Advanced polymeric systems for colon drug delivery: from experimental models to market applications

• Published in: Soft matter Vol. 21; no. 5; pp. 792 - 818
• Main Authors: Crispino, R, Lagreca, E, Procopio, A, D'Auria, R, Corrado, B, La Manna, S, Onesto, V, Di Natale, C
• Format: Journal Article
• Language: English
• Published: England Royal Society of Chemistry 29.01.2025
• Subjects: Administration, Oral; Animals; Bioavailability; Biocompatibility; Biodegradation; Cell Line, Tumor; Colitis, Ulcerative - drug therapy; Colon; Colon - drug effects; Colon cancer; Colonic Neoplasms - drug therapy; Colorectal carcinoma; Controlled release; Crohn's disease; Drug Carriers - chemistry; Drug delivery; Drug delivery systems; Drug Delivery Systems - instrumentation; Drug Delivery Systems - methods; Drug Industry; Drug Screening Assays, Antitumor; Gastrointestinal system; Gastrointestinal tract; Humans; Hydrogen-Ion Concentration; In vitro methods and tests; In vivo methods and tests; Inflammatory bowel diseases; Inflammatory Bowel Diseases - drug therapy; Intestine; Mathematical models; Mice; Microfluidics; Microparticles; Oral administration; Polymers; Polymers - chemistry; Sustained release; Time dependence; Toxicity; Transit time; Ulcerative colitis
• ISSN: 1744-683X; 1744-6848; 1744-6848
• DOI: 10.1039/d4sm01222d

In recent years, nano and micro drug delivery systems targeting the colon have gained more attention due to increasing interest in treating colon diseases such as colorectal cancer and inflammatory bowel disease, i.e. , Crohn's disease and ulcerative colitis. Usually, nanocarriers are exploited for their enhanced permeability properties, allowing higher penetration effects and bioavailability, while microcarriers are primarily used for localized and sustained release. In bowel diseases, carriers must go into a delicate environment with a strict balance of gut bacteria ( e.g. , colon), and natural or biodegradable polymers capable of ensuring lower toxicity are preferred. However, these systems are primarily delivered orally, so the carrier must go through the whole gastrointestinal tract, where it encounters significant pH fluctuations, different mucus layers, several enzymes, and a long transit time. For this reason, various approaches have been explored and evaluated, especially using pH-responsive and time-dependent systems. This review provides an overview of the contemporary methodologies employed in orally administered nano- and microparticles for colon delivery, encompassing both in vivo and in vitro investigations. It evaluates their strengths, weaknesses, constraints, and potential enhancements, leveraging mathematical and microfluidic models. Furthermore, it focuses explicitly on systems that have already reached the market and are presently employed in treating severe colon diseases. A diagram illustrating various nano- and micro-particle systems for colon treatment, emphasizing their biocompatibility, controlled drug release, anti-inflammatory action, and high target specificity. Created using https://BioRender.com .