Related Experiment Video
Updated: Mar 15, 2026
04:50
Preliminary Study on Acupuncture Combined with Grain-sized Moxibustion for Treating Rheumatoid Arthritis with Finger Joint Pain
Published on: May 16, 2025
1.3K
Investigating the Potential of High Permeation Vesicle-Based Methotrexate Gel for Localized Therapy in Rheumatoid
Keshav Kumar1, Junia Akhtar1, Sayali Dighe1
1Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Sector 67, Punjab, 160062, India.
Pharmaceutical Research
|March 14, 2026
Summary
This study developed methotrexate-loaded high permeation vesicles (MTX-HPVs) for localized rheumatoid arthritis treatment. The MTX-HPVs gel demonstrated enhanced efficacy and safety, offering a promising localized therapy option.
Area of Science:
- Pharmacology and Drug Delivery
- Rheumatology
- Biomaterials Science
Background:
- Methotrexate (MTX) is a key drug for rheumatoid arthritis but faces systemic toxicity and bioavailability issues.
- Localized drug delivery aims to improve therapeutic outcomes by targeting specific sites and reducing systemic side effects.
- High permeation vesicles (HPVs) offer a potential strategy for enhanced localized drug delivery.
Purpose of the Study:
- To investigate the therapeutic potential of systematically designed methotrexate-loaded high permeation vesicles (MTX-HPVs) for rheumatoid arthritis.
- To formulate and characterize MTX-HPVs integrated into a carbopol gel for localized application.
- To evaluate the in vitro and in vivo efficacy and safety of MTX-HPVs gel compared to free MTX.
Main Methods:
- Formulation of MTX-HPVs using phospholipids and permeation enhancers via thin-film hydration.
- Integration of MTX-HPVs into a Carbopol® 934P NF gelling matrix.
- In vitro characterization including release studies, flux, permeation, and cellular uptake in macrophage cells.
- In vivo evaluation of anti-inflammatory effects, safety, and joint restoration in a rheumatoid arthritis model.
Main Results:
- Optimized MTX-HPVs exhibited sustained release for 48 hours and spherical morphology.
- MTX-HPVs gel showed significantly enhanced flux (6.9-fold) and permeation (3.5-fold) compared to free MTX gel.
- Improved cellular internalization, reduced IC50 (0.57 µg/mL), significant reduction in inflammation, and superior safety were observed in vivo.
- Radiographic imaging confirmed enhanced efficacy and joint-restorative effects of MTX-HPVs gel.
Conclusions:
- MTX-HPVs gel substantially enhanced the therapeutic efficacy of methotrexate for rheumatoid arthritis.
- High permeation vesicles (HPVs) represent a promising carrier system for localized methotrexate therapy.
- This formulation offers a potential improvement over systemic MTX administration for rheumatoid arthritis management.
Related Concept Videos
01:18Transdermal Drug Delivery Systems
94
Transdermal drug delivery systems (TDDS) enable the controlled release of drugs across the skin into systemic circulation. They are particularly advantageous for drugs with short half-lives or narrow therapeutic indices, as they maintain consistent plasma concentrations and reduce the risk of subtherapeutic or toxic levels.TDDS are categorized into monolithic, reservoir, and mixed systems. Monolithic systems embed the drug in a polymer matrix, where diffusion governs release. Reservoir systems...
94
01:29Drugs for Treatment of Crohn's Disease in IBD Using Immunomodulatory Agents
637
Crohn's disease is an inflammatory bowel disorder marked by chronic inflammation of the GI tract. Various treatment strategies for Crohn's disease are employed, such as immunomodulatory agents, glucocorticoids, and biologics or anti-TNF therapy. Azathioprine (Imuran), a commonly used immunomodulatory drug for Crohn's disease, is converted in the body to mercaptopurine, which inhibits purine biosynthesis and cell proliferation. Both are utilized in severe cases of Inflammatory Bowel...
637
01:24Modified-Release Drug Delivery Systems: Site-Targeted
70
Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
70