Enhanced osteoarthritis treatment using an injectable pH-responsive and cartilage-targeted liposome-anchored kartogenin-incorporated methacrylated gelatin hydrogel microspheres.

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Tác giả: Zhangsheng Dai, Honghui Fan, Wei He, Xujun Hu, Chao Jiang, Yu Jin, Xin Li, Xuanyuan Lu, Fei Pang, Yihang Shen, Jing Wang, Lei Wang, Yefeng Wang, Huilong Zeng, Ping Zhou

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: Netherlands : International journal of biological macromolecules , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 746142

Osteoarthritis (OA) is a chronic joint disease characterized by cartilage degeneration. In this study, we developed hydrogel microspheres for cartilage repair in OA. We designed and synthesized a novel nanomaterial using liposomes (Lipo), which exhibits cartilage-targeting ability and pH responsiveness. These liposomes were surface-functionalized with cartilage-targeting peptides (WYRGRL), encapsulated with the cationic lipid 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), incorporated with a pH-responsive hydrazone (HyD) bond, and loaded with the bioactive molecule kartogenin (KGN). These novel liposomes were embedded within methacrylated gelatin (GM) hydrogel microspheres to create the WYRGRL-DOTAP-Lipo@KGN@GM (WDLKG) hydrogel microspheres. Characterization tests revealed that the novel liposomes WYRGRL-DOTAP-Lipo@KGN (WDLK) exhibited cartilage-targeting ability and pH responsiveness and the WDLKG hydrogel microspheres showed excellent dispersibility and uniform size. Further in vitro cell-experiments demonstrated that WDLKG hydrogel microspheres effectively promoted chondrogenesis, and exhibited anti-inflammatory effects via enhancing the anabolism while reducing the catabolism in chondrocytes. Transcriptomic analysis revealed that WDLKG induced chondrogenesis primarily through collagen trimer formation and collagen-containing extracellular matrix biosynthesis. In vivo experiments in a mouse OA model confirmed the sustained release of WDLKG and demonstrated that intra-articular injection of WDLKG significantly inhibited cartilage degeneration. These findings underscore the potential of our nanomaterials for targeted therapy, advancing OA cartilage treatment.
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