Department of Pharmaceutics, Dr. D.Y. Patil College of Pharmacy, Akurdi, Pune, 411044 Maharashtra, India.
Curr Drug Deliv. 2021;18(1):71-87. doi: 10.2174/1567201817666200804111614.
Periodontitis is an oral disease categorized by disturbance of periodontal tissue and the creation of periodontal pockets. Thymol (TH) loaded microsponge gelling systems was formulated for local action in the periodontal cavity for the management of periodontitis.
Solvent evaporation technique was utilized for the preparation of microsponges. A Fractional Factorial Design (FFD) was used to screen the high risk variables impacting the characteristics of the (TH) microsponges and further optimized using Box-Behnken design. The optimized microsponges were then characterized by DSC, SEM, antimicrobial activity, release, and then incorporated in the gelling system. A ligature model was used to induce periodontitis in Sprague Dawley rats.
The microsponges showed good characteristics, such as particle size, entrapment efficiency, and mucoadhesiveness of 45 μm, 92.99 ± 0.2%, 96 ± 0.26%, respectively. SEM revealed the spherical morphology of the microsponges with sustained release of TH for 10h and antimicrobial activity against and . Treatment with Thymol Loaded Gel (THLMG) showed a decrease in gingival inflammation and tooth mobility as well as in serum biochemical parameters like serum Creactive proteins, leucocyte count, alkaline phosphatase, and tartrate-resistant acid phosphatase, when compared to disease group. The histopathological study of the periodontium confirmed a significant reduction of inflammation and alveolar bone destruction (<0.05) in rats.
THLMG decreased the infiltration of inflammatory cells and prevented osteoclastogenesis and osteoblast apoptosis, which further favored a decrease in inflammation and alveolar bone loss in periodontitis. Thus, THLMG could be a better alternative to synthetic antimicrobials and antibiotics to treat periodontitis.
牙周炎是一种口腔疾病，其特征是牙周组织紊乱和牙周袋形成。载硫醇（TH）微海绵凝胶系统旨在通过局部作用于牙周腔来管理牙周炎。
采用溶剂蒸发技术制备微海绵。采用部分因子设计（FFD）筛选影响（TH）微海绵特性的高风险变量，并进一步采用 Box-Behnken 设计进行优化。然后对优化后的微海绵进行 DSC、SEM、抗菌活性、释放等特性进行表征，再将其掺入凝胶系统中。结扎模型用于诱导 Sprague Dawley 大鼠牙周炎。
微海绵具有良好的特性，如粒径、包封效率和粘膜粘附性分别为 45μm、92.99±0.2%和 96±0.26%。SEM 显示微海绵呈球形形态，TH 持续释放 10h，对 和 具有抗菌活性。与疾病组相比，载硫醇凝胶（THLMG）治疗可降低牙龈炎症和牙齿松动以及血清生化参数如血清 C 反应蛋白、白细胞计数、碱性磷酸酶和抗酒石酸酸性磷酸酶。牙周组织的组织病理学研究证实，载硫醇凝胶可显著减少大鼠炎症和牙槽骨破坏（<0.05）。
THLMG 减少了炎症细胞的浸润，防止了破骨细胞生成和成骨细胞凋亡，从而进一步有利于减少牙周炎的炎症和牙槽骨丧失。因此，THLMG 可能是治疗牙周炎的替代合成抗菌剂和抗生素的更好选择。
