Purpose

The study was aimed to formulate eugenol-loaded polymeric microsponges using eugenyl methacrylate (Eg-MA) incorporated in situ gelling system for the treatment of periodontitis.

Method

Eg-MA monomer was first synthesized by reacting eugenol with methacryloyl chloride, which acted as a monomer and cross-linking agent for preparing microsponges of Eg-MA using suspension polymerization method. The formation of Eg-MA monomer was confirmed by FTIR. A 3² Box–Behnken design was applied to optimize Eg-MA polymeric microsponges which were characterized by SEM and antimicrobial activity. An optimized batch of polymeric microsponges was incorporated into in situ gelling system which was evaluated on the basis of pH, viscosity, gelling temperature, and mucoadhesion on the goat buccal mucosa. Ligature-induced experimental periodontitis (EPD) was induced in rats to assess the efficacy of the formulation.

Results

SEM revealed the spherical shape of Eg-MA microsponges with antibacterial activity against Streptococcus mutans and potential to load eugenol with a drug content of 96.38 ± 0.09%. The study of the eugenol-loaded microsponges in situ gel showed sustained release of the drug up to 24 h with a mucoadhesive strength of 31 ± 0.13 N. Treatment with eugenol-loaded Eg-MA polymeric microsponges decreased tooth mobility and gingival inflammation in rats. The histological studies of the periodontium also confirmed decrease in the infiltration of inflammatory cells and alveolar bone destruction (p < 0.05) in EPD rats.

Conclusion

Thus, a novel formulation using Eg-MA with intrinsic antibacterial property was used to formulate eugenol-loaded polymeric microsponges in situ gel for the management of periodontitis.

中文翻译：

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装有丁香酚原位凝胶的甲基丙烯酸丁烯酯微海绵用于治疗牙周炎

目的

这项研究的目的是使用结合在原位胶凝系统中的甲基丙烯酸丁烯二酯（Eg-MA）来配制负载丁香酚的聚合物微海绵，以治疗牙周炎。

方法

首先使丁子香酚与甲基丙烯酰氯反应合成Eg-MA单体，甲基丙烯酰氯用作单体和交联剂，采用悬浮聚合法制备Eg-MA的微海绵。通过FTIR证实了Eg-MA单体的形成。应用3 ² Box–Behnken设计来优化Eg-MA聚合物微海绵，该微海绵具有SEM和抗菌活性。将优化的一批聚合物微海绵掺入原位胶凝体系中，该体系根据pH，粘度，胶凝温度和在山羊颊粘膜上的粘膜粘附性进行评估。在大鼠中诱发结扎诱导的实验性牙周炎（EPD）以评估该制剂的功效。

结果

扫描电镜显示，Eg-MA微海绵呈球形，具有对变形链球菌的抗菌活性，并具有负载丁香酚的潜力，药物含量为96.38±0.09％。丁香酚负载的微海绵原位凝胶的研究表明，该药物可持续释放长达24小时，粘膜粘附强度为31±0.13N。丁香酚负载的Eg-MA聚合物微海绵治疗可降低大鼠的牙齿活动性和牙龈炎症。牙周组织学研究还证实 ，EPD大鼠的炎性细胞浸润减少和牙槽骨破坏（p <0.05）。

结论

因此，使用具有固有抗菌特性的使用Eg-MA的新型配方，可以配制出丁香酚负载的聚合物微海绵原位凝胶，以治疗牙周炎。