Development and Characterization of Eudragit-RL-100-Based Aceclofenac Sustained-Release Matrix Pellets Prepared via...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nonsteroidal Anti-inflammatory Drugs (NSAIDs)

Background:

• Aceclofenac (AC) is an NSAID for chronic pain, requiring frequent dosing.
• Frequent AC administration can lead to gastric side effects.
• Sustained-release formulations offer a potential solution to improve AC therapy.

Purpose of the Study:

• To formulate sustained-release matrix pellets of Aceclofenac (AC).
• To investigate the effects of Eudragit RL 100 and PVP K90 concentrations on pellet properties.
• To optimize pellet formulation for controlled drug release and reduced gastric irritation.

Main Methods:

• Extrusion/spheronization technique used for pellet formulation.
• Response surface methodology employed to study formulation variables.
• Analysis of wet mass peak torque, pellet size, and in vitro drug release profiles.

Main Results:

• PVP K90 showed synergistic effects on peak torque and pellet size; Eudragit RL 100 had antagonistic effects.
• Formulations maintained <10% drug release in acidic medium (pH 1.2), suggesting reduced gastric irritation.
• Optimized formula (3.21% Eudragit, 5% PVP) exhibited enhanced peak torque, larger pellet size, and significant 8-hour drug release retardation.

Conclusions:

• Extrusion/spheronization is effective for formulating AC sustained-release matrix pellets.
• Formulation parameters significantly influence pellet physical characteristics and drug release kinetics.
• Optimized pellets offer a promising approach for improved Aceclofenac delivery with potentially fewer gastrointestinal side effects.