Abstract

DESIGN AND DEVELOPMENT OF NANOSUSPENSION OF ITACONAZOLE

Maniraj Singh*, Aditya Tiwari and Dr. Nitendra kumar sahu

ABSTRACT

The aim of present study was to design and evaluate Nanosuspension of poorly water soluble drug. Nanosuspension provides efficient formulation advantages as it could be used to improve the solubility of the selected drug. This would be accompanied by increased dissolution, permeation, absorption and overall bioavailability of the drug leading to a possibility of decreased doses and cost of therapy. The drug selected for this study was Itraconazole (ITZ). The optimized Nanosuspension were evaluated for particle size, zeta potential using particle size analyzer, zeta potential analyzer respectively and solubility enhancement study. The higher molecular weight of Poloxamer-407 (vs. Poloxamer-188 and Tween 80) and its relatively longer polymer chains lead to a higher degree of steric stabilization for the drug particles, which can enhance particle dispersion and result in a greater extent of size reduction. Although steric stabilization is not associated with SLS, the relatively high zeta potential keeps the drug particles well dispersed via electrostatic repulsion/stabilization. The batch of nanosuspension containing both Poloxamer- 407and SLS was found to be optimized. This batch was subjected to go through different bar pressure with change numbe of cycles. Optimized Nanosuspension formulation was found to be efficient with average particle size in the range of 600nm to 800nm (613 nm), zeta potential in the range of -40mV to -60mV, PI in the range of 0.5 to 0.6 (0.542).In comparison to plain drug, developed nanosuspension showed significant enhancement in aqueous solubility (nearly 9 folds) of Itraconazole. Optimized spray dried powder formulation was found to be efficient with average particle size in the range of 600nm to 800nm (733.8nm), PI in th erange of 0.7 to 0.8 (0.706). Agglomaration was observed (Large increase in particle size) after spray drying of nanosuspension, this problem was overcome by using Mannitol as adsorbent. Optimized spray dried powder formulation showed complete drug release at 90 min in both dissolution media i.e. Phosphate buffer pH 6.8 and Hydrochloric acid pH1.2 The routine tests of reconstituted nanosuspension, such as viscosity, sedimentation volume, redispersibility and degree of flocculation were found to be acceptable. The Nanosuspension, spray dried powder of Itraconazole were assessed for stability at 40°C/75% RH for aperiod of 2months respectively.

Keywords: Nanosuspension, Itraconazole, Poloxamer-188, Tween 80, Evaluation.