Development of Fluoride-Loaded Chitosan Microparticles for Controlled Drug Delivery: A Comparative Study of PVP K17 and Eudragit® RS 30D as Coating Polymer

Abstract

Purpose: The oral administration of drugs is usually the most convenient, economical, and preferred route for patients. Chitosan is a natural polymer that is biocompatible and possesses good mucoadhesion properties and has been proposed for various biomedical applications such as scaffolds in tissue engineering, wound dressing, and drug release systems. Fluoride is recognized for its ability to stimulate osteoblast differentiation and for its anticariogenic properties. When administered in low doses, it increases bone mass and reduces the risk of vertebral fractures in patients with osteoporosis. However, there is a debate about the potential negative effects of fluoride when applied in high doses or chronically. The objective of this study was to investigate the release of fluoride from chitosan microparticles loaded with fluoride and coated with two polymers, aimed at controlling its delivery. Methods: Fluoride-loaded chitosan microparticles were developed using fluidized bed technology. Additionally, polyvinylpyrrolidone (PVP) and Eudragit® RS were applied to the particles using fluidized bed and dip-coating techniques. The obtained particles were then studied to obtain their release profiles. Infrared spectroscopy studies were conducted to analyze the chemical composition of the particles. Results: The results showed that the coatings had a slight effect on the release of fluoride from the particles when applied using fluidized bed technology. Eudragit RS® 30D coatings by immersion were found to be more effective in sustaining release of fluoride. Conclusion: The study provides useful insights into the use of polymeric coatings in the development of chitosan-based oral delivery systems for the controlled release of a highly soluble API.