Polymer-amino-functionalized silica composites for the sustained-release multiparticulate system

Area of Science:

• Materials Science
• Pharmaceutical Technology
• Drug Delivery Systems

Background:

• Diclofenac sodium (DS) is a widely used nonsteroidal anti-inflammatory drug.
• Developing effective oral sustained-release formulations is crucial for improving patient compliance and therapeutic efficacy.
• Controlling drug release profiles requires advanced formulation strategies, particularly for enteric-coated systems.

Purpose of the Study:

• To develop and characterize a novel oral multiparticulate formulation for sustained-release diclofenac sodium (DS).
• To investigate the potential of functionalized hybrid silica gel as an enteric coating for controlling DS release.
• To evaluate the drug release properties of the developed formulation in a neutral environment.

Main Methods:

• Fabrication of hybrid silica gel by vapor phase gelation of tetraethoxysilane (TEOS) and (3-aminopropyl)triethoxysilane (APTES) in ammonia.
• Encapsulation of diclofenac sodium within the functionalized silica gel to form beads.
• Characterization of subunits using low-temperature N2 sorption, DSC, XRD, SEM, and 29Si MAS NMR.
• Assessment of drug release in a neutral environment.

Main Results:

• Successful synthesis of hybrid silica gel functionalized with 3-aminopropyl groups.
• Demonstrated ability of the functionalized silica gel to facilitate prolonged release of DS in a neutral environment.
• Characterization confirmed the properties of the silica gel subunits influencing drug release.

Conclusions:

• The developed multiparticulate formulation using functionalized silica gel shows promise for sustained-release diclofenac sodium.
• The hybrid silica gel acts as an effective enteric coating, enabling controlled drug release in the intestine.
• Further studies are warranted to optimize the formulation for clinical application.