| Abstrakt: |
Background: Clinically, melatonin (MLT) has variable oral absorption and extensive first‐pass effect, making its oral mode less preferable. Ethosomes are able to permeate intact through the human skin due to its high deformability. Aim: Present study assessed topical potential of ethosomes loaded with MLT for the prevention of UV radiation. Methods: Melatonin was encapsulated using different ratios of ethanol, soya lecithin, and cholesterol. Prepared ethosomes were characterized for scanning electron microscopy (SEM), zeta potential, % entrapment efficiency (%EE), in vitro drug release kinetics. Then, optimized formulation was incorporated in gel and evaluated for viscosity, pH, extrudability, homogeneity, skin irritation study, spreadability, in vitro skin permeation study, flux, and stability. Results: Ethosomes were spherical in structure as confirmed by SEM, and zeta potential was in range of −12.4 mV to −27.4 mV. %EE of the vesicles was in the range of 49.61%‐78.047%. Cumulative percentage drug release from various ethosomal formulations was ranged from 64.82%‐81.01%. F3 was selected as optimized formulation on the basis of highest %EE, zeta potential, and in vitro drug release. An ethosomal gel of optimized formulation F3 was prepared by using carbopol 934 and compared with plain gel formulation. G3 formulation showed pseudoplastic rheological behavior, optimum pH, spreadability and also showed maximum % in vitro drug permeation with flux 13.85 μg/cm2/hr and followed zero‐order release kinetics which was good for topical drug delivery system. Conclusion: This research suggested that MLT loaded ethosomes can be potentially used as a topically drug delivery system. [ABSTRACT FROM AUTHOR] |
