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

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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.

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Data Availability

Data can be available on request.

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Acknowledgements

The authors wish to express their gratitude to the Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET) and the Universidad Nacional del Litoral (UNL) of Argentina for the financial support provided for this contribution. We would also like to express our gratitude to the late Dr. Ignacio Helbling for his invaluable contributions to this research.

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Authors and Affiliations

  1. Laboratorio de Química Fina, Instituto de Desarrollo Tecnológico Para La Industria Química (INTEC), Universidad Nacional del Litoral and Consejo Nacional de Investigaciones Científicas y Técnicas (UNL-CONICET), CCT CONICET-SANTA FE, Ruta Nacional 168, Paraje El Pozo, 3000, Santa Fe, Argentina

    Federico A. Fookes, Natalia S. Velázquez & Julio A. Luna

  2. Laboratorio de Biología Ósea, Facultad de Ciencias Médicas, Universidad Nacional de Rosario, 3100, Rosario, Santa Fe, Argentina

    Alfredo Rigalli

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  1. Federico A. Fookes
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Contributions

Material preparation, data collection and analysis, and writing, original draft preparation, were performed by Federico A. Fookes. Review, editing, and analysis were performed by Natalia S. Velázquez. Supervision, review, and editing were performed by Alfredo Rigalli. Supervision, review, and editing were performed by Julio A. Luna.

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Correspondence to Federico A. Fookes.

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Fookes, F.A., Velázquez, N.S., Rigalli, A. et al. Development of Fluoride-Loaded Chitosan Microparticles for Controlled Drug Delivery: A Comparative Study of PVP K17 and Eudragit® RS 30D as Coating Polymer. J Pharm Innov 18, 1941–1953 (2023). https://doi.org/10.1007/s12247-023-09765-y

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