Development and in vitro characterization of 5-flurouracilloaded, colon-targeted drug delivery system

Purpose: To prepare chondroitin sulphate–polyvinyl alcohol cross-linked microcapsules (miCAPs) for controlled delivery of 5-flurouracil (5-FU) in cancer patients.Method: Nine different miCAP formulations were prepared using emulsion cross-linking procedure. The formulations were evaluated for their physicochemical properties, complex formation, stability at variable temperatures, safety, as well as drug-loading and drug-release characteristics. The effects of glutaraldehyde (GA), polymer concentration and stirring speed on 5-FU release at various pH were also assessed.Results: One of the miCAP formulations (miCAP-1) was adjudged the most suitable based on its particle size, high drug loading (75.3 %, p = 0.034), and high entrapment efficiency (85.2 %, p = 0.031). Best-fit drug release model was Higuchi model based on regression coefficient value (R2) while drug release mechanism was Fickian.Conclusion: Highly stable, crosslinked, amorphous and drug delivery system has been successfully developed. The delivery system is potentially suitable for acid-sensitive therapeutic moieties and where controlled release is desired.Keywords: Emulsion cross-linking, Colon-specific delivery, 5-Flurouracil, Glutaraldehyde, Kinetic models