Enhanced permeability of Cyclosporine from a transdermally applied nanoemulgel

The objective of this study was to investigate the potential of nanoemulgel for transdermal delivery of Cyclosporine. Different nanoemulsion components (oil, surfactant, and cosurfactant) were selected on the basis of solubility and emulsification ability. Pseudoternary phase diagrams were constructed using titration method to figure out the concentration range of components. Guar gum was added as gel matrix to convert nanoemulsion into nanoemulgel. Drug loaded nanoemulsions and nanoemulgels were characterized for particle size, transmission electron microscopy, viscosity, pH, rheology, spreadability, drug content, in vitro skin permeation using rat abdominal skin and stability studies. Nanoemulgel containing 20% oleic acid as oil, 65% Tween 80, and Transcutol P as surfactant cosurfactant mixture, 15% water, 2% drug, and 0.5% Guar gum was concluded as optimized formulation (BF5). The drug content o f t he optimized formulation was found to be 99.5 %. The flux value through rat skin was found to be 0.078 mg/cm2 /h. The ex vivo permeation profile of optimized formulation was compared with nanoemulsion and marketed formulation. Nanoemulgel showed significantly higher (P < 0.05) cumulative amount of drug permeated and flux along with lower lag time and skin retention than marketed formulation. Thus, the study substantiated that nanoemulgel formulation can be used as a feasible alternative to conventional formulations of cyclosporine with advanced permeation characteristics for transdermal application.

Author(s): Mahesh Begur, Vasanth Kumar Pai, D. V. Gowda, AtulSrivastava, H. V.Raghundan, Chetan G. Shindeand Manusri N.

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