Journal of Pharmaceutical Research International

Aim: An attempt was made to improve the solubility and to achieve better penetration of antifungal agent lawsone a poorly water-soluble naphthoquinone, derivative via co-crystallization to treat cutaneous candidiasis.

Methodology: The co-crystals of lawsone were prepared using benzoic acid as co former by solvent crystallization method. The formulated co-crystals were assessed for different parameters namely, saturation solubility, thermal properties, crystalline nature, particle size and its antifungal activity against Candida albicans.

Results: Lawsone co-crystals exhibited enhanced solubility of lawsone (9.57±2.5 mg/ml and 0.523±0.23 mg/ml respectively) and the particle size of the co-crystals were reduced to 560±2.2 nm as compared to pure lawsone (2478±1.5 nm) which further resulted in enhancement of antifungal activity. Lawsone co-crystals were loaded in the xanthan-gel base for easy applicability to the skin and to achieve patient compliance. The prepared gel was evaluated in terms of spreadability, adhesiveness, in vitro diffusion, viscosity, and antifungal activity. 

Conclusion: Lawsone co-crystals loaded gel showed enhanced retension of drug in the skin as compared to plain lawsone gel. The antifungal potential of lawsone co-crystals loaded gel was at par with marketed Clotrimazole gel formulation. The short-term stability study carried out as per ICH guideline indicated that the formulation was stable. Lawsone co-crystals loaded gel.