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

• Published in: Materials Science & Engineering C Vol. 90; pp. 356 - 364
• Main Authors: Tosato, Maira Gaspar, Maya Girón, Julie V., Martin, Airton A., Krishna Tippavajhala, Vamshi, Fernández Lorenzo de Mele, Mónica, Dicelio, Lelia
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.09.2018; Elsevier BV
• Subjects: Administration, Cutaneous; Anticancer properties; Antioxidants; Comparative studies; Confocal Raman spectroscopy; Data processing; Deformation; Drug delivery; Drug delivery systems; Drug Delivery Systems - methods; Drug therapy; Dynamic Light Scattering; Encapsulation; Ethanol; Ethanol - chemistry; Ethosomes; Fluidity; Formability; Formulations; Hydrophobicity; Inflammation; Light scattering; Liposomes; Liposomes - chemistry; Materials science; Metabolism; Microscopy, Electron, Transmission; Morphology; Nanoparticles; Nanoparticles - chemistry; Permeability; Phospholipids; Photon correlation spectroscopy; Polysorbates - chemistry; Raman spectroscopy; Resveratrol; Skin Absorption; Spectrum analysis; Spectrum Analysis, Raman; Stability; Stilbenes - chemistry; Stratum corneum; Structural analysis; Transdermal drug delivery; Transdermal medication; Nanoparticles; Transdermal drug delivery; Confocal Raman spectroscopy; Liposomes; Resveratrol
• ISSN: 0928-4931; 1873-0191
• DOI: 10.1016/j.msec.2018.04.073

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 gastrointestinal problems and first pass metabolism. However, its therapeutic potential is limited by its low solubility and low stability in water and the reduced permeability of stratum corneum. To overcome these inconveniences the encapsulation of this compound in a drug delivery system is proposed here. In order to find the best carrier for transdermal 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 to analyze 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 nanoparticles induced by the presence of RSV. Comparison of the results obtained with the different carrier systems (L-RSV, LD-RSV, LUD-RSV and Etho-RSV) revealed that the best RSV carrier was LD-RSV. The increase in the fluidity of the bilayers in the region of the hydrophobic chains of the phospholipid by ethanol probably facilitates the accommodation of the RSV in the bilayer and contributes to the improved encapsulation of RSV without affecting the mobility of this carrier. [Display omitted] •Four transdermal drug delivery systems of resveratrol (RSV) was assayed and characterized.•The best carrier for RSV was deformable liposome with 91.8% encapsulation efficiency.•Tween 80 and the adequate amount of ethanol contribute to the improved encapsulation.•Ordered rearrangements between the lipids chains of LD were found after RSV adding.