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Orally Administered Self-Microemulsifying Celastrol Alleviates Rheumatoid Arthritis by Modulating the Expression of
Boqin Ma1, Yan Li2, Jiahui Zhang3
1School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China.
Pharmaceutics
|June 26, 2026
Summary
This study developed an oral celastrol-loaded self-microemulsifying drug delivery system (Cel-SMEDDS) for rheumatoid arthritis (RA) treatment. Cel-SMEDDS demonstrated superior anti-inflammatory effects and safety compared to free celastrol, showing promise for RA therapy.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Immunology
Background:
- Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by joint inflammation and destruction.
- Celastrol, a natural compound, exhibits anti-inflammatory properties but suffers from poor oral bioavailability and potential toxicity.
- Developing effective and safe delivery systems for celastrol is crucial for its therapeutic application in RA.
Purpose of the Study:
- To formulate and characterize an oral celastrol-loaded self-microemulsifying drug delivery system (Cel-SMEDDS).
- To evaluate the in vitro and in vivo anti-inflammatory efficacy of Cel-SMEDDS against rheumatoid arthritis.
- To assess the preliminary safety profile of the Cel-SMEDDS formulation.
Main Methods:
- Formulation of Cel-SMEDDS using solubility screening, excipient compatibility, and pseudo-ternary phase diagrams.
- Characterization of Cel-SMEDDS including particle size, PDI, zeta potential, in vitro release, and stability.
- In vitro evaluation of anti-inflammatory activity in LPS-induced macrophages and in vivo assessment in collagen-induced arthritis (CIA) mouse model.
Main Results:
- The optimal Cel-SMEDDS formulation exhibited a particle size of 26.70 nm and enhanced celastrol's cytotoxicity against M1 macrophages.
- Cel-SMEDDS significantly suppressed pro-inflammatory cytokines (TNF-α, IL-1β) in vitro and reduced paw swelling and joint damage in CIA mice.
- Oral Cel-SMEDDS demonstrated superior anti-RA efficacy compared to free celastrol with no significant adverse effects in preliminary safety evaluations.
Conclusions:
- The optimized oral Cel-SMEDDS effectively delivers celastrol, showing enhanced anti-RA activity and improved safety profile.
- This formulation overcomes the limitations of free celastrol, presenting a promising therapeutic strategy for rheumatoid arthritis.
- Cel-SMEDDS holds significant potential for clinical translation in the treatment of RA.
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