Formulation and evaluation of lipid–polymeric hybrid nanovesicles for valsartan delivery: Bridging in vitro and in vivo Pharmacokinetics

Year 2025, Volume: 45 Issue: 3, 211 - 222, 01.09.2025

Sayani Bhattacharyya , Maithili Sinha , Sweta Jha

https://izlik.org/JA39MY37SU

Abstract

Hypertension, a leading global health concern, is associated with severe cardiovascular complications. Valsartan (VAS), an angiotensin II receptor blocker, is a preferred antihypertensive medication with limited oral bioavailability (~23%) due to first-pass metabolism and P-glycoprotein (p-gp) efflux. This study developed lipid-polymeric hybrid nanovesicles of VAS using Eudragit RL100 and PEG 4000 to overcome these barriers. Lipid-polymeric nanovesicles (P1-P3) were prepared by thin-film hydration combined with solvent evaporation techniques and evaluated for drug entrapment, particle size, zeta potential, and release kinetics. Formulation P3 at Eudragit RL100:PEG 4000 in a 2:1 ratio demonstrated superior entrapment efficiency (76%), nanoscale size (140 nm), and stability, achieving a 6-fold increase in AUC compared to pure VAS. In vitro and ex vivo studies showed sustained release and enhanced intestinal permeation, with P3 achieving a 3.25-fold higher permeability. Pharmacokinetic studies confirmed enhanced bioavailability, reduced clearance, and prolonged retention. These findings underscore lipid-polymeric nanovesicles as a promising delivery system for poorly soluble drugs like VAS, addressing bioavailability challenges effectively.

Keywords

Antihypertension , Lipid-polymeric nanovesicles , Valsartan , Bioavailability

Ethical Statement

Animal usage was approved by the Krupanidhi College of Pharmacy, Institutional Animal Ethics Committee vide the approval number KCP/IAEC/COL/CEU/118/2023, dated 20th July 2023.

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