FORMULATION AND EVALUATION OF 2% CRISABOROLE OINTMENT BY COSOLVENCY METHOD

Abstract

The aim of the present study is to increase the solubility as well as dissolution rate of Crisaborole drug by the preparation of crisaborole ointment 2% by cosolvency method by using hard paraffin wax, propylene glycol and PEG 400 as cosolvents. This approach of delivering drug is mostly suitable for lipophilic drug and poorly or water insoluble drugs. Crisaborole belongs to class IΙ under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility 0.0234 mg/ml. Hence it is necessary to increase the solubility of drug. The crisaborole ointment was prepared by using paraffin wax as base of the ointment, propylene glycol and PEG 400 as aqueous solvent to increase the solubility and dissolution profile. The prepared ointment was evaluated for Physical Analysis, pH measurements, Rheological Properties (Viscosity), Spread ability, Solubility study, Drug content, In-vitro release studies and Stability study of the formulations. The saturated solubility studies and In-vitro dissolution studies as observes that the increase in solubility of drug and enhanced dissolution rate in ointment as compared to pure drug. From the result of saturation solubility studies it was observed that there was an increase in solubility of drug in ointment formulations as compared to pure drug. With increase in the concentration of co-solvents solubility of drug increased and the ointment containing propylene glycol and polyethylene glycol (F5) and (F6) has increased the solubility up to five times. This improves its wettability resulting in a significant increase in solubility.