Characterization and Modulation of the Transferrin Receptor on Brain Capillary Endothelial Cells

Abstract

The TfR is expressed on BCECs and actively endocytoses Tf, making it a suitable target for drug delivery to the bloodbrain barrier and the CNS. DFO up-regulates the TfR expression level, which may influence targeting efficiency.

Angiopep-conjugated poly(ethylene glycol)-co-poly(ε-caprolactone) nanoparticles as dual-targeting drug delivery system for brain glioma

“…It is reported that various receptors are present on the luminal endothelial plasma membranes, including the transferring receptor, the insulin receptor, endothelial growth factors receptor, and low-density lipoprotein receptor [12,13]. Drug delivery systems which based on these receptors have been explored to deliver drugs across the BBB [14e16].…”

Gene delivery targeted to the brain using an Angiopep-conjugated polyethyleneglycol-modified polyamidoamine dendrimer

“…It has reported that different receptors are present on the luminal endothelial plasma membranes, including the transferrin receptor, the insulin receptor, and the low-density lipoprotein receptor-related protein (LRP) [17,18]. Drug delivery systems based on the receptor-mediated mechanism have been explored to deliver drugs into the brain [19][20][21].…”

Self-Assembled Polymersomes Conjugated with Lactoferrin as Novel Drug Carrier for Brain Delivery

“…One current candidate is receptors-mediated targeting via intravenous injection of ligand-conjugated drug delivery systems that target to receptors expressed on the luminal side of the BBB (2)(3)(4)(5)(6). Well-characterized BBB receptors mainly include the following: low-densities lipoprotein receptor (LDLR), transferrin receptor (7)(8)(9), epidermal growth factor receptor and insulin-like growth factor receptor (3,10). As a single-chain iron-binding glycoprotein, lactoferrin is a multifunctional protein to which several physiological roles have been attributed.…”