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Bioavailability enhancement

01

Overview

Bioavailability enhancement refers to a set of formulation and chemical strategies applied to pharmaceuticals to increase the proportion of an administered active pharmaceutical ingredient (API) that reaches systemic circulation and the site of action. Techniques for bioavailability enhancement include improving drug solubility (through nanoparticle formation, solid dispersions, salt formation, or micellization), increasing permeability, reducing particle size (micronization or nanonization), using permeability and metabolism enhancers, and optimizing formulation through excipients or delivery systems[1][2][3][4][5][6][7][8]. This is especially important for drugs with poor water solubility (such as BCS Class II and Class IV compounds), as low bioavailability can limit therapeutic efficacy, require higher doses, and cause greater side effects. While bioavailability enhancement is crucial in drug development, it describes a technological process and not a discrete molecular target, and thus is not appropriately classified as a therapeutic target for pharmacological intervention[1][2][3].

Other names
Bioavailability boostingdrug absorption enhancementsolubility enhancementpermeability enhancementformulation optimization

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