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Preparation of pH-sensitive beads for NSAID using three-component gel systems
Zsófia Fenyvesi1, Alíz Auner, Dirk Schmalz
1Department of Pharmaceutics, Semmelweis University, Hogyes E. Str. 7., H-1092 Budapest, Hungary. zsfenyvesi@gmail.com
Journal of Pharmaceutical Sciences
|March 14, 2009
Summary
Novel pH-sensitive beads were developed using sodium alginate, hydroxyethylcellulose, and hydroxypropylmethylcellulose for gastric protection. This formulation effectively reduced the ulcerogenic effects of diclofenac sodium in vivo.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery Systems
Background:
- Non-steroidal anti-inflammatory drugs (NSAIDs) like diclofenac sodium can cause gastric irritation and ulceration.
- Developing protective formulations is crucial for safe and effective NSAID delivery.
- pH-sensitive drug delivery systems offer targeted release and reduced side effects.
Purpose of the Study:
- To prepare novel pH-sensitive beads for gastric mucosa protection.
- To ensure targeted drug delivery of diclofenac sodium into the intestine.
- To investigate the influence of formulation parameters on bead characteristics and drug release.
Main Methods:
- Bead preparation via ionotropic gelation using sodium alginate (Na-Alg), hydroxyethylcellulose (HEC), and hydroxypropylmethylcellulose (HPMC).
- Swelling, erosion, and drug release studies using gravimetric methods and artificial digestive fluids.
- Evaluation of drug release kinetics using Korsmeyer-Peppas and Baker-Lonsdale models.
- Differential scanning calorimetry (DSC) for encapsulation behavior and in vivo studies in rats for ulcerogenicity and absorption.
Main Results:
- Hydroxypropylmethylcellulose (HPMC) enhanced encapsulation efficiency (EE), while hydroxyethylcellulose (HEC) improved intestinal drug release.
- Equilibrium water uptake (EWU) correlated with exposure time, calcium chloride concentration, and HEC content.
- Bead erosion increased with exposure time but decreased with higher calcium chloride concentrations.
- Higher HEC amounts increased encapsulation efficacy, whereas higher pH values reduced it.
Conclusions:
- The developed pH-sensitive beads provide gastric protection by reducing the ulcerogenic effect of diclofenac sodium.
- The ionotropic gelation method with Na-Alg, HEC, and HPMC is effective for creating drug delivery systems with tunable properties.
- The formulation demonstrates potential for targeted intestinal delivery of diclofenac sodium, improving its safety profile.
