Antibody-Targeted Liposomes: Development of a Cell-Specific Drug Delivery System

  • Timothy Heath
  • Keith Bragman
  • Katherine Matthay
  • Ninfa G. Lopez
  • Demetrios Papahadjopoulos


We have described the following important parameters for the development of antibody-directed liposomes in drug delivery.
  1. (i)

    Liposome-dependent cytotoxic agents: Drugs such as methotrexate-γ-aspartate which are unable to enter cells without a carrier are essential since their use eliminates the non-specific effects of drug which may leak from the liposomes.

  2. (ii)

    Multivalency of liposome interactions: Liposomes conjugated to antibody have a higher valency than the soluble antibody and can bind to cells with up to 1,000-fold higher affinity constant.

  3. (iii)

    Use of multiple ligands: Liposomes which interact with more than one ligand on the cell surface show marked resistance to inhibition of cell association by soluble ligands.

  4. (iv)

    Optimal liposome size for drug delivery: The optimal liposome size appears to vary from 0.05 to 0.1 µm depending on target cell type.


These experiments have been performed with liposomes conjugated to monoclonal anti H2Kk which bind to L929 cells and deliver drug 20 times more effectively to L929 cells than non-specific liposomes. We have also used liposomes conjugated to antiglycophorin antibody. These liposomes bind to K562 cells via an FC receptor and glycophorin A, and deliver drug 10 times more effectively than non-conjugated liposomes.


K562 Cell L929 Cell Free Drug Dihydrofolate Reductase Cell Association 
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Copyright information

© Plenum Press, New York 1984

Authors and Affiliations

  • Timothy Heath
    • 1
  • Keith Bragman
    • 1
  • Katherine Matthay
    • 1
  • Ninfa G. Lopez
    • 1
  • Demetrios Papahadjopoulos
    • 1
  1. 1.Cancer Research Institute, M-1282University of California Medical CenterSan FranciscoUSA

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