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<p>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 (R<sup>2</sup> > 0.97) best described physicochemical release phenomenon for each PLGA formulations.</p>
</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.

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

Grigore T. Popa University of Medicine and Pharmacy

Department of Chemistry and Chemical Engineering

Ovidius University Annals of Chemistry

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

The aim of this research was to investigate the release behavior of a combination of two poorly water-soluble active pharmaceutical ingredients (APIs) from...

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

Published Online: Dec 10, 2021

Page range: 132 - 136

Received: Jun 03, 2021

Accepted: Nov 19, 2021

DOI: https://doi.org/10.2478/auoc-2021-0020

Keywords
nanoparticles, amlodipine, valsartan, drug release

© 2021 Ramona-Daniela Pavaloiu et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

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

Published Online: Dec 10, 2021

Page range: 132 - 136

Received: Jun 03, 2021

Accepted: Nov 19, 2021

DOI: https://doi.org/10.2478/auoc-2021-0020

Keywordsnanoparticles, amlodipine, valsartan, drug release

© 2021 Ramona-Daniela Pavaloiu et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Keywords
nanoparticles, amlodipine, valsartan, drug release