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Purpose <p>Probiotics and their byproducts appear to offer specific advantages in managing dental caries. However, the contact time of the sample at the target area plays a key role in enhancing product efficacy.</p> Method <p>In this context, a series of mucoadhesive microparticles containing <i>L. rhamnosus</i>, glycyrrhizin, and vitamin-D3 were prepared with pectin and calcium chloride using the ionotropic gelation process. The microparticles were examined for compatibility and thermal stability, which revealed them to be thermally stable and compatible.</p> Results <p>The synthesized microparticles exhibited a porous surface with high surface-to volume-ratio as confirmed by SEM. The encapsulation efficiencies of glycyrrhizin and <i>L. rhamnosus</i> were 88.74 ± 1.5% and 85.24 ± 2.1%, respectively, while a cumulative drug release of 77.51% for glycyrrhizin and 13.30% for vitamin-D was also observed for 6&#xa0;h. The formulation demonstrated significant in vitro antimicrobial activity against <i>S. aureus</i> (MIC 187.5&#xa0;µg/ml, zone of inhibition 25.83 ± 0.62&#xa0;mm, biofilm inhibition at MIC/2 72.08%) and <i>S. mutans</i> (MIC 375&#xa0;µg/ml, zone of inhibition 21.86 ± 0.12&#xa0;mm, biofilm inhibition at MIC/2 70.68%) vs. a standard antibiotic doxycycline. Furthermore, the microparticles significantly reduced the pro-inflammatory cytokine IL-6, IL-1β and TNF-α levels and increased the anti-inflammatory cytokine IL-10 level in both in vitro and in vivo rat models, alongside exhibiting 82.71% antioxidant activity. X-ray imaging confirmed a 6-hour retention of the formulation in the rat oral cavity, demonstrating promising sustained delivery and therapeutic potential.</p> Conclusion <p>The notable antimicrobial and anti-inflammatory effects observed are likely due to the combined action of <i>L. rhamnosus</i> metabolites and glycyrrhizin. Traditional dental therapies often encounter challenges such as rapid salivary clearance, limited drug penetration and antibiotic-induced microbiome imbalances. Conversely, the developed microparticles can facilitate the prolonged, site-specific delivery effectively by mitigating these drawbacks improving patient adherence, and representing a substantial improvement in dental caries management.</p> Graphical Abstract <p></p>

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Preparation and Characterisation of Lactobacillus rhamnosus, Glycyrrhizin and Vitamin-D3 Loaded Mucoadhesive Pectin Microparticles for Dental Caries Management

  • 期刊论文

  • 发表日期：

    2025年10月20日

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  • Sumita Mishra,
  • Sudhanshu Ranjan Rout,
  • Ritu Mahanty,
  • Jitu Halder,
  • Vineet Kumar Rai,
  • Priyanka Dash,
  • Chandan Das,
  • Salim Manoharadas,
  • Muralidhar Tata,
  • Biswakanth Kar,
  • Goutam Ghosh,
  • Neeta Mohanty,
  • Goutam Rath

摘要

Purpose

Probiotics and their byproducts appear to offer specific advantages in managing dental caries. However, the contact time of the sample at the target area plays a key role in enhancing product efficacy.

Method

In this context, a series of mucoadhesive microparticles containing L. rhamnosus, glycyrrhizin, and vitamin-D3 were prepared with pectin and calcium chloride using the ionotropic gelation process. The microparticles were examined for compatibility and thermal stability, which revealed them to be thermally stable and compatible.

Results

The synthesized microparticles exhibited a porous surface with high surface-to volume-ratio as confirmed by SEM. The encapsulation efficiencies of glycyrrhizin and L. rhamnosus were 88.74 ± 1.5% and 85.24 ± 2.1%, respectively, while a cumulative drug release of 77.51% for glycyrrhizin and 13.30% for vitamin-D was also observed for 6 h. The formulation demonstrated significant in vitro antimicrobial activity against S. aureus (MIC 187.5 µg/ml, zone of inhibition 25.83 ± 0.62 mm, biofilm inhibition at MIC/2 72.08%) and S. mutans (MIC 375 µg/ml, zone of inhibition 21.86 ± 0.12 mm, biofilm inhibition at MIC/2 70.68%) vs. a standard antibiotic doxycycline. Furthermore, the microparticles significantly reduced the pro-inflammatory cytokine IL-6, IL-1β and TNF-α levels and increased the anti-inflammatory cytokine IL-10 level in both in vitro and in vivo rat models, alongside exhibiting 82.71% antioxidant activity. X-ray imaging confirmed a 6-hour retention of the formulation in the rat oral cavity, demonstrating promising sustained delivery and therapeutic potential.

Conclusion

The notable antimicrobial and anti-inflammatory effects observed are likely due to the combined action of L. rhamnosus metabolites and glycyrrhizin. Traditional dental therapies often encounter challenges such as rapid salivary clearance, limited drug penetration and antibiotic-induced microbiome imbalances. Conversely, the developed microparticles can facilitate the prolonged, site-specific delivery effectively by mitigating these drawbacks improving patient adherence, and representing a substantial improvement in dental caries management.

Graphical Abstract