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Purpose <p>Azithromycin has proven effective in treating several periodontal diseases. The drug requires three daily doses associated with common side effects of antibiotics. A local sustained azithromycin delivery system would be ideal. This study aims to formulate and evaluate azithromycin sustained-release microparticles.</p> Methods <p>PLGA was used as the carrier polymer, where different formulations were prepared using the emulsion solvent evaporation method, allowing adjustment of formulation parameters to ensure better drug delivery system performance. Formulation parameters tested included drug: polymer ratio following the optimization of the internal: external volume ratio, PVA, and PLGA concentration.</p> Results <p>Eight different microparticles formulations were successfully prepared. Particle size ranged from 32 to 57 microns with 44–97% drug loading depending on the specific formulation parameters. Variation in formulation parameters impacted particles size and drug content. Particles are spherical as evident by SEM and exhibited the biphasic release characteristics of PLGA particles. The optimum formula exhibited diffusion-controlled release with 38.14%± 5.71 initial release and 95% ±0.99 total AZI release.</p> Conclusions <p>Higher polymer concentration in the internal phase enhanced drug loading and encapsulation efficacy. The biphasic extended-release formulation is expected to improve treatment outcomes in periodontal diseases by maintaining an effective antibiotic level. Formulated particles retained their drug content and release profile after 8 months of storage. While antibacterial-loaded microspheres for subgingival administration, such as minocycline and doxycycline, are well studied for periodontal therapy, azithromycin has not been thoroughly investigated for this route. Azithromycin offers advantages over other antibiotics due to its improved biofilm and tissue penetration, as well as its anti-inflammatory properties. In this study, the formulation was tailored to prolong the release of azithromycin in subgingival tissue, sustain the therapeutic level for an extended duration, reduce dosing frequency, and enhance patient acceptance.</p>

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Preparation and Evaluation of Azithromycin Microspheres for Subgingival Administration in Periodontal Diseases Management

  • 期刊论文

  • 发表日期：

    2025年11月3日

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  • Zahraa Hasan Falhi Al-Saedi,
  • Kawther Khalid Ahmed,
  • Zainab Thabit Salih

摘要

Purpose

Azithromycin has proven effective in treating several periodontal diseases. The drug requires three daily doses associated with common side effects of antibiotics. A local sustained azithromycin delivery system would be ideal. This study aims to formulate and evaluate azithromycin sustained-release microparticles.

Methods

PLGA was used as the carrier polymer, where different formulations were prepared using the emulsion solvent evaporation method, allowing adjustment of formulation parameters to ensure better drug delivery system performance. Formulation parameters tested included drug: polymer ratio following the optimization of the internal: external volume ratio, PVA, and PLGA concentration.

Results

Eight different microparticles formulations were successfully prepared. Particle size ranged from 32 to 57 microns with 44–97% drug loading depending on the specific formulation parameters. Variation in formulation parameters impacted particles size and drug content. Particles are spherical as evident by SEM and exhibited the biphasic release characteristics of PLGA particles. The optimum formula exhibited diffusion-controlled release with 38.14%± 5.71 initial release and 95% ±0.99 total AZI release.

Conclusions

Higher polymer concentration in the internal phase enhanced drug loading and encapsulation efficacy. The biphasic extended-release formulation is expected to improve treatment outcomes in periodontal diseases by maintaining an effective antibiotic level. Formulated particles retained their drug content and release profile after 8 months of storage. While antibacterial-loaded microspheres for subgingival administration, such as minocycline and doxycycline, are well studied for periodontal therapy, azithromycin has not been thoroughly investigated for this route. Azithromycin offers advantages over other antibiotics due to its improved biofilm and tissue penetration, as well as its anti-inflammatory properties. In this study, the formulation was tailored to prolong the release of azithromycin in subgingival tissue, sustain the therapeutic level for an extended duration, reduce dosing frequency, and enhance patient acceptance.