty of Technology & Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara 390 001, Gujarat, India.
authors.forename: Dhruv
authors.initials: D
authors.lastname: Butani
authors.affiliation: Pharmacy Department, Faculty of Technology & Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara 390 001, Gujarat, India.
authors.forename: Chetan
authors.initials: C
authors.lastname: Yewale
authors.affiliation: Pharmacy Department, Faculty of Technology & Engineering, The Maharaja Sayajirao University of Baroda, Kalabhavan, Vadodara 390 001, Gujarat, India. Electronic address: misraan@hotmail.com.
authors.forename: Ambikanandan
authors.initials: A
authors.lastname: Misra
mesh_terms: D000279:Administration, Cutaneous; D000666:Amphotericin B / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001692:Biological Transport; D004075:Diglycerides / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D004339:Drug Compounding; D004355:Drug Stability; D005227:Fatty Acids / Q000737:chemistry*; D005260:Female; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D010316:Particle Size; D010539:Permeability; D020442:Poloxamer / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D004075:Diglycerides; D004337:Drug Carriers; D005227:Fatty Acids; D011136:Polysorbates; D013501:Surface-Active Agents; D020442:Poloxamer; C086409:glyceryl behenate; D000666:Amphotericin B; C009032:precirol
keywords: Amphotericin B; Antifungal; Drug permeation; Drug retention; SLN; Solvent diffusion