Design, Preparation, and ex vivo Skin Permeation of Naringenin Liposomal Formulation for Topical Delivery

Abstract

Background: Naringenin is one of the most important flavonoids in the class of flavanones. It has interesting medicinal properties, including anti-cancer, antioxidant, and anti-inflammatory effects. However, low water solubility and low oral bioavailability limit the use of this natural product. The aim of this study was to prepare and introduce a new anti-inflammatory topical formulation of naringenin with effective and enhanced dermal permeability. Methods: Eight liposomal formulations of naringenin were prepared using cholesterol and egg lecithin by the thin-film hydration method. The variables of this study were cholesterol level, lecithin level, and duration of sonication. After preparation, physicochemical properties such as particle size, loading percentage, release profile, and permeability of rat abdominal skin were evaluated using Franz diffusion cells in all formulations. Results: The results of this study showed that the prepared liposomal formulations had a particle size in the range of 76.85 to 169 nm. The loading percentage in all formulations was in the range of 98.01 to 99.11%. Evaluation of the release profile showed that the release kinetics in all formulations followed a first-order release model. Examination of permeability and related parameters showed that the levels of permeability coefficient (P), diffusivity coefficient (Dapp​), and fluxes (Jss​) in all liposomal formulations were significantly higher compared to the drug saturation solution. Conclusions: The results show that the naringenin liposomal formulation has good physicochemical properties. The topical application of naringenin as a liposomal formulation (specifically formulation LIP-NG-8) can overcome drug delivery limitations such as low solubility.