Effect of microemulsion in topical sertaconazole hydrogel: in vitro and in vivo study.
OBJECTIVE
A topical microemulsion (ME)-based hydrogel was developed to enhance permeation of an antifungal drug, sertaconazole (STZL) for effective eradication of cutaneous fungal infection.


METHODS
Pseudo-ternary phase diagrams were used to determine the existence of MEs region. ME formulations were prepared with oleic acid, Tween 80, propylene glycol (PG) and water. Carbopol 940 (0.75% w/w) was used for preparation of hydrogel of STZL microemulsion (HSM) and characterized. The in vitro and in vivo evaluation of prepared HSM and commercial cream of STZL were compared.


RESULTS
The viscosity, average droplet size and pH of HSM were 154.23 ± 0.54 to 162.52 ± 0.21 Pas, 42.3-91.7 nm and 6.9-7.2, respectively. Permeation rate of STZL from optimized formulation (HSM-4), composed with oleic acid (8.75 % w/w), Tween 80 (33.35% w/w), PG (33.35% w/w) and water (24.55% w/w) was observed higher in compare with other HSMs and commercial cream. HSM-4 was stable, three times higher drug retention capacity in skin than commercial cream and did not caused any erythema or edema based on skin sensitivity study on rabbit. The average zone of inhibition of HSM-4 (23.54 ± 0.72 mm) was higher in compare with commercial cream (16.53 ± 0.63 mm) against Candida albicans.


CONCLUSIONS
The results of study showed that ME played a major role in permeation enhancing and skin retention effect of HSM and the concentration of STZL used for cutaneous fungal infection could be decreased by using ME based hydrogel preparation.
a Department of Pharmaceutics , Gayatri College of Pharmacy , Sambalpur , Odisha , India and.
Susijit
S
Sahoo
a Department of Pharmaceutics , Gayatri College of Pharmacy , Sambalpur , Odisha , India and.
Nihar Ranjan
NR
Pani
b University Department of Pharmaceutical Sciences , Utkal University , Bhubaneswar , Odisha , India.
Sunit Kumar
SK
Sahoo
D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D002176:Candida albicans / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003881:Dermatomycoses / Q000188:drug therapy; D004655:Emulsions; D004890:Erythema / Q000139:chemically induced; D005079:Excipients; D006801:Humans; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate / Q000737:chemistry*; D007093:Imidazoles / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D011817:Rabbits; D012869:Skin Absorption; D013876:Thiophenes / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D014783:Viscosity
D000935:Antifungal Agents; D004655:Emulsions; D005079:Excipients; D007093:Imidazoles; D013876:Thiophenes; D020136:Hydrogel, Polyethylene Glycol Dimethacrylate; C061131:sertaconazole
Hydrogel; in vitro study; in vivo study; microemulsion; sertaconazole