García-Couce Jomarien, Schomann Timo, Chung Chih Kit, Que Ivo, Jorquera-Cordero Carla, Fuentes Gastón, Almirall Amisel, Chan Alan, Cruz Luis J
Biomaterials Center, University of Havana, Avenida Universidad Entre G y Ronda, Vedado, Plaza, La Habana 10400, Cuba.
Translational Nanobiomaterials and Imaging Group, Department of Radiology, Leiden University Medical Center, 2333 ZA Leiden, The Netherlands.
Gels. 2022 Aug 5;8(8):488. doi: 10.3390/gels8080488.
The intra-articular administration of drugs has attracted great interest in recent decades for the treatment of osteoarthritis. The use of modified drugs has also attracted interest in recent years because their intra-articular administration has demonstrated encouraging results. The objective of this work was to prepare injectable-thermosensitive hydrogels for the intra-articular administration of Etanercept (ETA), an inhibitor of tumor necrosis factor-α. Hydrogels were prepared from the physical mixture of chitosan and Pluronic F127 with β-glycerolphosphate (BGP). Adding β-glycerolphosphate to the system reduced the gelation time and also modified the morphology of the resulting material. In vitro studies were carried out to determine the cytocompatibility of the prepared hydrogels for the human chondrocyte line C28/I2. The in vitro release study showed that the incorporation of BGP into the system markedly modified the release of ETA. In the in vivo studies, it was verified that the hydrogels remained inside the implantation site in the joint until the end of the study. Furthermore, ETA was highly concentrated in the blood of the study mice 48 h after the loaded material was injected. Histological investigation of osteoarthritic knees showed that the material promotes cartilage recovery in osteoarthritic mice. The results demonstrate the potential of ETA-loaded injectable hydrogels for the localized treatment of joints.
近几十年来,药物关节内给药在骨关节炎治疗方面引起了极大关注。近年来,改性药物的应用也备受关注,因为其关节内给药已显示出令人鼓舞的效果。本研究的目的是制备用于肿瘤坏死因子-α抑制剂依那西普(ETA)关节内给药的可注射热敏水凝胶。水凝胶由壳聚糖、泊洛沙姆F127与β-甘油磷酸酯(BGP)的物理混合物制备而成。向体系中添加β-甘油磷酸酯可缩短凝胶化时间,并改变所得材料的形态。进行体外研究以确定所制备水凝胶对人软骨细胞系C28/I2的细胞相容性。体外释放研究表明,将BGP加入体系中显著改变了ETA的释放。在体内研究中,证实水凝胶在研究结束前一直保留在关节内的植入部位。此外,在注射负载材料48小时后,研究小鼠血液中ETA高度浓缩。对骨关节炎膝关节的组织学研究表明,该材料可促进骨关节炎小鼠的软骨恢复。结果证明了负载ETA的可注射水凝胶在关节局部治疗中的潜力。