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Enhancement of bioavailability of nebivolol hydrochloride through liquisolid formulations: In Vitro and In Vivo evaluation | Abstract
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Abstract

Enhancement of bioavailability of nebivolol hydrochloride through liquisolid formulations: In Vitro and In Vivo evaluation

Author(s): Pravala K, Vijay Kumar Nagabandi, Ajmeera Divya

Nebivolol hydrochloride {α, α’-[iminobis (methylene) bis [6-fluoro-3, 4-dihydro-2H-1-benzopyran-2-methanol] hydrochloride} is a selective β1- antagonist falls under class II biopharmaceutical classification system. In this present study liquisolid technique was applied to improve the solubility and dissolution properties thereby enhancing the oral bioavailability of nebivolol hydrochloride. Different formulations were developed by dissolving the drug in various non-volatile liquid vehicles like PEG 400, Propylene glycol, Tween 80 and Glycerine using Avicel PH 102, Lactose Monohydrate and Syloid 244 FP as carriers and Aerosil as coating material. In vitro drug release profiles of liquisolid compacts shown enhanced drug release when compared to pure drug as well as marketed formulation and the formulation containing PEG 400 (25%w/w) as solvent with syloid 244 FP and Aerosil (30:1) shown maximum dissolution rate compared to other formulations. The in vivo studies indicated that the enhanced bioavailability in case of liqisolid formulations which might be due to increased wetting properties and more surface of drug available for dissolution. XRD and FTIR studies conformed that there was no interaction between drug and excipients used. From this study we can conclude that liquisolid technique is one of the promising alternative techniques to improve the dissolution rate of class II drugs.