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Evaluation of cross-linked chitosan microparticles containing metronidazole for periodontitis treatment
Wiwat Pichayakorn1, Prapaporn Boonme
1Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
Abstract:
The aims of this study were to find the optimal formulation for the preparation of metronidazole-loaded chitosan microparticles (MTZ-MPs) via an emulsion cross-linking process, and to compare the in vitro release of MTZ from hydrogels and films containing the drug in forms of MTZ-MPs and raw powders. The effects of emulsifier type and concentration, amount of cross-linking agent, cross-linking time, drug:chitosan ratio, form of drug adding and washing method on the properties of the MTZ-MPs were investigated. The results indicated that the optimal conditions for round and free-flowing MTZ-MPs with a high percentage of entrapped drug and preferable release profile were 1% of Span80 in soybean oil, 5% of glutaraldehyde based on chitosan solution, 30 min of cross-linking time, 1:1 drug:chitosan ratio, drug adding in form of ethanol solution and washing with hexane only. MTZ-MPs prepared from the optimal formulation were incorporated in mucoadhesive hydrogel and film. The release profiles of the drug from hydrogel and film containing MTZ-MPs were in prolong pattern compared with those containing drug powders. However, the hydrogels exhibited higher preferable pattern of release profile than the films. Therefore, the hydrogel containing MTZ-MPs was possible to be further clinically investigated for peridontitis treatment.
Insights
Researchers optimized metronidazole-loaded chitosan microparticles (MTZ-MPs) for improved drug delivery. These MTZ-MPs, when formulated into hydrogels, demonstrated a prolonged and preferable release profile for potential periodontitis treatment.
Area of Science:
- Pharmaceutical Sciences
- Biomaterials Science
- Drug Delivery Systems
Background:
- Chitosan microparticles offer a promising platform for controlled drug release.
- Metronidazole is a key antibiotic used in treating periodontal diseases.
- Optimizing microparticle formulation is crucial for effective drug delivery.
Purpose of the Study:
- To determine the optimal formulation for metronidazole-loaded chitosan microparticles (MTZ-MPs) using emulsion cross-linking.
- To compare the in vitro drug release of MTZ from hydrogels and films containing MTZ-MPs versus raw powders.
- To evaluate the potential of MTZ-MPs in hydrogel formulations for periodontitis treatment.
Main Methods:
- Emulsion cross-linking technique was employed to prepare MTZ-MPs.
- Various formulation parameters were investigated, including emulsifier, cross-linker, time, drug:chitosan ratio, and washing method.
- In vitro drug release studies were conducted using hydrogels and films containing MTZ-MPs and raw metronidazole powder.
Main Results:
- Optimal MTZ-MPs were achieved with 1% Span80, 5% glutaraldehyde, 30 min cross-linking, 1:1 drug:chitosan ratio, ethanol solution addition, and hexane washing.
- Hydrogels and films containing MTZ-MPs exhibited prolonged drug release compared to raw drug powders.
- Hydrogel formulations showed a more favorable release profile than film formulations.
Conclusions:
- The optimized formulation yields high-quality metronidazole-loaded chitosan microparticles with desirable release characteristics.
- Hydrogel formulations incorporating MTZ-MPs demonstrate superior sustained release, indicating potential for periodontitis treatment.
- Further clinical investigation of metronidazole-loaded chitosan microparticle hydrogels is warranted for periodontal therapy.
