Development and Evaluation of Novel Leflunomide SPION Bioemulsomes for the Intra-Articular Treatment of Arthritis

Abstract

Systemic treatments for rheumatoid arthritis are associated with many side effects. This study aimed to minimize the side effects associated with the systemic administration of leflunomide (LEF) by formulating LEF-loaded emulsomes (EMLs) for intra-articular administration. Additionally, EMLs were loaded with supramagnetic nanoparticles (SPIONs) to enhance joint localization, where a magnet was placed on the joint area after intra-articular administration. Full in vitro characterization, including colloidal characteristics, entrapment efficiency, and in vitro release were conducted besides the in vivo evaluation in rats with adjuvant-induced arthritis. In vivo study included joint diameter measurement, X-ray radiographic analysis, RT-PCR analysis, Western blotting, ELISA for inflammatory markers, and histopathological examination of dissected joints. The particle size and entrapment efficiency of the selected LEF SPION EMLs were 198.2 nm and 83.7%, respectively. The EMLs exhibited sustained release for 24 h. Moreover, in vivo evaluation revealed LEF SPION EMLs to be superior to the LEF suspension, likely due to the increase in LEF solubility by nanoencapsulation that improved the pharmacological effects and the use of SPION that ensured the localization of EMLs in the intra-articular cavity upon administration.

Protective effect of Moringa oleifera leaf ethanolic extract against uranyl acetate-induced testicular dysfunction in rats

“…Afterward, sections were washed using immune washing Tris buffer and incubated with the secondary antibody HRP Envision kit (DAKO) for 20 min, followed by another wash using immune washing Tris buffer. The sections were stained with hematoxylin for 2–5 min after establishing the reaction with DAB for 2–3 minutes 30 .…”

Neuroprotective Effect of Artichoke-Based Nanoformulation in Sporadic Alzheimer’s Disease Mouse Model: Focus on Antioxidant, Anti-Inflammatory, and Amyloidogenic Pathways

“…Another set of tissue sections was stained by Toluidine blue stain for the quantification of intact neurons, then inspected with light microscope. Standard protocols for sample preparation, staining, and analysis were followed according to Abbas, Culling and Abbas [ 81 , 82 , 83 ].…”

Magnetic targeting of lornoxicam/SPION bilosomes loaded in a thermosensitive in situ hydrogel system for the management of osteoarthritis: Optimization, in vitro, ex vivo, and in vivo studies in rat model via modulation of RANKL/OPG

“…Superparamagnetic iron oxide nanoparticles (SPIONs) can enhance the targeting of nanocarrier loaded with the drug by guiding it to the site of action with the aid of an external magnetic field [ 28 ]. SPIONs provide a number of benefits, including ease of fabrication, biocompatibility, possibility of surface functionalization, and the capacity for accurate remote control without leaving a residual magnetic impact after the elimination of the external magnetic field [ 29 ]. Drug-SPION coupling for magnetic drug delivery can be accomplished either by binding the drug directly to the iron oxide surface or by encasing drugs as well as SPIONs within nanocarriers [ 30 ].…”