Drug Delivery and Translational Research

, Volume 8, Issue 5, pp 1545–1563 | Cite as

Transferrin receptors-targeting nanocarriers for efficient targeted delivery and transcytosis of drugs into the brain tumors: a review of recent advancements and emerging trends

  • Hira ChoudhuryEmail author
  • Manisha Pandey
  • Pei Xin Chin
  • Yee Lin Phang
  • Jeng Yuen Cheah
  • Shu Chien Ooi
  • Kit-Kay Mak
  • Mallikarjuna Rao Pichika
  • Prashant Kesharwani
  • Zahid Hussain
  • Bapi Gorain
Review Article


Treatment of glioblastoma multiforme (GBM) is a predominant challenge in chemotherapy due to the existence of blood–brain barrier (BBB) which restricts delivery of chemotherapeutic agents to the brain together with the problem of drug penetration through hard parenchyma of the GBM. With the structural and mechanistic elucidation of the BBB under both physiological and pathological conditions, it is now viable to target central nervous system (CNS) disorders utilizing the presence of transferrin (Tf) receptors (TfRs). However, overexpression of these TfRs on the GBM cell surface can also help to avoid restrictions of GBM cells to deliver chemotherapeutic agents within the tumor. Therefore, targeting of TfR-mediated delivery could counteract drug delivery issues in GBM and create a delivery system that could cross the BBB effectively to utilize ligand-conjugated drug complexes through receptor-mediated transcytosis. Hence, approach towards successful delivery of antitumor agents to the gliomas has been making possible through targeting these overexpressed TfRs within the CNS and glioma cells. This review article presents a thorough analysis of current understanding on Tf-conjugated nanocarriers as efficient drug delivery system.


Cancer Glioblastoma Transferrin receptor Targeted delivery Blood–brain barrier Nanotechnology Brain tumor chemotherapy Theranostic application 



The authors would like to acknowledge the School of Pharmacy, International Medical University for providing resources and support in completing this work.

Compliance with ethical standards

Conflict of interest

The authors declare that there is no conflict of interest.


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Copyright information

© Controlled Release Society 2018

Authors and Affiliations

  • Hira Choudhury
    • 1
    Email author return OK on get
  • Manisha Pandey
    • 1
  • Pei Xin Chin
    • 2
  • Yee Lin Phang
    • 2
  • Jeng Yuen Cheah
    • 2
  • Shu Chien Ooi
    • 2
  • Kit-Kay Mak
    • 3
  • Mallikarjuna Rao Pichika
    • 4
    • 5
  • Prashant Kesharwani
    • 6
  • Zahid Hussain
    • 7
  • Bapi Gorain
    • 8
  1. 1.Department of Pharmaceutical Technology, School of PharmacyInternational Medical UniversityKuala LumpurMalaysia
  2. 2.School of PharmacyInternational Medical UniversityKuala LumpurMalaysia
  3. 3.School of Postgraduate Studies and ResearchInternational Medical UniversityKuala LumpurMalaysia
  4. 4.Department of Pharmaceutical Chemistry, School of PharmacyInternational Medical UniversityKuala LumpurMalaysia
  5. 5.Centre for Bioactive Molecules and Drug Delivery, Institute for Research, Development and InnovationInternational Medical UniversityKuala LumpurMalaysia
  6. 6.Pharmaceutics DivisionCSIR-Central Drug Research InstituteLucknowIndia
  7. 7.Department of Pharmaceutics, Faculty of PharmacyUniversiti Teknologi MARA SelangorPuncak AlamMalaysia
  8. 8.Faculty of PharmacyLincoln University CollegeKuala LumpurMalaysia

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