Receptor-Mediated Drug Delivery

Chris V. Galliford, Philip S. Low

Research output: Chapter in Book/Report/Conference proceedingChapter

4 Scopus citations


The development of receptor-targeted therapeutic agents has been initiated primarily to limit the distribution of toxic drugs to only the pathologic cells, thus minimizing collateral damage to normal cells. Receptor-mediated drug delivery can also enable otherwise membrane-impermeable drugs to enter target cells by receptor-mediated endocytosis, or it can induce desirable changes in cell behavior by activating a receptor's normal signaling pathway. This chapter begins by summarizing the basic characteristics of the receptor-mediated endocytosis process. It then elaborates on two important characteristics for selection of a receptor for drug delivery: receptor specificity and internalization/recycling. While the ligand, linker, and drug can all take on a diversity of sizes, shapes, and chemistries, a few fundamental principles can be followed to enhance therapeutic efficacy. The chapter describes the preferred characteristics of both the ligand and the drug. It also illustrates the techniques of folate-targeted drug delivery, folate-targeted radiodiagnostic imaging, chemotherapy, and immunotherapy.

Original languageEnglish (US)
Title of host publicationDrug Delivery
Subtitle of host publicationPrinciples and Applications: Second Edition
EditorsB. Wang, L Hu, T. J. Siahaan
Number of pages24
ISBN (Electronic)9781118833322
ISBN (Print)9781118833360
StatePublished - Mar 25 2016


  • Folate-targeted chemotherapy
  • Folate-targeted drug delivery
  • Folate-targeted immunotherapy
  • Folate-targeted radiodiagnostic imaging
  • Ligand
  • Receptor specificity
  • Receptor-mediated drug delivery
  • Receptor-mediated endocytosis

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)
  • Engineering(all)
  • Medicine(all)


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