Microneedle-assisted transdermal delivery of carvedilol nanosuspension for the treatment of hypertension

Abstract

Carvedilol nanosuspension loaded microneedles patch was formulated and characterized by particle size,  zeta potential, solubility, Transmission Electron Microscopy, X-Ray Diffraction, in-vitro release and in-vivo pharmacokinetic studies A nanosuspension-loaded microneedle patch was successfully prepared and characterized by optical microscopy, scanning electron microscopy, axial fracture force, in vitro dissolution study, % drug content, in vitro drug-release study, ex vivo studies, an in vivo study, and stability studies. The particle size, PDI, and zeta potential of the carvedilol nanosuspension were found to be 179.6 ± 1.15 nm, 0.163 ± 0.01, and −14.2 ± 0.55 mV, respectively. There was a 9.21-fold increase in the saturation solubility of the carvedilol nanosuspension. Nanosuspension-loaded microneedles contained 98.78 ± 0.12% carvedilol. The relative bioavailability of the carvedilol from the microneedle patch was found to be 2.82-fold higher compared to the marketed formulation. The drug release from the microneedles followed zero-order kinetics, which is desirable in the case of transdermal delivery. The stability study indicated that the prepared formulation was stable under the storage conditions used. Thus, the developed transdermal microneedle patch containing the carvedilol nanosuspension seems to be a promising approach to foster greater patient compliance for the management of hypertension.