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.
Highlights
Bioavailability is a key requirement for the application of bioactive compounds in pharmaceutical drug products [1]
To understand the surface-active behavior of Eudragit® RLPO, the interfacial tension (IFT) of a solution of the polymer was measured in presence of 1% of Polyvinyl alcohol (PVA)
A broad array of formulation strategies is aiming at the development of more sustainable drug products with high therapeutic efficacy
Summary
Bioavailability is a key requirement for the application of bioactive compounds in pharmaceutical drug products [1]. Novel formulation strategies often lead to improved bioavailability and allow dose reduction while achieving similar therapeutic effects in patients [2]. They contribute to more sustainable use of drug substances by reducing drug emissions released into the environment [3]. Common monomers include methacrylic acid, methacrylic acid esters, and dimethylaminoethyl methacrylate Their pH-dependent water solubility enables the modulation of the drug release in different segments of the human gastrointestinal tract. Mesoporous silica nanoparticles were used to enhance the oral bioavailability and antihypertensive activity of valsartan [12] They were functionalized with aminopropyl groups and coated with the pH-sensitive polymer Eudragit® L100-55. Conditions in the human gastrointestinal tract were simulated in vitro using fasted-state simulated gastric fluid (FaSSGF) and fasted-state simulated intestinal fluid (FaSSIF)
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