High drug loading hydrophobic cross-linked dextran microspheres as novel drug delivery systems for the treatment of osteoarthritis  

作　　者：Zhimin Li Xianjing Feng Shixing Luo Yanfeng Ding Zhi Zhang Yifeng Shang Doudou Lei Jinhong Cai Jinmin Zhao Li Zheng Ming Gao 

机构地区：[1]Guangxi Engineering Center in Biomedical Materials for Tissue and Organ Regeneration,The First Affiliated Hospital of Guangxi Medical University,Nanning 530021,China [2]Collaborative Innovation Centre of Regenerative Medicine and Medical BioResource Development and Application Co-constructed by the Province and Ministry,Guangxi Medical University,Nanning 530021,China [3]Department of Spine and Osteopathic Surgery,The First Affiliated Hospital of Guangxi Medical University,Nanning 530021,China [4]Department of Orthopedics,The Ninth Affiliated Hospital of Guangxi Medical University,Beihai,Guangxi 536000,China [5]Department of Orthopaedics Trauma and Hand Surgery,The First Affiliated Hospital of Guangxi Medical University,Nanning 530021,China [6]Guangxi Key Laboratory of Regenerative Medicine,The First Affiliated Hospital of Guangxi Medical University,Nanning 530021,China

出　　处：《Asian Journal of Pharmaceutical Sciences》2023年第4期109-123,共15页亚洲药物制剂科学（英文）

基　　金：supported by National Natural Science Foundation of China(Grant No.82160430);Natural Science Foundation of Guangxi(Grant No.2020GXNSFAA159134 and 2019GXNSFAA185060);Guangxi Science and Technology Base and Talent Special Project(Grant No.GuikeAD19254003 and GuikeAD21075002);Nanning Qingxiu District Science and Technology Major Special Project(Grant No.2020013).

摘　　要：Drug delivery via intra-articular(IA)injection has proved to be effective in osteoarthritis(OA)therapy,limited by the drug efficiency and short retention time of the drug delivery systems(DDSs).Herein,a series of modified cross-linked dextran(Sephadex,S0)was fabricated by respectively grafting with linear alkyl chains,branched alkyl chains or aromatic chain,and acted as DDSs after ibuprofen(Ibu)loading for OA therapy.This DDSs expressed sustained drug release,excellent anti-inflammatory and chondroprotective effects both in IL-1βinduced chondrocytes and OA joints.Specifically,the introduction of a longer hydrophobic chain,particularly an aromatic chain,distinctly improved the hydrophobicity of S0,increased Ibu loading efficiency,and further led to significantly improving OA therapeutic effects.Therefore,hydrophobic microspheres with greatly improved drug loading ratio and prolonged degradation rates show great potential to act as DDSs for OA therapy.

关 键 词：Sephadex microsphere Hydrophobic modification Drug delivery system High drug loading ratio OSTEOARTHRITIS 

分 类 号：R943[医药卫生—药剂学]