Abstract

BackgroundGastroretentive drug delivery system (GDDS) are novel systems that have been recently developed for treating stomach diseases. The key function of all GDDS systems is to control the retention time in the stomach. However, research into the bulk density or entanglement of polymers, especially regarding their effects on drug float and release times, is scarce.MethodsIn this research, we prepared the floating core-shell beads carrying tetracycline. The ratio of chitosan and xanthan gum in the shell layer was changed to modify polymer compactness. Tetracycline was encapsulated in the alginate core.ResultsUsing scanning electron microscopy (SEM) techniques, we observed that the shell formulation did not change the bead morphology. The cross-sectional images showed that the beads were highly porous. The interaction between anionic xanthan gum and cationic chitosan made the shell layer dense, resisting to the mass transfer in the shell layer. Due to the high mass transfer resistance to water penetration, the longer float and delivery time were caused by the dense surface of the beads. The cell culture demonstrated that floating core-shell beads were biocompatible. Importantly, the beads with tetracycline showed a significant prolonged anti-bacterial effect.ConclusionResearch results proved that the floating and releasing progress of core-shell beads can be well controlled by adjusting the shell layer formulation that could promote the function of gastroretentive drugs.

Highlights

  • Oral administration is the most common drug delivery method as it is multifunctional and convenient [1]

  • Dulbecco’s modified eagle medium (DMEM), fetal bovine serum (FBS), penicillin, trypsin was purchased from Gibco Life Technologies (Thermo Fisher Scientific - TW)

  • We assume that interactions between chitosan and xanthan gum increase the density of the two components

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Summary

Introduction

Oral administration is the most common drug delivery method as it is multifunctional and convenient [1]. GDDS could keep drugs in stomach for a prolonged period to achieve a specific release, including several types: floating, mucoadhesive, expandable and rafting forming drug delivery systems. In FDDS, the drugs carriers float in gastric juice to ensure that drugs do not leave stomach shortly. It efficiently increases drug bioavailability by prolonging the release period. Better stability and prolonged residence time allow more effective antibiotic penetration through the gastric mucus layer to suppress or eradicate Helicobacter Pylori in stomach [5, 6], which would be achieved by FDDS. Gastroretentive drug delivery system (GDDS) are novel systems that have been recently developed for treating stomach diseases. Research into the bulk density or entanglement of polymers, especially regarding their effects on drug float and release times, is scarce

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