ENHANCED TRANSDERMAL PERMEABILITY OF TELMISARTAN BY A NOVEL NANOEMULSION GEL
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 4
Abstract
Objective: Telmisartan is an angiotensin II type I receptor blocker antihypertensive agent with 42% oral bioavailability. The aim of the present investigation was to develop a nanoemulsion gel to enhance bioavailability of poorly water soluble Telmisartan.Methods: Different nanoemulsion components (oil, surfactant and co-surfactant) were selected on the basis of solubility and emulsification ability. Pseudotemary phase diagrams were constructed using aqueous titration method. Carbopol 934 was added as a gel matrix to convert nanoemulsion into nanoemulsion gel. Drug loaded nanoemulsions and nanoemulsion gels were characterized for particle size, viscosity, rheological behavior, thermodynamic stability studies and ex vivo permeation studies using rat skin. Transdermal permeation of Telmisartan from nanoemulsion gels was determined using Franz Diffusion cell.Results: The optimized nanoemulsion gel (NEG) contained Labrafil®M 2125 CS (14.3%) as oil, Acrysol®EL 135 (30.84%) as surfactant, Carbitol® (15.42%) as co-surfactant and (32.44%) water; 20 mg drug and 1% w/w carbopol. The ex vivo permeation profile of optimized formulation was compared to nanoemulsion and normal gel. Permeability parameters like steady-state flux (Jss), permeability coefficient (Kp), and enhancement ratio (Er) were significantly increased in nanoemulsion (NE) and nanoemulsion gel (NEG) as compared to conventional gel. There was a considerable improvement in bio availability for nanoemulsion gel compared to the conventional telemisartan gel.Conclusion: Nanoemulsion gel has significantly increased the bio-availability of the drug.Â
Authors and Affiliations
C. Aparna, Prathima Srinivas, K. S. K. Rao Patnaik
Keywords
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