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Doxycycline-Loaded pH-Sensitive Microparticles as a Potential Site-Specific Drug Delivery System against
Ardiyah Nurul Fitri Marzaman1, Ulfah Mahfufah1, Nurul Fauziah1
1Faculty of Pharmacy, Hasanuddin University, Makassar 90245, Indonesia.
ACS Omega
|February 24, 2025
Summary
This study developed pH-sensitive microparticles of doxycycline to improve biofilm penetration for periodontitis treatment. The novel hydrogel formulation effectively delivered the drug to infection sites, showing significant antibacterial activity against key bacteria.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Periodontal Therapeutics
Background:
- Periodontitis treatment is challenged by bacterial biofilms in periodontal pockets.
- Current therapies suffer from poor antibacterial agent penetration and nonspecific targeting.
- Novel drug delivery systems are needed to enhance biofilm penetration and targeted delivery.
Purpose of the Study:
- To develop pH-sensitive microparticles (MPs) of doxycycline (DOX) for enhanced biofilm penetration.
- To create an in situ hydrogel formulation for targeted delivery of DOX-MPs to periodontal infection sites.
- To evaluate the antimicrobial efficacy and mucoadhesive properties of the developed system.
Main Methods:
- DOX-loaded MPs were fabricated using a double-emulsion technique with PLGA and chitosan.
- MP characterization included morphology, particle size, PDI, encapsulation, and drug loading efficiency.
- Drug release kinetics were studied under varying pH conditions.
- An in situ hydrogel formulation was prepared using Pluronic F127/F68 and HPMC.
- Antimicrobial activity was assessed against Escherichia coli and Staphylococcus aureus in vitro and ex vivo.
Main Results:
- DOX-MPs exhibited spherical morphology (3.54 ± 0.32 μm) with good encapsulation (69.43%) and drug loading (14.81%).
- Accelerated drug release was observed under low-pH conditions, indicating pH-sensitivity.
- The hydrogel formulation demonstrated liquid-to-gel transition at body temperature and good mucoadhesion.
- Ex vivo studies showed significant reduction in microbial count, biofilm quantity, and metabolic activity.
- Antibacterial efficacy of DOX-MPs was comparable to free DOX.
Conclusions:
- pH-sensitive DOX-MPs formulated into an in situ hydrogel offer a promising strategy for periodontitis treatment.
- The system enhances targeted drug delivery and biofilm penetration.
- The formulation exhibits effective antimicrobial activity and mucoadhesive properties.
- This novel approach addresses limitations of conventional therapies for periodontitis.
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