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Design and optimization of diclofenac sodium controlled release solid dispersions by response surface methodology
H N Shivakumar1, B G Desai, G Deshmukh
1Department of Pharmaceutical Technology, K. L. E. S's College of Pharmacy, Rajajinagar 2 Block, Bangalore - 560 010, India.
Indian Journal of Pharmaceutical Sciences
|April 15, 2010
Summary
This study optimized controlled-release diclofenac sodium solid dispersions using Eudragit polymers. Formulation variables significantly impacted drug release, leading to a predictable and effective drug delivery system.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Polymer Science
Background:
- Controlled drug release systems are crucial for improving therapeutic efficacy and patient compliance.
- Diclofenac sodium is a widely used non-steroidal anti-inflammatory drug (NSAID) requiring optimized delivery for sustained action.
- Eudragit RS and RL polymers offer tunable properties for developing advanced drug formulations.
Purpose of the Study:
- To develop and optimize controlled-release solid dispersions of diclofenac sodium using Eudragit RS and RL polymers.
- To investigate the influence of formulation variables on drug incorporation and release kinetics.
- To establish mathematical models for predicting drug release and optimize the formulation for enhanced performance.
Main Methods:
- A 3(2) factorial design was utilized for formulation development.
- Coevaporation technique in a flash evaporator was employed to create solid dispersions.
- Response surface methodology, multiple linear regression, and analysis of variance were used for data analysis.
- Fourier transform infrared spectroscopy, Differential scanning calorimetry, and Powder X-ray diffractometry were used for characterization.
Main Results:
- Both total polymer load and Eudragit RL levels significantly affected drug release profiles (p < 0.05).
- Total polymer load was the primary factor influencing percent drug incorporation.
- Optimized formulation achieved high drug incorporation (95.22%) and predictable drug release profiles.
- Characterization confirmed diclofenac sodium existed in molecular or microcrystalline form within the polymer matrix.
Conclusions:
- Controlled-release solid dispersions of diclofenac sodium can be effectively produced using Eudragit RS/RL and coevaporation.
- Mathematical models accurately predict drug release, enabling formulation optimization.
- The developed solid dispersions exhibit first-order release kinetics, following Higuchian diffusion, suitable for sustained drug delivery.
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