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Peer-reviewedCC BY-NCInternational journal of nanomedicine

Triptolide and Celastrol for Rheumatoid Arthritis: Mechanism-Guided Nanoarchitectonics for Delivery Strategies to Enhance Efficacy and Reduce Toxicity.

7 affiliations
  1. 1Guangdong Traditional Medical and Sports Injury Rehabilitation Research Institute, The Affiliated Guangdong Second Provincial General Hospital of Jinan University, Guangzhou, Guangdong, 510317, People's Republic of China.
  2. 2Department of Rheumatology, The First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510405, People's Republic of China.
  3. 3Department of Orthopedics and Traumatology, Guangzhou Yuexiu District Orthopedics and Traumatology Rehabilitation Hospital, Guangzhou, Guangdong, 510100, People's Republic of China.
  4. 4Department of Acupuncture and Moxibustion, Baiyun Hospital of the First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510470, People's Republic of China.
  5. 5Department of General Surgery, Liuzhou Traditional Chinese Medical Hospital, Liuzhou, Guangxi, 545000, People's Republic of China.
  6. 6State Key Laboratory of Traditional Chinese Medicine Syndrome, The First Clinical Medical College of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510405, People's Republic of China.
  7. 7Guangdong Clinical Research Academy of Chinese Medicine, Guangzhou, Guangdong, 510405, People's Republic of China.

Abstract

Peidan Yang,1,2 Gangzhong Zhang,3 Liqun Wu,4 Chunfeng Xie,5 Qiang Xu2,6,71Guangdong Traditional Medical and Sports Injury Rehabilitation Research Institute, The Affiliated Guangdong Second Provincial General Hospital of Jinan University, Guangzhou, Guangdong, 510317, People’s Republic of China; 2Department of Rheumatology, The First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510405, People’s Republic of China; 3Department of Orthopedics and Traumatology, Guangzhou Yuexiu District Orthopedics and Traumatology Rehabilitation Hospital, Guangzhou, Guangdong, 510100, People’s Republic of China; 4Department of Acupuncture and Moxibustion, Baiyun Hospital of the First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510470, People’s Republic of China; 5Department of General Surgery, Liuzhou Traditional Chinese Medical Hospital, Liuzhou, Guangxi, 545000, People’s Republic of China; 6State Key Laboratory of Traditional Chinese Medicine Syndrome, The First Clinical Medical College of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510405, People’s Republic of China; 7Guangdong Clinical Research Academy of Chinese Medicine, Guangzhou, Guangdong, 510405, People’s Republic of ChinaCorrespondence: Qiang Xu, Department of Rheumatology, The First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510405, People’s Republic of China, Email [email protected]: Rheumatoid arthritis remains a leading cause of irreversible joint disability worldwide. Triptolide and celastrol, major bioactive compounds derived from Tripterygium wilfordii Hook F. (TwHF), have substantial therapeutic potential for rheumatoid arthritis. However, poor solubility, low oral bioavailability, narrow therapeutic windows, and dose-limiting systemic toxicity limit their clinical translation.Objective: This review integrates the anti-rheumatoid arthritis mechanisms of triptolide and celastrol with recent advances in nanodelivery systems to establish a mechanism-guided framework for nanocarrier design and clinical translation.Results: Triptolide and celastrol exert multifaceted anti-rheumatoid arthritis effects by inhibiting inflammatory signaling pathways, regulating macrophage polarization and T-cell homeostasis, suppressing fibroblast-like synoviocyte proliferation, and protecting bone and cartilage. Diverse nanodelivery platforms—including lipid-based, polymeric, inorganic, biomimetic, carrier-free, and hybrid systems—have substantially improved the bioavailability and lesion-targeting capability of triptolide and celastrol, achieving superior anti-inflammatory and joint-protective efficacy while minimizing systemic toxicity.Conclusion: Mechanism-guided nanodelivery may help translate triptolide and celastrol into safer, targeted rheumatoid arthritis therapies. Realizing this potential requires a shift from material-centric research toward application-oriented development supported by rigorous validation.Keywords: rheumatoid arthritis, mechanism-guided delivery, triptolide, celastrol, nanomedicine

