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Formulation and in-vitro Evaluation of Supersaturable Dry Micro-emulsion for the Enhancement of Dissolution | Abstract
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Abstract

Formulation and in-vitro Evaluation of Supersaturable Dry Micro-emulsion for the Enhancement of Dissolution

Author(s): Nitin Londhe, Pallavi Chede

The present study deals with formulation of Supersaturable solid self-microemulsifying drug delivery system of poorly water soluble drug.SMEDDS are isotropic mixtures of oil, surfactant, co-surfactant and drug that form a fine oil-in-water emulsion when introduced into aqueous phase under gentle agitation. The present research work describes a Supersaturable solid self-microemulsifying drug delivery system of Nebivolol using Castor oil, Tween 80 and PEG 400. Nebivolol is a cardioselective β-adrenergic receptor antagonist with limited water solubility which accounts for low oral bioavailability (12%). Hence, the main objective of study was to formulate Supersaturable S-SMEDDS of Nebivolol in order to achieve a better dissolution rate which would further help in enhancing oral bioavailability using HPMC as PPI.Pseudo-ternary phase diagrams were plotted to check for the micro-emulsification range and to evaluate the effect of Nebivolol on the emulsification behavior of the phases. Prepared SMEDDS formulations were tested for microemulsifying properties and microemulsions were evaluated for robustness to dilution, assessment of efficiency of self emulsication, emulsification time, viscosity, drug content and in-vitro dissolution. The optimized SMEDDS formulation further evaluated for centrifugation studies, freeze thaw cycling, particle size distribution, DSC, SEM and zeta potential were carried out to confirm the stability of the formed SMEDDS. The liquid formulation was solidified by using spray dryer, using Aerosil 200 as solid carrier. Thus Supersaturable S-SMEDDS of Nebivolol may provide the useful solid dosage form for oral poorly water soluble drugs.