Smart Pellets for Controlled Delivery of 5-Fluorouracil

This work aimed to develop a new one-pot and readily scaled-up formulation capable of retaining 5-fluorouracil and prolonging its release to obtain a site-specific medication delivery for the potential treatment of colorectal cancer. Six polymer-based formulations were successfully produced using a thermal bulk polymerization method and loaded with 5-fluorouracil, which is a chemotherapeutic agent used in the treatment of colorectal carcinoma. The pellets produced were characterized by measuring the glass transition temperature, tensile strength, Young's modulus, and tensile elongation at break. Studies on in vitro swelling and release were carried out in phosphate-buffered saline to evaluate the behaviour of the developed system. The Young's modulus, glass transition temperature, and tensile strength all increased significantly as the crosslinker concentration increased, but the fracture strain value reduced significantly. The in vitro swelling profile of the produced formulations was significantly reduced by increasing crosslinking density. Less than 27% cumulative drug release was achieved for all formulations after 5 h of starting the release study. The highest cumulative drug release reached after 24 h was 69%. The developed drug delivery system demonstrated the ability to delay the release of 5-fluorouracil in upper gastrointestinal tract-mimicking conditions, while permitting its release in a controlled way afterward, which makes it promising for the potential delivery of 5-fluorouracil to the colon.

Automated summary

This study aimed to develop a new formulation that can both retain and control the release of 5-fluorouracil for targeted medication delivery to treat colorectal cancer. Six polymer-based formulations loaded with 5-fluorouracil were successfully produced using a thermal bulk polymerization method. The formulation's properties, such as glass transition temperature, tensile strength, and swelling behavior, were evaluated. The developed drug delivery system showed promising results by delaying the release of 5-fluorouracil in the upper gastrointestinal tract and controlling its release afterward for potential delivery to the colon.