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BibTeX
@article{yang2026triptolide,
  title = {{Triptolide and Celastrol for Rheumatoid Arthritis: Mechanism-Guided Nanoarchitectonics for Delivery Strategies to Enhance Efficacy and Reduce Toxicity.}},
  author = {Peidan Yang and Gangzhong Zhang and Liqun Wu and Chunfeng Xie and Qiang Xu},
  journal = {International journal of nanomedicine},
  year = {2026},
  month = oct,
  doi = {10.2147/ijn.s646722},
  url = {https://europepmc.org/article/MED/42953758},
  note = {CC BY-NC},
}
RIS
TY  - JOUR
TI  - Triptolide and Celastrol for Rheumatoid Arthritis: Mechanism-Guided Nanoarchitectonics for Delivery Strategies to Enhance Efficacy and Reduce Toxicity.
AU  - Peidan Yang
AU  - Gangzhong Zhang
AU  - Liqun Wu
AU  - Chunfeng Xie
AU  - Qiang Xu
PY  - 2026
DA  - 2026/10/24
JO  - International journal of nanomedicine
DO  - 10.2147/ijn.s646722
UR  - https://europepmc.org/article/MED/42953758
AB  - Peidan Yang,1,2 Gangzhong Zhang,3 Liqun Wu,4 Chunfeng Xie,5 Qiang Xu2,6,71Guangdong Traditional Medical and Sports Injury Rehabilitation Research Institute, The Affiliated Guangdong Second Provincial General Hospital of Jinan University, Guangzhou, Guangdong, 510317, People’s Republic of China; 2Department of Rheumatology, The First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510405, People’s Republic of China; 3Department of Orthopedics and Traumatology, Guangzhou Yuexiu District Orthopedics and Traumatology Rehabilitation Hospital, Guangzhou, Guangdong, 510100, People’s Republic of China; 4Department of Acupuncture and Moxibustion, Baiyun Hospital of the First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510470, People’s Republic of China; 5Department of General Surgery, Liuzhou Traditional Chinese Medical Hospital, Liuzhou, Guangxi, 545000, People’s Republic of China; 6State Key Laboratory of Traditional Chinese Medicine Syndrome, The First Clinical Medical College of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510405, People’s Republic of China; 7Guangdong Clinical Research Academy of Chinese Medicine, Guangzhou, Guangdong, 510405, People’s Republic of ChinaCorrespondence: Qiang Xu, Department of Rheumatology, The First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, 510405, People’s Republic of China, Email [email protected]: Rheumatoid arthritis remains a leading cause of irreversible joint disability worldwide. Triptolide and celastrol, major bioactive compounds derived from Tripterygium wilfordii Hook F. (TwHF), have substantial therapeutic potential for rheumatoid arthritis. However, poor solubility, low oral bioavailability, narrow therapeutic windows, and dose-limiting systemic toxicity limit their clinical translation.Objective: This review integrates the anti-rheumatoid arthritis mechanisms of triptolide and celastrol with recent advances in nanodelivery systems to establish a mechanism-guided framework for nanocarrier design and clinical translation.Results: Triptolide and celastrol exert multifaceted anti-rheumatoid arthritis effects by inhibiting inflammatory signaling pathways, regulating macrophage polarization and T-cell homeostasis, suppressing fibroblast-like synoviocyte proliferation, and protecting bone and cartilage. Diverse nanodelivery platforms—including lipid-based, polymeric, inorganic, biomimetic, carrier-free, and hybrid systems—have substantially improved the bioavailability and lesion-targeting capability of triptolide and celastrol, achieving superior anti-inflammatory and joint-protective efficacy while minimizing systemic toxicity.Conclusion: Mechanism-guided nanodelivery may help translate triptolide and celastrol into safer, targeted rheumatoid arthritis therapies. Realizing this potential requires a shift from material-centric research toward application-oriented development supported by rigorous validation.Keywords: rheumatoid arthritis, mechanism-guided delivery, triptolide, celastrol, nanomedicine
SN  - 1176-9114
SN  - 1178-2013
ER  -