Nano-liposomal encapsulation of isorhamnetin to enhance bioavailability and anticancer efficacy.

Abstract

This study aimed to improve the bioavailability and anticancer efficacy of isorhamnetin (Iso), a flavonoid with poor water solubility, by encapsulating it into nanoliposomes and evaluating their effects. Iso-loaded nanoliposomes (Iso.NLP) were prepared via thin-film hydration and characterised for particle size, morphology, polydispersity index (PDI), zeta potential, and entrapment efficiency (EE%). In vitro drug release, stability at 4 °C, cytotoxicity against MCF-7 cells, and cellular uptake using FITC-labelled Iso.NLP were assessed. Optimised Iso.NLP were spherical (101-168 nm) with zeta potentials of -16.5 to -4.5 mV and EE% of 87-94%. Iso.NLP2 showed sustained release (∼65% in 24 h vs. 100% free Iso in 6 h), stable for ≥10 days at 4 °C. MTT assay revealed higher cytotoxicity for Iso.NLP2 (42.5% viability) versus free Iso (71.2%, 4 µM; p < 0.01). Cellular uptake was markedly enhanced. Iso.NLPs improved Iso's bioavailability and anticancer efficacy, supporting their potential for further studies in breast cancer therapy.