ISBN-13: 9783659138447 / Angielski / Miękka / 2012 / 80 str.
Carvedilol has oral bioavailability 25% to 30% due to high first pass metabolism (80%) and presence of food decreases its absorption rate in gastrointestinal tract. Short half life of Carvedilol (4 to 6 hr) indicates need of controlled release delivery. To overcome these limitations carvedilol was incorporated in proniosome for transdermal delivery. Proniosome drug delivery was preferred due to improved stability of the system than niosomes. To optimize the formulation, various proniosome gels composed of various ratios of sorbitan fatty acid esters, polysorbates, cholesterol, lecithin were prepared by coacervation-phase separation method. Optimized formulation gave flux 3.416 g/cm2/hr up to 12 hrs. with highest permeation (65%) of carvedilol among all formulations. Penetration enhancers, non-ionic surfactants and vesicle-skin interaction may contributed to the enhanced carvedilol permeation. Thus Proniosome was found to be a promising carrier system for Carvedilol because of ease in preparation and stability for prolonged period."
Carvedilol has oral bioavailability 25% to 30% due to high first pass metabolism (80%) and presence of food decreases its absorption rate in gastrointestinal tract. Short half life of Carvedilol (4 to 6 hr) indicates need of controlled release delivery. To overcome these limitations carvedilol was incorporated in proniosome for transdermal delivery. Proniosome drug delivery was preferred due to improved stability of the system than niosomes. To optimize the formulation, various proniosome gels composed of various ratios of sorbitan fatty acid esters, polysorbates, cholesterol, lecithin were prepared by coacervation-phase separation method. Optimized formulation gave flux 3.416μg/cm2/hr up to 12 hrs. with highest permeation (65%) of carvedilol among all formulations. Penetration enhancers, non-ionic surfactants and vesicle-skin interaction may contributed to the enhanced carvedilol permeation. Thus Proniosome was found to be a promising carrier system for Carvedilol because of ease in preparation and stability for prolonged period.