Oral delivery of micro/nanoparticulate systems based on natural polysaccharides for intestinal diseases therapy: Challenges, advances and future perspectives

• Published in: Journal of controlled release 2021-06, Vol.334, p.353-366
• Main Authors: dos Santos, Aline Martins, Carvalho, Suzana Gonçalves, Meneguin, Andréia Bagliotti, Sábio, Rafael Miguel, Gremião, Maria Palmira Daflon, Chorilli, Marlus
• Format: Article
• Language: English
• Subjects: Colon-targeted drug delivery; Colorectal cancer; Crohn's disease; Inflammatory bowel disease; Micro/nanoparticulate systems; Oral administration; Polysaccharides; Ulcerative colitis
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/j.jconrel.2021.04.026

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. [Display omitted] •Oral colon-targeted systems remains as a promising tool to treat intestinal diseases.•Micro- and nanoparticles systems can offer protection from harsh environments of GIT.•Natural polysaccharides properties add key advantages to achieve colon site.•Judicious design become crucial for the next-generation of oral colon-targeted systems.