Gastroretentive delivery systems: hollow beads

Area of Science:

• Pharmaceutical Technology
• Materials Science

Background:

• Developing floatable multiparticulate systems is key for intragastric sustained drug delivery.
• Calcium-pectinate and calcium-pectinate-alginate beads were explored for drug encapsulation and release.

Purpose of the Study:

• To develop a floatable multiparticulate system for sustained intragastric drug delivery.
• To evaluate the impact of drying methods and cross-linking on bead characteristics and drug release.

Main Methods:

• Beads were fabricated using calcium and low methoxylated pectin (LMP), with and without sodium alginate.
• Air-dried and freeze-dried beads were tested for buoyancy and drug release using Riboflavin, tetracycline (TCN), and Methotrexate (MTX).
• Confocal laser microscopy analyzed bead structure, and TCN entrapment was studied at different pH levels.

Main Results:

• Freeze-dried beads exhibited buoyancy for over 12 hours due to internal air-filled spaces, unlike air-dried beads.
• Calcium-pectinate-alginate beads showed faster drug release (100% in 10 hours) compared to calcium-pectinate beads (50% in 10 hours).
• Drug entrapment efficiency for TCN was highest when cross-linking media pH matched the drug's least soluble pH.

Conclusions:

• Freeze-drying is essential for achieving floatable beads for gastroretentive drug delivery.
• Bead composition, cross-linking, drying method, and drug properties significantly influence drug release kinetics.
• This study demonstrates the potential for developing effective gastroretentive drug delivery systems using these bead formulations.