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An attempt was made to develop and evaluate the membrane-controlled transdermal systems for the controlled release of nicorandil. The carbopol gel was selected as a drug reservoir, crosslinked blend membranes of XG and SA were selected as rate-controlled membranes (RCM), and a film of poly(vinyl alcohol) (PVA) was selected as the backing membrane. The aim of the current work was to formulate the membrane-controlled transdermal drug delivery systems for the effective delivery of a vasodilator, nicorandil, for the management of hypertension and angina pectoris, and in-vitro and ex-vivo evaluation of these developed formulations.
Reservoir gel was evaluated for drug content, pH, viscosity, and RCMs by weight uniformity, thickness uniformity, differential scanning calorimetric (DSC) analysis, x-ray diffraction (XRD) analysis, scanning electron microscopy (SEM), water vapor transmission, skin irritation, and histopathology.
Depending on crosslink density, variation in the water vapor permeation of RCMs was noticed. The RCMs showed no signs of skin irritation. In-vitro drug permeation through rat skin was extended for a period of 24 hours. With an increase in acetaldehyde concentration in the RCM, there was a decrease in drug permeation. Among the two terpenes used as penetration enhancers, the cineole at a concentration of 20% exhibited a maximum permeation rate. The release mechanism from all systems followed non-Fickian transport. Histopathology results indicated minor changes in skin structure after skin permeation studies, which were reversible.
The developed transdermal systems were found to be versatile dosage forms for the controlled release of nicorandil, a vasodilator.