DIACEREIN NANOSUSPENSION: PROCESS OPTIMIZATION, PHYSICOCHEMICAL CHARACTERIZATION, CYTOTOXICITY ASSESSMENT AND IN-VIVO EVALUATION FOR ORAL BIOAVAILABILITY ENHANCEMENT

2016-11-08T01-11-23Z
Source: Indo American Journal of Pharmaceutical Research
Abhishek Pathak*, Sadhana J Rajput.
The present research was focused on bioavailability enhancement of Diacerein (DAR) by formulating an efficient Diacerein nanosuspension (DAR-NS) through wet media milling using Poloxamer-407 (P-407) and zirconium oxide beads. A 33 factorial design was employed to evaluate the combinatorial effect of P-407 concentration, DAR concentration and milling time on the particle size (PS) and saturation solubility (SS) of DAR-NS. The morphology of DAR-NS was examined by Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The loss of crystalline nature of DAR was confirmed by Differential Scanning Calorimetry (DSC) and X-Ray Diffraction (XRD). The in-vitro studies revealed significant increment in SS and dissolution efficiency of drug in DAR-NS. The MTT assay and in-vitro permeability studies using Caco-2 cells described the reduction in cytotoxicity and improved permeation. The in-vivo studies illustrated the enhancement in oral bioavailability of drug from DAR-NS by 3.93 and 2.41 fold compared to plain DAR and commercial formulation, respectively. The DAR-NS was found to be stable at 5°C±3°C and room temperature for 6 months. These results concise that prepared nanosuspension significantly improved the oral bioavailability of DAR which could minimize the drug side effects by reducing dose frequency and thus will lead to improved patient compliance.


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