Comparative study of transdermal drug delivery systems of resveratrol: High efficiency of deformable liposomes

Abstract

Trans-resveratrol (3, 5, 4′ trihydroxystilbene, RSV) is a natural compound that shows antioxidant, cardioprotective, anti-inflammatory and anticancer properties. The transdermal, painless application of RSV is an attractive option to other administration routes owing to its several advantages like avoiding gastrointestinalproblems and first pass metabolism. However, its therapeutic potential is limited by its low solubility and lowstability in water and the reduced permeability of stratum corneum. To overcome these inconveniences theencapsulation of this compound in a drug delivery system is proposed here. In order to find the best carrier fortransdermal application of RSV various liposomal nanoparticulate carriers like conventional liposomes (L-RSV),deformable liposomes (LD-RSV), ultradeformable liposomes (LUD-RSV) and ethosomes (Etho-RSV) were assayed. Transmission electron microscopic (TEM) and dynamic light scattering (DLS) studies were performed toanalyze the surface morphology of these carriers. Structural characterization for these formulations was performed by confocal Raman spectroscopy. The spectroscopic results were analysed in conjunction with calorimetric data to identify the conformational changes and stability of formulations in the different nanoparticlesinduced by the presence of RSV.Comparison of the results obtained with the different carrier systems (L-RSV, LD-RSV, LUD-RSV and EthoRSV) revealed that the best RSV carrier was LD-RSV. The increase in the fluidity of the bilayers in the region ofthe hydrophobic chains of the phospholipid by ethanol probably facilitates the accommodation of the RSV in thebilayer and contributes to the improved encapsulation of RSV without affecting the mobility of this carrier.