Abstract
Objective: The aim of this study was to investigate the potential of a liquisolid system to improve the dissolution rate and the bioavailability of nebivolol hydrochloride. Methods: Solubility of nebivolol was determined in different nonvolatile solvents to finalize the best nonvolatile vehicle having maximum solubility. The liquisolid compacts were prepared using Fujicalin as a carrier material, Aerosil 200 as a coating material, Polyethylene glycol 400 as a liquid vehicle, and Croscarmellose sodium as a super disintegrating agent. 23 full factorial design was used to optimize the formulation in which the drug concentration, PVP K 30, Excipient ratio (R), and nebivolol containing nonvolatile solvent liquid level were selected as independent variables by using design expert software. The eight liquisolid compact formulations were prepared. Nebivolol liquisolid compacts were evaluated for drug content, tablet hardness, Friability, disintegration, and dissolution. An in vivo study was carried out in male Wistar rats. Results: The solubility of nebivolol hydrochloride in polyethylene glycol 400 was found to be greater than the other nonvolatile solvents. The liquisolid system of nebivolol was formulated successfully using Fujicalin, Aerosil 200, and polyethylene glycol 400. In vitro evaluation parameters for the liquisolid compact were within the prescribed limits. It was found that optimized liquisolid tablet formulation showed higher dissolution than the marketed tablet, with 88.33±0.94 % drug release within 120 min and the drug release was more than 75 % in 30 min for nebivolol LS-3N, which is optimized. LS-3N liquisolid compacts follow the Peppas model and exhibited first-order release. Conclusion: The liquisolid compacts can be a promising alternative for the formulation of water-insoluble drug nebivolol hydrochloride with improved dissolution and bioavailability.
Highlights
According to the biopharmaceutical classification system (BCS), drug candidates featuring poor solubility and high membrane permeability are categorized as BCS class 2, for which the oral absorption is often limited by the dissolution rate in the gastrointestinal tract
The selection of nonvolatile solvent with a high solubilizing capacity for the drug leads to an increased fraction of molecularly dispersed nebivolol which in turn leads to enhanced drug release [47]
The angle of slide test was performed to assess the flow properties of liquid/powder admixtures of various excipients employed in the formulation of liquisolid compacts of nebivolol
Summary
The most convenient and commonly employed route of drug delivery is oral ingestion. The oral route remains the preferred route of drug administration due to its convenience, better patient compliance, and low production costs [1, 2]. The term "liquisolidmedication" implies oily liquid drugs and solutions or suspensions of water-insoluble solid drugs carried in suitable nonvolatile solvent systems. Using this new formulation technique, a liquid medication may be converted into a dry-looking, non-adherent, free flowing and compressible powder by a simple blending with selected powder excipients referred to as the carrier and coating materials [15]. The liquisolid tablets that contain water-insoluble drugs are expected to enhance drug dissolution because of the increased wetting properties of the drug particles and the large surface area available for dissolution. The liquisolid tablets are suitable to formulate low-dose water-insoluble drugs [17]
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