Effects of lipid nanoparticles on physicochemical properties, cellular uptake, and lymphatic uptake of 6-methoxflavone

초록

Purpose Recently, therapeutic effects of 6-methoxyflavone (6MF) have been reported. However, the use of 6MF is limited due to its poor water solubility. The low aqueous solubility of 6MF results in its low plasma level after oral administration, which limits its clinical application. Lymphatic uptake is a promising way to enhance oral bioavailability. Thus, the purpose of this study was to investigate the effect of solid lipid nanoparticles (SLN) and nanostructured lipid carrier (NLC) on the lymphatic uptake of 6MF. Methods 6MF-loaded solid lipid nanoparticle (6MF-SLN) and 6MF-loaded nanostructured lipid carrier (6MF-NLC) were fabricated with a hot homogenization and sonication technique. These 6MF-SLN and 6MF-NLC were characterized for their particle sizes, zeta potentials, in vitro release, cytotoxicity, and cellular uptake. They were also subjected to in vivo lymphatic uptake studies. Results In this study, 6MF-SLNs and 6MF-NLC were fabricated to achieve improved oral bioavailability and sustained therapeutic effect of 6MF. The composition of lipid matrix affected physicochemical properties and release profiles of 6MF. Encapsulation of 6MF in lipid nanoparticles resulted in an enhanced cellular uptake in Caco-2 cells. In vivo lymphatic uptake study in rats revealed that SLN and NLC significantly improved lymphatic uptake of 6MF than the control without SLN or NLC (6MF alone). Conclusion SLN and NLC could be promising oral delivery platforms for 6MF.

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