Nanostructured Lipid Carriers for Enhanced Oral Delivery of Antidiabetic Phytochemicals

Antidiabetic phytochemicals including berberine, quercetin, and curcumin demonstrate potent pharmacological activities but are hampered by poor oral bioavailability attributable to low aqueous solubility, extensive first-pass metabolism, Pglycoprotein-mediated efflux, and limited intestinal permeability. Nanostructured lipid carriers (NLCs), second-generation lipid-based nanoparticles composed of a blend of solid and liquid lipids, represent a promising strategy to overcome these biopharmaceutical barriers. The present study describes the systematic formulation, optimisation, and in vitro evaluation of berberine-loaded NLCs (NLC-F1 to NLC-F8) prepared by hot melt homogenisation-ultrasonication. Formulations were characterised for particle size, polydispersity index (PDI), zeta potential, encapsulation efficiency (EE%), and drug loading. The optimised formulation NLC-F3 exhibited a particle size of 148.2 ± 3.6 nm, PDI of 0.198 ± 0.009, zeta potential of −38.2 ± 1.4 mV, and EE of 91.8 ± 1.6%. In vitro drug release studies demonstrated 88.6% cumulative release at 24 h at pH 6.8. Caco-2 permeability studies confirmed a 3.02-fold improvement in apparent permeability coefficient compared to pure berberine. NLC-F3 also exhibited superior α-glucosidase inhibitory activity (IC₅₀ = 38.6 μg/mL) relative to free berberine (IC₅₀ = 68.4 μg/mL; p < 0.001). These findings confirm that NLC encapsulation significantly enhances oral bioavailability and antidiabetic efficacy of berberine, warranting further preclinical and clinical investigation.

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