FORMULATION AND EVALUATION OF NANOSUSPENSION TO IMPROVE SOLUBILITY AND DISSOLUTION OF DIACEREIN

Diacerein is an Osteoarthritic drug that exhibited suboptimal oral bioavailability upon oral administration of conventional dosage form. Nanosuspension gaining more attention for improving oral bioavailability of such drugs. This study was aimed to enhance the solubility and dissolution of diacerein by preparing Nanosuspension. Diacerein Nanosuspension was prepared using combination of High Speed Homogenization (HSH) and Media Milling (MM), Poloxamer 407 (stabilizer) and ZrO₂ beads (milling media). Various formulation and processing parameters were optimized in preliminary studies. Concentration of stabilizer and milling media were optimized for Cumulative percentage release (%CPR), saturation solubility (SS) and mean particle size (MPS) using 3²full factorial design. Optimized batch was derived statistically using desirability function of Minitab17. Model was validated by formulating checkpoint batch. Accelerated stability study was carried out for optimized batch. Identification and compatibility study of drug and stabilizers were carried out using FTIR and DSC studies. Preliminary parameters were optimized by varying one parameter at a time, while keeping other constant by trial and error method. Optimized batch has 100%w/v milling media and 1%w/v of Poloxamer407. %CPR, SS and MPS were found to be 97.74%, 1.245mg/ml and 221.5nm respectively. Four hundred times enhancement in SS that of bulk drug and 97.74%CPR at 2min was observed after nanonization. It was concluded that Combination of HSH and MM technique can be successfully used for preparation of Diacerein Nanosuspension. Prepared nanosuspension significantly enhances solubility and in-vitro dissolution of Diacerein.