Nanostructured Valsartan Microparticles with Enhanced Bioavailability Produced by High-Throughput Electrohydrodynamic Room-Temperature Atomization

• DOI: 10.1021/acs.molpharmaceut.1c00098
• Publication Date: 2021-06-28T16:16:52Z
• Authors: Cristina Prieto; Zoran Evtoski; María Pardo-Figuerez; Julia Hrakovsky; Jose M. Lagaron
• Keywords: Microparticle; Dispersity

The high-throughput drying and encapsulation technique called electrospraying assisted by pressurized gas (EAPG) was used for the first time to produce nanostructured valsartan within microparticles of excipients. Valsartan, a poorly absorbed lipid-soluble drug, selected since it is considered good model BCS class II drugs. Two different polymeric matrices were as excipients, i.e., hydroxypropyl methylcellulose (HPMC) lactose monohydrate, while Span 20 surfactant. produced 80% loading formulations characterized in terms morphology, crystallinity, vitro release, Caco-2 cells' permeability, vivo pharmacokinetic study. Spherical ca. 4 μm obtained which nanoparticles seen range from 150 650 nm. Wide-angle X-ray scattering differential scanning calorimetry confirmed that had lower and/or more ill-defined crystallinity than commercial source, photon correlation spectroscopy transmission electron microscopy proved dispersed distributed form controlled size. In dissolution tests showed HPMC formulation with lowest API particle size, nm, dissolved 2.5-fold faster 10 min. This also 4-fold permeability 3-fold higher systemic exposure sample. results potential EAPG processing production safe-to-handle containing high quantities highly nanonized drug enhanced bioavailability.