Carrier rocket-inspired hydrogel microspheres targeting subchondral bone osteoclast activity alleviate osteoarthritic pain and cartilage degeneration

Abstract Background Osteoarthritis (OA) represents a major global health challenge, characterized by progressive cartilage degeneration and subchondral bone remodeling, which culminate in debilitating pain and functional impairment. While recent studies have underscored the pivotal role of activated...

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Main Authors: Zhenglin Zhu, Yujia Luo, Pengcheng Xiao, Yi Xie, Jun Zhang, Ke Huang, Xiangdong Wu, Ke Lu, Yuting Zhang, Jianye Tan, Hong Chen, Wei Huang, Yiting Lei, Junyi Liao
Format: Article
Language:English
Published: BMC 2025-08-01
Series:Journal of Nanobiotechnology
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Online Access:https://doi.org/10.1186/s12951-025-03598-2
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author Zhenglin Zhu
Yujia Luo
Pengcheng Xiao
Yi Xie
Jun Zhang
Ke Huang
Xiangdong Wu
Ke Lu
Yuting Zhang
Jianye Tan
Hong Chen
Wei Huang
Yiting Lei
Junyi Liao
author_facet Zhenglin Zhu
Yujia Luo
Pengcheng Xiao
Yi Xie
Jun Zhang
Ke Huang
Xiangdong Wu
Ke Lu
Yuting Zhang
Jianye Tan
Hong Chen
Wei Huang
Yiting Lei
Junyi Liao
author_sort Zhenglin Zhu
collection DOAJ
description Abstract Background Osteoarthritis (OA) represents a major global health challenge, characterized by progressive cartilage degeneration and subchondral bone remodeling, which culminate in debilitating pain and functional impairment. While recent studies have underscored the pivotal role of activated osteoclasts in the pathogenesis of OA and its associated pain, the therapeutic potential of intra-articular drug delivery has been hindered by challenges such as rapid synovial clearance and the poor permeability of cartilage, limiting the effective inhibition of subchondral osteoclast activity. Methods Sixth generation polyamidoamine (PAMAM) dendrimers were used to delivery pamidronate disodium (PD) penetrating cartilage (PD@PM). PD@PM was loaded in aldehyde modified hyaluronic acid methacrylate (AHAMA) (PD@PM@MG), to facilitating the joint injection and conglutinating on the cartilage. Therapeutic effects of PD@PM@MG were validated by in vitro and in vivo OA models. Results PD@PM@MGs microspheres are uniformly distributed across the cartilage surface and sustained releasing of PD-loaded PAMAM. The positively charged PD-loaded PAMAM (< 10 nm) efficiently permeates the cartilage matrix, neutralizes damage-associated molecular patterns, and effectively inhibits subchondral osteoclasts activities. Mice OA model tests demonstrated that intra-articular injection of PD@PM@MGs markedly alleviated arthritic pain, mitigated cartilage degeneration, and attenuated subchondral bone remodeling. Conclusions The intra-articular injection of PD@PM@MGs significantly alleviates OA symptoms and progression, offering a novel direction for clinical OA intervention. Graphical Abstract
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spelling doaj-art-5ebb18cdaac74cea95eb7943514bc3c62025-08-20T04:02:55ZengBMCJournal of Nanobiotechnology1477-31552025-08-0123111810.1186/s12951-025-03598-2Carrier rocket-inspired hydrogel microspheres targeting subchondral bone osteoclast activity alleviate osteoarthritic pain and cartilage degenerationZhenglin Zhu0Yujia Luo1Pengcheng Xiao2Yi Xie3Jun Zhang4Ke Huang5Xiangdong Wu6Ke Lu7Yuting Zhang8Jianye Tan9Hong Chen10Wei Huang11Yiting Lei12Junyi Liao13Department of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, Beijing Jishuitan Hospital, Capital Medical University, Fourth Clinical College of Peking University, National Center for OrthopaedicsShenzhen Hospital, Southern Medical UniversityResearch Center for Computer-aided Drug Discovery, Shenzhen Institute of Advanced Technology, Chinese Academy of SciencesDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityDepartment of Orthopaedic Surgery, The First Affiliated Hospital of Chongqing Medical UniversityAbstract Background Osteoarthritis (OA) represents a major global health challenge, characterized by progressive cartilage degeneration and subchondral bone remodeling, which culminate in debilitating pain and functional impairment. While recent studies have underscored the pivotal role of activated osteoclasts in the pathogenesis of OA and its associated pain, the therapeutic potential of intra-articular drug delivery has been hindered by challenges such as rapid synovial clearance and the poor permeability of cartilage, limiting the effective inhibition of subchondral osteoclast activity. Methods Sixth generation polyamidoamine (PAMAM) dendrimers were used to delivery pamidronate disodium (PD) penetrating cartilage (PD@PM). PD@PM was loaded in aldehyde modified hyaluronic acid methacrylate (AHAMA) (PD@PM@MG), to facilitating the joint injection and conglutinating on the cartilage. Therapeutic effects of PD@PM@MG were validated by in vitro and in vivo OA models. Results PD@PM@MGs microspheres are uniformly distributed across the cartilage surface and sustained releasing of PD-loaded PAMAM. The positively charged PD-loaded PAMAM (< 10 nm) efficiently permeates the cartilage matrix, neutralizes damage-associated molecular patterns, and effectively inhibits subchondral osteoclasts activities. Mice OA model tests demonstrated that intra-articular injection of PD@PM@MGs markedly alleviated arthritic pain, mitigated cartilage degeneration, and attenuated subchondral bone remodeling. Conclusions The intra-articular injection of PD@PM@MGs significantly alleviates OA symptoms and progression, offering a novel direction for clinical OA intervention. Graphical Abstracthttps://doi.org/10.1186/s12951-025-03598-2OsteoarthritisPolyamidoamineHydrogel microspheresPain therapyCartilage degeneration
spellingShingle Zhenglin Zhu
Yujia Luo
Pengcheng Xiao
Yi Xie
Jun Zhang
Ke Huang
Xiangdong Wu
Ke Lu
Yuting Zhang
Jianye Tan
Hong Chen
Wei Huang
Yiting Lei
Junyi Liao
Carrier rocket-inspired hydrogel microspheres targeting subchondral bone osteoclast activity alleviate osteoarthritic pain and cartilage degeneration
Journal of Nanobiotechnology
Osteoarthritis
Polyamidoamine
Hydrogel microspheres
Pain therapy
Cartilage degeneration
title Carrier rocket-inspired hydrogel microspheres targeting subchondral bone osteoclast activity alleviate osteoarthritic pain and cartilage degeneration
title_full Carrier rocket-inspired hydrogel microspheres targeting subchondral bone osteoclast activity alleviate osteoarthritic pain and cartilage degeneration
title_fullStr Carrier rocket-inspired hydrogel microspheres targeting subchondral bone osteoclast activity alleviate osteoarthritic pain and cartilage degeneration
title_full_unstemmed Carrier rocket-inspired hydrogel microspheres targeting subchondral bone osteoclast activity alleviate osteoarthritic pain and cartilage degeneration
title_short Carrier rocket-inspired hydrogel microspheres targeting subchondral bone osteoclast activity alleviate osteoarthritic pain and cartilage degeneration
title_sort carrier rocket inspired hydrogel microspheres targeting subchondral bone osteoclast activity alleviate osteoarthritic pain and cartilage degeneration
topic Osteoarthritis
Polyamidoamine
Hydrogel microspheres
Pain therapy
Cartilage degeneration
url https://doi.org/10.1186/s12951-025-03598-2
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