Galantamine transdermal patch shows higher tolerability over oral galantamine in rheumatoid arthritis rat model

Abstract

Rheumatoid arthritis (RA) is a chronic autoimmune disease of idiopathic etiology that triggers inflammatory cytokines compromising the joint mobility. Epidemiological evidences recommend the utilization of galantamine (GH) to reverse the anti-inflammatory reactions induced RA. Oral administration of GH is non-selectivity due to its association with serious gastrointestinal symptoms which, could hinder its therapeutic success. Therefore, the present study aimed to validate the therapeutic potential of GH transdermal patches as a novel application to constitute an effective and tolerable delivery system for managing RA in adjuvant arthritis model. RA was induced in Sprague-Dawley rats intradermally by Heat-killed M (0.12 ml/day). Oral GH (1.25 mg/kg/day) and GH transdermal patch (2.5 mg/kg/2 days) were administrated for 14 days, during which the hind paw and body weight (BW) were assessed. Effects of C-reactive protein (CRP), inflammatory cytokines (TNF-α, IL-10 and IL-1β) and Janus kinase (JAK-2) were evaluated. Oral- and transdermal GH significantly improved the hind paw edema in arthritis animal model and offered a protective impact against RA. Oral GH group showed marked decrease in BW than that of transdermal patches group. Transdermal patch group showed a significant decrease in the level of IL-1β more than the oral group. However, no significant difference was detected in the levels of TNF-α and IL-10 between the two groups. It is concluded that GH transdermal patch can be a promising drug delivery system that copes with side effects better than oral GH consequently represents novel strategy in management of RA.

Keywords:

• Rheumatoid arthritis
• transdermal drug delivery
• galantamine
• adjuvant-induced arthritis
• complete Freund's adjuvant

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.

Additional information

Funding

This study was funded by the authors themselves.