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Hyaluronic-Acid-Functionalized Tofacitinib Loaded Transethosomes for Targeted Drug Delivery in Rheumatoid Arthritis
Pavani Chowdary1,2, Eswara Rao Puppala3, Chandra Lekha Putta1
1Department of Biomedical Engineering, Indian Institute of Technology Hyderabad, Kandi 502284, Telangana, India.
Hyaluronic acid-coated transethosomes offer targeted topical delivery of tofacitinib for rheumatoid arthritis, reducing systemic side effects. This novel HA-TOF-TE system demonstrates significant anti-inflammatory effects and improved efficacy compared to traditional treatments.
Area of Science:
- Nanotechnology
- Pharmacology
- Rheumatology
Background:
- Oral tofacitinib (TOF) is effective for rheumatoid arthritis (RA) but causes systemic side effects.
- Targeted topical delivery systems are needed to improve RA treatment efficacy and reduce toxicity.
Purpose of the Study:
- To develop and evaluate hyaluronic-acid-coated transethosomes (HA-TOF-TE) for targeted topical delivery of tofacitinib (TOF).
- To assess the potential of HA-TOF-TE to reduce systemic toxicity and enhance therapeutic efficacy in rheumatoid arthritis.
Main Methods:
- Transethosomes (TE) were synthesized using cold sonication and functionalized with hyaluronic acid (HA).
- Formulations were characterized for particle size, zeta potential, and entrapment efficiency.
- In vitro drug release, ex vivo skin permeability, and in vivo anti-inflammatory efficacy in a rat model were evaluated.
Main Results:
- Optimized HA-TOF-TE showed a particle size of 151.5 nm and high entrapment efficiency.
- Ex vivo studies indicated enhanced skin retention and drug flux for HA-TOF-TE.
- In vivo studies demonstrated significant anti-inflammatory effects of HA-TOF-TE in arthritic rats, with reduced pro-inflammatory cytokines (IL-1, IL-6, PGE-2) and gene expression (IL-6, CD44, collagen II).
Conclusions:
- Hyaluronic acid-coated transethosomes provide an effective targeted delivery system for tofacitinib in rheumatoid arthritis.
- HA-TOF-TE significantly reduces inflammation and systemic side effects, offering a promising alternative to conventional oral tofacitinib therapy.
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