Abstract
BackgroundCarvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally. Ethosomes-mediated transdermal delivery is considered a potential route of administration to increase the bioavailability of carvedilol. The central composite design could be used as a tool to optimize ethosomal formulation. 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.ResultsThe optimized carvedilol-loaded ethosomes were spherical in shape. 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 in-vitro drug release showed sustained release of carvedilol from ethosomes and ethosomal hydrogel. Compared to free carvedilol-loaded hydrogel, the ethosomal gel showed increased penetration of carvedilol through the skin. Moreover, ethosomal hydrogels showed a gradual reduction in blood pressure for 24 h in rats.ConclusionsTaken 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 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.
Highlights
Carvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally
Solubility profile of carvedilol The permeation and efficacy of carvedilol delivered through the transdermal route are highly dependent on the extent of its solubility in ethosomal suspension
Optimization of carvedilol‐loaded ethosome (CLE) formulation using central composite design (CCD) A rotatable CCD was used around a fixed point for preparing carvedilol-loaded ethosomes (CLE) suspensions [26]
Summary
Carvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally. Ethosomesmediated transdermal delivery is considered a potential route of administration to increase the bioavailability of carvedilol. This study aims to optimize carvedilol-loaded ethosomes using central composite design, followed by incorporation of synthe‐ sized ethosomes into hydrogels for transdermal delivery of carvedilol. The transdermally-administered drugs can evade enzymatic degradation and offers a non-invasive route for drug administration, providing better. Carvedilol is well accepted in clinics, it undergoes first-pass metabolism and has low oral bioavailability (about 25% to 35%) [5]. The low oral bioavailability of carvedilol is possibly because of its low dissolution capability (ranked in the class II category of Amarachinta et al J Nanobiotechnol (2021) 19:100 biopharmaceutical classification system), and its profound pre-systemic metabolism [6, 7]. Carvedilol is ideal for transdermal delivery because of its high lipophilicity and low molecular weight (406.5 g/ml) [8]
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