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Development of Metronidazole Loaded Chitosan Nanoparticles Using QbD Approach-A Novel and Potential Antibacterial
Nagaraja Sreeharsha1,2, Kuldeep Rajpoot3, Muktika Tekade4
1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
Pharmaceutics
|September 30, 2020
Summary
This study developed metronidazole (Met) nanoparticles (MetNp) using quality-by-design principles for targeted colon delivery. The optimized MetNp capsules show potential for treating amoebiasis by releasing Met specifically in the colon.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Drug Delivery Systems
Background:
- Metronidazole is a key drug for treating amoebiasis.
- Targeted drug delivery to the colon can enhance efficacy and reduce systemic side effects.
- Nanoparticle formulations offer potential for improved drug bioavailability and controlled release.
Purpose of the Study:
- To design, optimize, and develop metronidazole-loaded nanoparticles (MetNp) using a quality-by-design (QbD) approach.
- To create an enteric-coated MetNp capsule for targeted colon delivery of metronidazole.
- To evaluate the physicochemical properties, drug release, and stability of the developed MetNp.
Main Methods:
- Quality-by-design (QbD) methodology with fractional factorial design was employed.
- Independent variables included chitosan concentration, tripolyphosphate concentration, stirring speed, and stirring time.
- Metronidazole nanoparticles (MetNp) were synthesized using an ionic-gelation technique and formulated into enteric-coated capsules.
Main Results:
- Optimized MetNp exhibited a particle size of 558.06 ± 2.52 nm and %entrapment efficiency of 59.07 ± 2.15%.
- The enteric-coated MetNp capsules demonstrated pH-triggered, sustained release of metronidazole at pH > 7.0.
- Formulations showed good stability regarding particle size and residual drug content under various temperature conditions.
Conclusions:
- The QbD approach was effective in developing stable metronidazole-loaded nanoparticles (MetNp).
- Enteric-coated MetNp capsules facilitate targeted metronidazole release in the colon.
- These MetNp capsules show promise for the effective treatment of colonic amoebiasis.

