Optimizing indomethacin-loaded chitosan nanoparticle size, encapsulation, and release using Box-Behnken experimental
Mohd Abul Kalam1, Abdul Arif Khan1, Shahanavaj Khan1
1Nanomedicine Research Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Indomethacin chitosan nanoparticles were optimized for size and drug release. The study identified optimal concentrations and stirring time for effective nanoparticle formulation.
Area of Science:
- Materials Science
- Nanotechnology
- Pharmaceutical Sciences
Background:
- Indomethacin is a nonsteroidal anti-inflammatory drug (NSAID) commonly used for pain and inflammation.
- Chitosan nanoparticles (NPs) offer potential for improved drug delivery due to their biocompatibility and biodegradability.
- Developing optimized nanoparticle formulations is crucial for enhancing drug efficacy and patient outcomes.
Purpose of the Study:
- To develop and optimize indomethacin-loaded chitosan nanoparticles (NPs) using ionotropic gelation.
- To determine the optimal concentrations of chitosan and tripolyphosphate (TPP), and stirring time for NP formulation.
- To evaluate the impact of formulation parameters on particle size, encapsulation efficiency, and drug release.
Main Methods:
- Utilized a 3-factor, 3-level Box-Behnken experimental design for optimization.
- Investigated the effects of chitosan concentration (A), TPP concentration (B), and stirring time (C) on nanoparticle properties.
- Analyzed in vitro drug release kinetics using various kinetic models, identifying Higuchi-matrix as the best fit.
Main Results:
- Optimal formulation achieved with 0.6 mg/mL chitosan, 0.4 mg/mL TPP, and 120 min stirring time.
- Resulting nanoparticles exhibited sizes between 321-675 nm with positive zeta potentials (+25 to +32 mV) after 6 months.
- Encapsulation efficiency ranged from 56-79%, drug release from 48-73%, and drug content from 98-99%.
Conclusions:
- The Box-Behnken design effectively optimized indomethacin chitosan nanoparticles for desired characteristics.
- Formulation parameters significantly influenced particle size, encapsulation efficiency, and drug release profiles.
- The developed nanoparticles demonstrate potential for controlled indomethacin delivery, following Higuchi-matrix release kinetics.
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