Evaluation of drug release kinetics from polymeric nanoparticles loaded with poorly water-soluble APIs

Pavaloiu, Ramona-Daniela; Sha’at, Fawzia; Hlevca, Cristina; Sha’at, Mousa; Savoiu, Gabriela; Osman, Sibel

doi:10.2478/auoc-2021-0020

Abstract

The aim of this research was to investigate the release behavior of a combination of two poorly water-soluble active pharmaceutical ingredients (APIs) from poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles. Amlodipine besylate - AML, a calcium channel blocker, and valsartan - VAL, an angiotensin II receptor antagonist drug, were used as poorly water-soluble model drugs. PLGA nanoparticles loaded with AML-VAL (1:16 w/w) were obtained by nanoprecipitation using an amphiphilic block copolymer - Pluronic F127 as stabilizer. The drugs release from the PLGA nanoparticles was determined by a dialysis membrane method under sink conditions. Nanoparticles provided a slow release for both APIs and an attenuated burst effect compared to free drug. Five kinetics models such as Zero-order, First-order, Korsmeyer-Peppas, Higuchi and Hixson-Crowell were applied to predict drug release profiles. The Higuchi and Korsmeyer-Peppas models (R² > 0.97) best described physicochemical release phenomenon for each PLGA formulations.

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Evaluation of drug release kinetics from polymeric nanoparticles loaded with poorly water-soluble APIs

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