Nanoemulsion gel-based topical delivery of an antifungal drug: in vitro activity and in vivo evaluation.
OBJECTIVE
In this study, attempt has been focused to prepare a nanoemulsion (NE) gel for topical delivery of amphotericin B (AmB) for enhanced as well as sustained skin permeation, in vitro antifungal activity and in vivo toxicity assessment.


MATERIALS AND METHODS
A series of NE were prepared using sefsol-218 oil, Tween 80 and Transcutol-P by slow spontaneous titration method. Carbopol gel (0.5% w/w) was prepared containing 0.1% w/w AmB. Furthermore, NE gel (AmB-NE gel) was characterized for size, charge, pH, rheological behavior, drug release profile, skin permeability, hemolytic studies and ex vivo rat skin interaction with rat skin using differential scanning calorimeter. The drug permeability and skin irritation ability were examined with confocal laser scanning microscopy and Draize test, respectively. The in vitro antifungal activity was investigated against three fungal strains using the well agar diffusion method. Histopathological assessment was performed in rats to investigate their toxicological potential.


RESULTS AND DISCUSSION
The AmB-NE gel (18.09 ± 0.6 µg/cm(2)/h) and NE (15.74 ± 0.4 µg/cm(2)/h) demonstrated the highest skin percutaneous permeation flux rate as compared to drug solution (4.59 ± 0.01 µg/cm(2)/h) suggesting better alternative to painful and nephrotoxic intravenous administration. Hemolytic and histopathological results revealed safe delivery of the drug. Based on combined results, NE and AmB-NE gel could be considered as an efficient, stable and safe carrier for enhanced and sustained topical delivery for AmB in local skin fungal infection.


CONCLUSION
Topical delivery of AmB is suitable delivery system in NE gel carrier for skin fungal infection.
['Hussain|Afzal|A|', 'Samad|Abdus|A|', 'Singh|S K|SK|', 'Ahsan|M N|MN|', 'Haque|M W|MW|', 'Faruk|A|A|', 'Ahmed|F J|FJ|']
D000180:Acrylic Resins D000279:Administration, Cutaneous D000666:Amphotericin B D000818:Animals D000935:Antifungal Agents D001230:Aspergillus D002152:Calorimetry, Differential Scanning D002176:Candida albicans D052978:Disk Diffusion Antimicrobial Tests D004337:Drug Carriers D004339:Drug Compounding D004655:Emulsions D005026:Ethylene Glycols D005260:Female D005782:Gels D006461:Hemolysis D006801:Humans D006863:Hydrogen-Ion Concentration D008055:Lipids D008297:Male D018613:Microscopy, Confocal D053758:Nanoparticles D036103:Nanotechnology D010316:Particle Size D010539:Permeability D011108:Polymers D011136:Polysorbates D011409:Propylene Glycols D017208:Rats, Wistar D012212:Rheology D012867:Skin D012869:Skin Absorption D012995:Solubility D013499:Surface Properties D013678:Technology, Pharmaceutical
nanoemulsion topical delivery gel Amphotericin B nephrotoxicity