São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, SP 14800-903, Brazil.
São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, SP 14800-903, Brazil.
J Control Release. 2021 Jun 10;334:353-366. doi: 10.1016/j.jconrel.2021.04.026. Epub 2021 Apr 24.
Colon-targeted oral delivery of drugs remains as an appealing and promising approach for the treatment of prevalent intestinal diseases (ID), such as inflammatory bowel disease (IBD) and colorectal cancer (CRC). Notwithstanding, there are numerous challenges to effective drug delivery to the colon, which requires the design of advanced strategies. Micro- and nanoparticles have received great attention as colon-targeted delivery platforms due to their reduced size and structural composition that favors the accumulation and/or residence time of drugs at the site of action and/or absorption, contributing to localized therapy. The choice by natural polysaccharides imparts key properties and advantages to the nano-in-microparticulate systems to effective colon-specific oral delivery. This review proposes to discuss the physiological barriers imposed by the gastrointestinal tract (GIT) against oral administration of drugs, as well as pathological factors and challenges of the ID for oral delivery of colon-targeted systems. We then provide an updated progress about polysaccharides-based colon-targeted drug delivery systems, including microparticulate, nanoparticulate and nano-in-microparticulate systems, highlighting their key properties, advantages and limitations to achieving targeted delivery and efficacious therapy within the colon. Lastly, we provide future perspectives, towards advances in the field and clinical translation of colon-targeted oral delivery systems for ID therapy.
肠道靶向口服递药系统用于治疗常见的肠道疾病(ID),如炎症性肠病(IBD)和结直肠癌(CRC),具有很大的吸引力和应用前景。然而,将药物有效递送到结肠存在诸多挑战,这需要设计先进的策略。由于其尺寸较小且结构组成有利于药物在作用部位和/或吸收部位的积累和/或驻留时间,因此微纳米粒作为肠道靶向递药平台受到了极大的关注,有助于实现局部治疗。天然多糖的选择赋予纳米-微颗粒系统以关键特性和优势,以实现有效的结肠特异性口服递药。本综述拟讨论胃肠道(GIT)对药物口服给药的生理屏障,以及 ID 对口服递药的病理因素和挑战。然后,我们提供了基于多糖的结肠靶向药物递药系统的最新进展,包括微颗粒、纳米颗粒和纳米-微颗粒系统,突出了它们在实现靶向递药和在结肠内进行有效治疗方面的关键特性、优势和局限性。最后,我们对 ID 治疗的结肠靶向口服递药系统的领域进展和临床转化提出了未来展望。