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Drug delivery via the transferrin receptor-mediated endocytosis pathway

Qing Xia, Xiu-Wei Yang, Xiao-Da Yang*, Zhong-Ming Qian, Kui Wang
  

  1. 1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
    2. The State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China
    3. Laboratory of Iron Metabolism, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Kowloon, Hong Kong
  • Received:2008-11-10 Revised:2009-02-10 Online:2009-03-15 Published:2009-03-15
  • Contact: Xiao-Da Yang*

Abstract:

The membrane transferrin receptor-mediated endocytosis has been exploited for developing novel targeted drug delivery systems, which could have a variety of applications in the site-specific delivery of anticancer drugs, proteins and therapeutic genes into proliferating malignant cells that overexpress the transferrin receptors. This is achieved by coupling transferrin or monoclonal antibody to transferrin receptor with therapeutic drugs or drug delivery vesicles. The transferrin conjugates can be obtained by use of either bifunctional chemical linkers or by genetic infusion of therapeutic peptides/proteins into the structure of transferrin / and monoclonal antibody to transferrin receptor. A variety of drug carriers such as liposomes, nanoparticles and DNA-polymer complexes (i.e. polyplex and lipoplex) were used to efficiently deliver the transferrin conjugates. Use of transferrin conjugates results in improvement in drug efficacy, selectivity and drug release as well as reduction in drug toxicity. This paper reviews the basic biochemistry of transferrin and the transferrin receptor as well as the strategy for developing targeted drug delivery system.

Key words: Transferrin, Transferrin, Transferrin receptor, Transferrin receptor, Drug delivery, Drug delivery

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