Nano Methotrexate versus Methotrexate in Targeting Rheumatoid Arthritis

Abstract

Nanomedicine has emerged as an important approach for targeting RA medication. Rheumatoid arthritis (RA) is a widespread autoimmune disorder marked by multiple inflamed joints. Gold nanoparticles (GNPs) have been demonstrated as efficacious nanocarriers due to their unique characteristics and the relative simplicity of their synthesis in varied sizes; moreover, they have the capability to alleviate several inflammatory markers. The current objective was to combine methotrexate (MTX) with GNPs to overcome MTX restrictions. GNPs were fabricated by a chemical reduction technique, utilizing sodium citrate and tween 20. The MTX-GNPs formulations were characterized in vitro by % entrapment efficiency (%EE), particle size, polydispersity index (PDI) zeta potential, and % release. The MTX-GNPs formulation was administrated as an intra-articular solution, and additionally, incorporated into a Carbopol gel to investigate its anti-arthritic effectiveness and bioavailability in vivo. The results indicated that a %EE of 87.53 ± 1.10%, and a particle size of 60.62 ± 2.41 nm with a PDI of 0.31 ± 0.03, and a zeta potential of −27.80 ± 0.36 mV were optimal. The in vitro release of MTX from the MTX-GNPs formulation demonstrated that the MTX-GNPs formulation’s release was 34.91± 1.96% and considerably (p < 0.05) lower than that of free MTX, showing a significant difference in dissolution patterns (p < 0.05). In vivo, MTX-GNPs formulations inhibited IL-6 by 36.52%, ACCP (63.25 %), COMP (28.16%), and RANKL (63.67%), as well as elevated IL-10 by 190.18%. Transdermal MTX-GNPs decreased IL-6 by 22.52%, ACCP (56.63%), COMP (52.64%), and RANKL (79.5%), as well as increased IL-10 by 168.37%. Histological investigation supported these recent findings. Conclusions: Marked improvements in MTX anti-arthritic effects are seen when it is conjugated to GNPs.

Fucoidan and dendrimer-based nanocapsule exhibiting effectiveness in methotrexate controlled delivery towards rheumatoid arthritis treatment

“…Materials MTX (Methotrexate) was acquired from Sigma (USA). PAMAM dendrimer G3.0 was synthesised at the Institute for Applied Materials Science following the described method [10,11]. Fucoidan (Fu) was purchased from Vietnam (Vietnam Fucoidan Joint Stock Company) [32].…”

“…These innovative delivery systems have demonstrated promising potential in improving the management of RA [6][7][8][9]. Among these advancements, various polymeric platforms have been extensively explored and engineered with precisely designed structures to enhance drug loading efficiency [10,11]. Nano-drug delivery systems play crucial roles in improving the effectiveness of treatment and reducing side effects of hydrophobic drugs.…”

Special Issue “Rheumatic Diseases: Pathophysiology, Targeted Therapy, Focus on Vascular and Pulmonary Manifestations 2022”

“…This study showed a marked improvement in the anti-arthritic effects of MTX when it was conjugated with GNPs. Furthermore, histological investigation supported these observations [5]. The aim of the third study was to study the IFN-regulated sialic-acid-binding Ig-like lectin 1 (SIGLEC-1) protein as a biomarker of disease phenotype, therapeutic response, and differential diagnosis in systemic sclerosis (SSc).…”