Liranaftate loaded Xanthan gum based hydrogel for topical delivery: Physical properties and ex-vivo permeability.

A topical microemulsion (ME)-based hydrogel was developed to enhance permeation of an antifungal drug, liranaftate (LRFE) for effective eradication of cutaneous fungal infection. Pseudo-ternary phase diagrams were used to determine the existence of MEs region. ME formulations were prepared with Di-isopropyl adaptate, Cremophore-EL, Ethanol and distilled water. Xanthan Gum (1.5% w/w) was used for preparation of hydrogel of LRFE microemulsion (HLM) and characterized. The in-vitro and ex-vivo evaluation of prepared HLM and saturated drug solution were compared. The viscosity, average droplet size and pH of HLM were 142.30±0.42 to 165.15±0.21Pas, 52.53-93.40nm and 6.6-7.1, respectively. Permeation rate of LRFE from optimized formulation (HLM-3), composed with Di-isopropyl adaptate (4.5% w/w), Cremophor-EL (30% w/w), Ethanol (10% w/w) and water (52% w/w) was observed higher in compare with other HLMs and saturated drug solution. HLM-3 was stable, six times higher drug deposition capacity in skin than saturated drug solution and did not caused any erythema based on skin sensitivity study on rat. The average zone of inhibition of HLM-3 (25.52±0.26mm) was higher in compare with saturated drug solution (13.44±0.40mm) against Candida albicans.

Effect of microemulsion in topical sertaconazole hydrogel: in vitro and in vivo study.

PURPOSE: 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. CONCLUSION: 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.

Microemulsion based topical hydrogel of sertaconazole: formulation, characterization and evaluation.

A microemulsion (ME) based hydrogel had studied as a topical delivery of sertaconazole (STZL) for effective eradication of cutaneous fungal infection. The existence of microemulsion region was investigated in pseudo-ternary phase diagrams and various ME formulations were prepared using oleic acid, Tween 80, propylene glycol and water. Hydrogel of STZL microemulsions (HSM) were prepared in Carbopol 940 (0.75%, w/w) and characterized. The prepared HSM and commercial cream of STZL were evaluated in vitro and ex vivo. The permeation rate of STZL from optimized formulation (HSM-4), composed with oleic acid (8.75%, w/w), tween 80 (33.35%, w/w), propylene glycol (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, had 3 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±0.72mm) was higher in compare with commercial cream (16.53±0.63mm) against Candida albicans which may be due to permeation enhancing effect of ME and skin retention effect of HSM. It is promising that the concentration of STZL used to treat cutaneous fungal infection could be decreased due to the high permeation and anti-fungal effect of STZL in HSM-4.