Effectiveness of anti-folate receptor β antibody conjugated with truncatedPseudomonas exotoxin in the targeting of rheumatoid arthritis synovial macrophages

Imaging of activated macrophages in experimental osteoarthritis using folate-targeted animal single-photon-emission computed tomography/computed tomography

“…The cell specificity of folate-based imaging has been thoroughly investigated in multiple previous studies, using flow cytometry, confocal microscopy, and in vivo macrophage elimination using clodronate-laden liposomes as determinants for cell phenotyping (11,14,(32)(33)(34). In the present study, an almost total absence of radioactivity in the knee joint after elimination of macrophages using clodronate-laden liposomes was observed.…”

Cholesterol as a bilayer anchor for PEGylation and targeting ligand in folate‐receptor‐targeted liposomes

“…It is also possible that folate-PEG-Chol targeted liposomes were more easily captured by the FR on activated macrophage, which can be utilized for treatment chronic inflammatory diseases such as rheumatoid arthritis. [67][68][69][70] In summary, we have prepared and evaluated FR-targeted liposomes incorporating cholesterol derivatives mPEG-Chol and F-PEG-Chol. The particle properties, such as the morphology, stability, in vitro release, targeting efficacy, and in vivo circulation were evaluated in parallel with liposomes containing DSPE-anchored derivatives.…”

The Development of Targeted Drug Delivery Systems for Rheumatoid Arthritis Treatment

“…In addition to the potential for passive targeting, the two primary cell types found within the pannus tissue, rheumatoid arthritis synovial fibroblasts (RASFs) and rheumatoid arthritis synovial macrophages (RASMs) selectively express surface receptors, such as CD44 (Haynes et al, 1991;Johnson et al, 1993), folate receptor  (Nagayoshi et al, 2005;van der Heijden et al, 2009), and integrin  V  3 (Wilder, 2002) that are candidates for active targeting. Angiogenic vascular endothelial cells (VECs) are also present as a result of neovascularization, and the E-selectin adhesion molecule has been identified as another viable target for drug delivery (Jamar et al, 2002).…”

“…In contrast, membrane associated folate receptors (MFRs) are restricted in expression and facilitate uptake by endocytosis. The beta isoform of MFR (FR ) is expressed selectively by activated macrophages within the pannus tissue (Nagayoshi et al, 2005;van der Heijden et al, 2009). Thus, folate may serve as an effective means of actively targeting the pannus tissue.…”