Optimization of preparation method for ketoprofen-loaded microspheres consisting polymeric blends using simplex
Sanjoy Kumar Das1, Jasmina Khanam1, Arunabha Nanda1
1Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
Materials Science & Engineering. C, Materials for Biological Applications
|September 11, 2016
Summary
This study optimized ketoprofen microspheres using ethylcellulose and Eudragit®RL 100 for controlled release. The developed formulation achieved high drug entrapment and prolonged release over 8 hours.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Developing effective controlled-release drug delivery systems is crucial for improving therapeutic outcomes and patient compliance.
- Ketoprofen, a non-steroidal anti-inflammatory drug (NSAID), requires optimized delivery to manage pain and inflammation effectively.
- Microsphere technology offers a promising approach for sustained drug release, minimizing dosing frequency.
Purpose of the Study:
- To formulate and optimize ketoprofen microspheres using ethylcellulose and Eudragit®RL 100 for controlled drug release.
- To investigate the impact of polymer concentration, stirring speed, and emulsifier concentration on microsphere characteristics.
- To evaluate the in vitro drug release profile and characterize the optimized formulation.
Main Methods:
- Simplex lattice mixture design was employed for formulation development and optimization.
- Oil-in-oil emulsion solvent evaporation method was used for microsphere preparation.
- Analysis of Variance (ANOVA), Fourier Transform Infrared (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC), and Scanning Electron Microscopy (SEM) were utilized for characterization.
Main Results:
- The optimized formulation (KTF-O) demonstrated a high desirability factor (0.811) with good agreement between predicted and actual responses.
- SEM confirmed discrete microspheres with an average particle size of 149.2±1.25μm.
- The optimized batch exhibited high drug entrapment efficiency (~90%) and prolonged drug release (~91.25% over 8 hours).
Conclusions:
- The simplex lattice design effectively optimized ketoprofen microspheres for controlled release.
- The developed microspheres, utilizing ethylcellulose and Eudragit®RL 100, show potential as a favorable controlled-release dosage form.
- Drug release kinetics followed Korsmeyer-Peppas and Higuchi models, indicating diffusion-controlled release mechanisms.
