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- Title
Sustainable Stabilizer-Free Nanoparticle Formulations of Valsartan Using Eudragit ® RLPO.
- Authors
Hajba-Horváth, Eszter; Fodor-Kardos, Andrea; Shah, Nishant; Wacker, Matthias G.; Feczkó, Tivadar
- Abstract
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.
- Subjects
VALSARTAN; BIODEGRADABLE nanoparticles; NANOPARTICLES manufacturing; POLYVINYL alcohol; ANTIHYPERTENSIVE agents; BIOMEDICAL adhesives; DRUG bioavailability; MONODISPERSE colloids
- Publication
International Journal of Molecular Sciences, 2021, Vol 22, Issue 23, p13069
- ISSN
1661-6596
- Publication type
Article
- DOI
10.3390/ijms222313069