Nanosuspension-based microneedle skin patch of baclofen for sustained management of multiple sclerosis-related spasticity

Abstract

Baclofen (BAC) is the first-line recommendation to treat spasticity in people with multiple sclerosis whose treatment goals include improving mobility or easing pain. The short half-life of BAC calls for multiple daily dosing which may be eliminated by the development of a transdermal system. This study aimed to assess the effect of transdermal microneedle patches on improving the skin permeation of BAC. Nanosuspension-loaded microneedle patch containing BAC was fabricated and characterized. In vitro permeation of BAC across intact and microneedle-treated dermatomed porcine ear skin was evaluated. In vitro passive permeation of BAC solution after 72 h was observed to be 92.56 ± 11.24 µg/cm2. A near 9-fold enhancement was observed when employing the strategy of microneedle-mediated delivery of the solution. To increase drug loading, two strategies, nanosizing and microneedle-mediated delivery, were combined and permeation of BAC after 72 h resulted to be 1951.95 ± 82.01 µg/cm2 (p < 0.05). Microneedle-mediated transdermal delivery of BAC holds potential for sustained management of multiple sclerosis-related spasticity. Nanosizing of BAC particles facilitated higher drug loading in MN patches and an eventual increase in cumulative drug permeation from the patches.