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Diclofenac sodium releasing pH-sensitive monolithic devices
Hasan Basan1, Menemşe Gümüşderelíoğlu, Tevfik Orbey
1Faculty of Pharmacy, Department of Analytical Chemistry, Gazi University, 06330, Ankara, Turkey
International Journal of Pharmaceutics
|September 25, 2002
Summary
This study developed pH-sensitive polymeric discs for controlled diclofenac sodium release. The novel drug delivery system demonstrated pH-dependent drug release, with minimal release in simulated gastric fluid and near-complete release in simulated intestinal fluid.
Area of Science:
- Polymer Science
- Materials Science
- Pharmaceutical Sciences
Background:
- Non-steroidal anti-inflammatory drugs (NSAIDs) like diclofenac sodium (DFNa) are widely used.
- Developing effective drug delivery systems for NSAIDs is crucial for targeted and controlled release.
- pH-sensitive polymers offer potential for site-specific drug delivery in the gastrointestinal tract.
Purpose of the Study:
- To synthesize and characterize pH-sensitive monolithic systems for diclofenac sodium (DFNa) incorporation.
- To investigate the in vitro release kinetics of DFNa from these systems under different pH conditions.
- To evaluate the influence of polymer composition and physical parameters on drug release.
Main Methods:
- Copolymerization of 2-hydroxyethyl methacrylate (HEMA) with acrylic acid (AA) and/or dimethylaminoethyl methacrylate (DMAEMA) to form pH-sensitive matrices.
- Incorporation of DFNa into the polymeric matrix before polymerization and crosslinking.
- In vitro release studies conducted in simulated gastric fluid (SGF) followed by simulated intestinal fluid (SIF) at 37°C.
- Analysis of drug release profiles based on varying matrix composition, disc thickness, and drug loading.
Main Results:
- DFNa-loaded polymeric discs were successfully prepared with controlled dimensions.
- AA-containing gels exhibited low swelling and minimal DFNa release (<5%) in SGF (low pH) over 3 hours.
- In SIF (high pH), AA-containing discs showed increased swelling and high DFNa release (approx. 97.5%).
- The presence of DMAEMA in the polymer structure resulted in inverse pH-dependent release behavior.
Conclusions:
- pH-sensitive monolithic systems based on HEMA copolymers can effectively control DFNa release.
- The developed systems demonstrate potential for targeted drug delivery, minimizing gastric irritation and maximizing intestinal absorption.
- Tailoring the comonomer composition (AA vs. DMAEMA) allows for modulation of pH-triggered drug release profiles.