Optimization of drug release from compressed multi unit particle system (MUPS) using generalized regression neural...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Diclofenac sodium is a widely used non-steroidal anti-inflammatory drug (NSAID).
• Achieving controlled and extended drug release is crucial for improving therapeutic efficacy and patient compliance.
• Conventional dosage forms may lead to suboptimal drug release profiles and potential side effects.

Purpose of the Study:

• To develop and optimize extended-release diclofenac sodium compressed matrix pellets using Carbopol 71G.
• To investigate the influence of polymer percentage and tablet crushing strength on drug release kinetics.
• To utilize Generalized Regression Neural Network (GRNN) for modeling and optimizing the in vitro drug release profile.

Main Methods:

• Formulation of ten diclofenac sodium matrix tablets using Central Composite Design (CCD).
• Utilized Carbopol 71G as the primary matrix-forming polymer for extended release.
• Employed direct pelletisation and compression into MUPS (Multiple Unit Pellet System) tablets.
• Investigated the effects of polymer percentage (X1) and tablet crushing strength (X2) on drug release.
• Analyzed in vitro dissolution profiles at five different time points.
• Applied GRNN to model the relationship between formulation factors and drug release.

Main Results:

• Drug release rates varied significantly across different formulations, ranging from 1 to 8 hours.
• The percentage of Carbopol 71G (X1) was identified as the most critical factor influencing drug release.
• GRNN successfully modeled the in vitro release profile of diclofenac sodium from the compressed matrix pellets.
• Optimized formulations aimed to achieve specific in vitro release targets: 15-40% at 1h, 25-60% at 2h, 35-75% at 4h, and >70% at 8h.

Conclusions:

• Extended-release diclofenac sodium matrix pellets can be effectively developed using Carbopol 71G.
• Formulation parameters, particularly polymer concentration, significantly impact drug release characteristics.
• GRNN is a valuable tool for optimizing drug release profiles in extended-release formulations.
• The developed MUPS tablets offer a promising approach for controlled diclofenac sodium delivery with optimized release kinetics.