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Article

Sustainable Stabilizer-Free Nanoparticle Formulations of Valsartan Using Eudragit® RLPO

1
Faculty of Engineering, Research Institute of Biomolecular and Chemical Engineering, University of Pannonia, Egyetem u. 10, H-8200 Veszprém, Hungary
2
Research Centre for Natural Sciences, Institute of Materials and Environmental Chemistry, Magyar Tudósok Körútja 2, H-1117 Budapest, Hungary
3
College of Pharmacy, University of Michigan, 500 S State Street, Ann Arbor, MI 48109, USA
4
Department of Pharmacy, National University of Singapore, 4 Science Drive 2, Singapore 117544, Singapore
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Arik Dahan and Michael J. Parnham
Int. J. Mol. Sci. 2021, 22(23), 13069; https://doi.org/10.3390/ijms222313069
Received: 17 November 2021 / Revised: 29 November 2021 / Accepted: 1 December 2021 / Published: 2 December 2021
(This article belongs to the Special Issue Pharmacological Plasticity)
The bioavailability of the antihypertensive drug valsartan can be enhanced by various microencapsulation methods. In the present investigation, valsartan-loaded polymeric nanoparticles were manufactured from Eudragit® RLPO using an emulsion–solvent evaporation method. Polyvinyl alcohol (PVA) was found to be a suitable stabilizer for the nanoparticles, resulting in a monodisperse colloid system ranging in size between 148 nm and 162 nm. Additionally, a high encapsulation efficiency (96.4%) was observed. However, due to the quaternary ammonium groups of Eudragit® RLPO, the stabilization of the dispersion could be achieved in the absence of PVA as well. The nanoparticles were reduced in size (by 22%) and exhibited similar encapsulation efficiencies (96.4%). This more cost-effective and sustainable production method reduces the use of excipients and their expected emission into the environment. The drug release from valsartan-loaded nanoparticles was evaluated in a two-stage biorelevant dissolution set-up, leading to the rapid dissolution of valsartan in a simulated intestinal medium. In silico simulations using a model validated previously indicate a potential dose reduction of 60–70% compared to existing drug products. This further reduces the expected emission of the ecotoxic compound into the environment. View Full-Text
Keywords: nanoparticles for drug delivery; valsartan; Eudragit®; emulsion-solvent evaporation; drug release; in silico modeling nanoparticles for drug delivery; valsartan; Eudragit®; emulsion-solvent evaporation; drug release; in silico modeling
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MDPI and ACS Style

Hajba-Horváth, E.; Fodor-Kardos, A.; Shah, N.; Wacker, M.G.; Feczkó, T. Sustainable Stabilizer-Free Nanoparticle Formulations of Valsartan Using Eudragit® RLPO. Int. J. Mol. Sci. 2021, 22, 13069. https://doi.org/10.3390/ijms222313069

AMA Style

Hajba-Horváth E, Fodor-Kardos A, Shah N, Wacker MG, Feczkó T. Sustainable Stabilizer-Free Nanoparticle Formulations of Valsartan Using Eudragit® RLPO. International Journal of Molecular Sciences. 2021; 22(23):13069. https://doi.org/10.3390/ijms222313069

Chicago/Turabian Style

Hajba-Horváth, Eszter, Andrea Fodor-Kardos, Nishant Shah, Matthias G. Wacker, and Tivadar Feczkó. 2021. "Sustainable Stabilizer-Free Nanoparticle Formulations of Valsartan Using Eudragit® RLPO" International Journal of Molecular Sciences 22, no. 23: 13069. https://doi.org/10.3390/ijms222313069

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