Nanostructured Valsartan Microparticles with Enhanced Bioavailability Produced by High-Throughput Electrohydrodynamic...

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Nanotechnology

Background:

• Valsartan, a BCS class II drug, exhibits poor absorption and high lipid solubility, necessitating advanced formulation strategies.
• Traditional methods often struggle to enhance the bioavailability of such challenging drug compounds.

Purpose of the Study:

• To utilize electrospraying assisted by pressurized gas (EAPG) for the first time to create nanostructured valsartan within microparticles.
• To evaluate the potential of EAPG in improving the physicochemical properties and *in vivo* performance of a model BCS class II drug.

Main Methods:

• Production of 80% valsartan-loaded microparticles using EAPG with hydroxypropyl methylcellulose (HPMC) or lactose monohydrate as excipients.
• Characterization included morphology, crystallinity (XRD, DSC), nanoparticle size (PCS, TEM), *in vitro* dissolution, Caco-2 cell permeability, and *in vivo* pharmacokinetics.

Main Results:

• EAPG yielded spherical microparticles (approx. 4 μm) containing valsartan nanoparticles (150-650 nm).
• Valsartan exhibited reduced and less defined crystallinity within the microparticles.
• The HPMC formulation with 150 nm valsartan nanoparticles showed 2.5x faster dissolution, 4x higher *in vitro* permeability, and 3x greater systemic exposure compared to commercial valsartan.

Conclusions:

• EAPG is a promising high-throughput technique for producing microparticles with high drug loading of nanonized BCS class II drugs.
• The developed formulations demonstrate significantly enhanced bioavailability, highlighting the potential of EAPG for improving drug delivery.