Enhanced Floating and Intragastric Release of 5-Flourouracil through Sesame Oil Entrapped Gellan Composite Hydrogel Beads

Abstract

Background: 5-Fluorouracil is an anti-metabolite compound used for several years as an anti-tumor drug. The development of a gastroretentive drug delivery system of 5-Fluorouracil may have advantages since they retain in the stomach for an extended time and release the drug in a sustained manner, which ultimately enhances the absorption of the drug and consequently the bioavailability. Objective: The objective of the present work was to prepare a sesame oil-entrapped gellan gum hydrogel bead for controlled stomach specific delivery of 5-Fluorouracil. Methods: Sesame oil-entrapped gellan gum hydrogel bead was prepared by ionotropic gelation method. The developed hydrogels were characterized by SEM, FTIR, DSC, and XRD. The entrapment efficiency, floating ability, swelling and drug release in vitro were also determined. Results: Electrostatic interaction between the carboxylic group of polymers and Ca++ was confirmed by FTIR analysis. The SEM photograph of the hydrogel beads portrayed an approximately spherical shaped structure. DSC thermogram and XRD spectra exhibited the molecular dispersion of the drug inside the hydrogel beads. The developed beads of 5-Fluorouracil floated in pH 1.2 buffer solutions for a prolonged time period and the duration of floating was improved significantly with increasing the concentration of oil. The developed formulations showed controlled release of drug and incorporation of oil retarded the release of the drug. Fickian and non-Fickian mechanism of drug transport was observed from the prepared hydrogel beads. Conclusion: Overall, the oil-entrapped gellan matrices could be used for the intragastric delivery of 5-Fluorouracil to treat stomach cancer.