Department of Pharmaceutical Sciences, Bill Gatton College of Pharmacy, East Tennessee State University, Johnson City, TN 37614, United States.
Department of Pharmaceutical Sciences, Bill Gatton College of Pharmacy, East Tennessee State University, Johnson City, TN 37614, United States.
Int J Pharm. 2023 Sep 25;644:123352. doi: 10.1016/j.ijpharm.2023.123352. Epub 2023 Aug 28.
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/cm. 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/cm (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.
巴氯芬（BAC）是多发性硬化症患者痉挛治疗的一线推荐药物，其治疗目标包括改善移动能力或缓解疼痛。BAC 的半衰期短，需要每日多次给药，而经皮系统的开发可能会消除这种需求。本研究旨在评估透皮微针贴片对改善 BAC 皮肤渗透的作用。制备并表征了载有 BAC 的纳米混悬剂负载的微针贴片。评估了 BAC 经完整和微针处理的去皮猪耳皮肤的体外渗透。观察到 BAC 溶液在 72 小时后的体外被动渗透为 92.56±11.24µg/cm。当采用微针介导的溶液传递策略时，观察到近 9 倍的增强。为了增加药物载量，采用纳米化和微针介导的传递两种策略，渗透后 72 小时 BAC 的渗透量为 1951.95±82.01µg/cm（p<0.05）。BAC 的微针介导经皮传递有可能持续管理多发性硬化症相关痉挛。BAC 颗粒的纳米化促进了 MN 贴片中的更高药物载量，并最终增加了贴片的累积药物渗透量。
