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Transferrin Receptor and Targeting Strategies

  • Harsh A. Joshi
  • Esha S. Attar
  • Prajakta Dandekar
  • Padma V. DevarajanEmail author
Chapter
Part of the AAPS Advances in the Pharmaceutical Sciences Series book series (AAPS, volume 39)

Abstract

Treatment of cancer is an extraordinary challenge using conventional therapy due to serious side effects. Targeted delivery of therapeutics has changed this paradigm. Among various approaches, receptor-mediated targeting presents great promise. Since transferrin receptor (TfR) is known to be overarticulated in various cancers, it is a lucrative target in cancer research. TfR-mediated drug delivery can deliver therapeutic cargo into tumor cells to enhance cytotoxicity with significant reduction in systemic toxicity. This has propelled the exploration of innovative targeting approaches using nanodrug delivery systems. This chapter discusses the TfR physiology and related pathophysiology, and also summarizes various drug-targeting strategies and theranostics, which rely on transferrin (Tf) as the targeting ligand for cell-directed delivery. Further forays into evaluating TfR-mediated targeting as a strategy to tackle brain infections are also proposed.

Keywords

Transferrin targeted drug delivery cancer infection blood–brain barrier theranostics 

Abbreviations

AL

Acute leukemia

ALL

Acute lymphoblastic leukemia

CMC

Critical micelle concentration

Copper sulfate

CuS

DA

Dodecylamine

DAB

Diaminobutyric poly(propylene imine)

Fe-Tf

Iron-carrier protein transferrin

HFE

Hereditary hemochromatosis protein

H-ferritin

Ferritin-H homopolymer

HIF

Hypoxia-inducible factors

hLf

Human lactoferrin

HRE

Hypoxia-responsive elements

hTf

Human serum transferrin

hTF/2N

Human serum transferrin

IgG1

Antihuman TfR antibody

IgG1

Monoclonal antibody 454A12 P

IgG1

Monoclonal antibody 5E9

IgG1

Monoclonal antibody HB21

IgG3

Chimeric human TfR antibody fused

IRE

Iron-responsive elements

IRP

Iron regulatory proteins

MrTf

Rabbit serum transferrin

MTF

Melanotransferrin

mTOR

Mammalian target of rapamycin

NIR

Near-infrared

NLCs

Nanostructured lipid carriers

oTf

Chicken ovotransferrin

PEG

Polyethylene glycol

PEG-PE

Polyethylene glycol-phosphatidylethanolamine

PHD

Prolyl hydroxylases

Reg1

Regnase-1

RGD

Arginine–glycine–aspartic acid

ROS

Reactive oxygen species

SA

Stearylamine

SLNs

Solid lipid nanoparticles

SP

Spermine

Tf

Transferrin

TfR

Transferrin receptor

TfR1

Transferrin receptor 1

TfR2

Transferrin receptor 2

TPGS-COOH

D-α-tocopheryl polyethylene glycol 1000 succinate

TTP

Tristetraprolin

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Harsh A. Joshi
    • 1
  • Esha S. Attar
    • 1
  • Prajakta Dandekar
    • 2
  • Padma V. Devarajan
    • 2
    Email author
  1. 1.Department of Pharmaceutical Sciences & TechnologyInstitute of Chemical TechnologyMatunga, MumbaiIndia
  2. 2.Department of Pharmaceutical SciencesInsitute of Chemical Technology, Deemed University, Elite Status and Centre of Excellence, Government of MaharashtraMumbaiIndia

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