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Transdermal drug delivery is advantageous over other established routes of delivery, because unlike oral route, the transdermal delivery prevents the drug from pre-systemic metabolism which results in better bioavailability.
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Moreover the carvedilol-loaded ethosomal gel can extend the anti-hypertensive effect of carvedilol for a longer time, as compared to free carvedilol, suggesting its therapeutic potential in future clinics. Taken together, central composite design can be used for successful optimization of carvedilol-loaded ethosomes formulation, which can serve as the promising transdermal delivery system for carvedilol. Moreover, ethosomal hydrogels showed a gradual reduction in blood pressure for 24 h in rats. Compared to free carvedilol-loaded hydrogel, the ethosomal gel showed increased penetration of carvedilol through the skin. The in-vitro drug release showed sustained release of carvedilol from ethosomes and ethosomal hydrogel. The optimized ethosomes had mean particle size of 130 ± 1.72 nm, entrapment efficiency of 99.12 ± 2.96%, cumulative drug release of 97.89 ± 3.7%, zeta potential of − 31 ± 1.8 mV, and polydispersity index of 0.230 ± 0.03. The optimized carvedilol-loaded ethosomes were spherical in shape. Thus, this study aims to optimize carvedilol-loaded ethosomes using central composite design, followed by incorporation of synthesized ethosomes into hydrogels for transdermal delivery of carvedilol. The central composite design could be used as a tool to optimize ethosomal formulation.
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Ethosomes-mediated transdermal delivery is considered a potential route of administration to increase the bioavailability of carvedilol. Carvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally.