Yu Zhaohan, Xiong Yan, Fan Menglin, Li Jiyao, Liang Kunneng
State Key Laboratory of Oral Diseases, National Clinical Research Center for Oral Diseases, Department of Cariology and Endodontics, West China Hospital of Stomatology, Sichuan University, Chengdu 610041, China.
Orthopedic Research Institute, Department of Orthopedics, West China Hospital, Sichuan University, Chengdu 610041, China.
ACS Omega. 2023 Jul 5;8(28):25441-25452. doi: 10.1021/acsomega.3c02968. eCollection 2023 Jul 18.
In the clinical pharmacological treatment of acute periodontitis, local periodontal administration is expected to be preferable to systemic administration. However, the action of the active medicine component is hindered and diminished by the limitation of drug solubility, which does not provide timely relief of the enormous pain being suffered by patients. This study aimed to develop a mesoporous magnesium carbonate (MMC) medicine loading system consisting of MMC, metronidazole (MET), and ketoprofen (KET), which was noted as MET-KET@MMC. A solvent evaporation process was utilized to load MET and KET in MMC. Scanning electron microscopy, nitrogen sorption, thermogravimetric analysis, and X-ray diffraction were performed on the MET-KET@MMC. The rapid drug release properties were also investigated through the drug release curve. The rapid antiseptic property against () and the rapid anti-inflammatory property (within 1 min) were analyzed . The cytotoxicity of MET-KET@MMC was tested in direct contact with human gingival cells and human oral keratinocytes. Crystallizations of MET and KET were completely suppressed in MMC. As compared to crystalline MET and KET, MMC induced higher apparent solubility and rapid drug release, resulting in 8.76 times and 3.43 times higher release percentages of the drugs, respectively. Over 70.11% of MET and 85.97% of KET were released from MMC within 1 min, resisting bacteria and reducing inflammation. MET-KET@MMC nanoparticles enhanced the solubility of drugs and possess rapid antimicrobial and anti-inflammatory properties. The MET-KET@MMC is a promising candidate for the pharmacotherapy of acute periodontitis with drugs, highlighting a significant clinical potential of MMC-based immediate drug release systems.
在急性牙周炎的临床药物治疗中，局部牙周给药有望优于全身给药。然而，活性药物成分的作用受到药物溶解度限制的阻碍和削弱，无法及时缓解患者所遭受的剧痛。本研究旨在开发一种由介孔碳酸镁（MMC）、甲硝唑（MET）和酮洛芬（KET）组成的介孔碳酸镁载药系统，记为MET-KET@MMC。采用溶剂蒸发法将MET和KET载入MMC中。对MET-KET@MMC进行了扫描电子显微镜、氮吸附、热重分析和X射线衍射表征。还通过药物释放曲线研究了其快速释药性能。分析了其对（）的快速抗菌性能和（1分钟内）快速抗炎性能。测试了MET-KET@MMC与人牙龈细胞和人口腔角质形成细胞直接接触时的细胞毒性。MET和KET在MMC中的结晶被完全抑制。与结晶MET和KET相比，MMC诱导了更高的表观溶解度和快速药物释放，导致药物释放百分比分别提高了8.76倍和3.43倍。超过70.11%的MET和85.97%的KET在1分钟内从MMC中释放出来，具有抗菌和抗炎作用。MET-KET@MMC纳米颗粒提高了药物的溶解度，并具有快速抗菌和抗炎性能。MET-KET@MMC是急性牙周炎药物治疗的一个有前景的候选者，突出了基于MMC的即时释药系统的巨大临床潜力。
