Centre of Biological Engineering, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal; CBMA - Centre of Molecular and Environmental Biology, Department of Biology, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal.
CBMA - Centre of Molecular and Environmental Biology, Department of Biology, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal; IB-S - Institute of Science and Innovation for Sustainability, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal.
Eur J Pharm Biopharm. 2021 Oct;167:89-103. doi: 10.1016/j.ejpb.2021.07.014. Epub 2021 Jul 28.
Inflammatory bowel disease incidence has been constantly rising for the past few decades. Current therapies attempt to mitigate its symptoms since no cure is established. The most commonly prescribed drug for these patients is 5-aminosalicylic acid (5-ASA). Due to the low rate and seriousness of side effects compared to other therapies, 5-ASA is still largely prescribed in many stages of inflammatory bowel disease, including scenarios where evidence suggests low effectiveness. Although commercialized formulations have come a long way in improving pharmacokinetics, it is still necessary to design and develop novel delivery systems capable of increasing effectiveness at different stages of the disease. In particular, micro- and nano-sized particles might be the key to its success in Crohn's disease and in more serious disease stages. This review provides an overview on the clinical significance of 5-ASA formulations, its limitations, challenges, and the most recent micro- and nanoparticle delivery systems being designed for its controlled release. Emergent alternatives for 5-ASA are also discussed, as well as the future prospects for its application in inflammatory bowel disease therapies.
过去几十年来，炎症性肠病的发病率一直在不断上升。目前的治疗方法试图减轻其症状，因为尚未确定治愈方法。这些患者最常开的药物是 5-氨基水杨酸（5-ASA）。由于与其他疗法相比，其副作用发生率和严重程度较低，因此在炎症性肠病的许多阶段仍广泛开 5-ASA，包括在有证据表明疗效较低的情况下。尽管商业化制剂在改善药代动力学方面已经取得了很大进展，但仍需要设计和开发新型给药系统，以在疾病的不同阶段提高疗效。特别是，微纳米颗粒可能是其在克罗恩病和更严重疾病阶段取得成功的关键。本综述概述了 5-ASA 制剂的临床意义、其局限性、挑战以及为其控释而设计的最新微纳米给药系统。还讨论了 5-ASA 的新兴替代品，以及其在炎症性肠病治疗中的应用的未来前景。
