In vitro and in vivo comparison of immunoliposomes made by conventional coupling techniques with those made by a new post-insertion approach

Biochim Biophys Acta. 2001 Aug 6;1513(2):207-16. doi: 10.1016/s0005-2736(01)00357-1.


Ligand-targeted liposomes have the potential to increase the therapeutic efficacy of antineoplastic agents. Recently, a combinatorial approach to the preparation of ligand-targeted liposomes has been developed, termed the post-insertion technique, which will facilitate the production of targeted liposomes. In this paper, Stealth immunoliposomes (SIL) coupled to anti-CD19 made by either a conventional coupling technique (SIL[anti-CD19]), or by the post-insertion technique (PIL[anti-CD19], were compared with respect to their in vitro binding and cytotoxicity and their ability to improve in vivo survival in tumor-bearing mice. The in vitro binding and uptake of PIL[anti-CD19] by CD19-expressing, B-cell lymphoma (Namalwa) cells was similar to that of SIL[anti-CD19] and both were significantly higher than binding of non-targeted liposomes (SL). In addition, no significant differences were found between the respective in vitro cytotoxicities of doxorubicin-loaded PIL[anti-CD19] or SIL[anti-CD19], or in their in vivo therapeutic efficacy in a murine model of human B-lymphoma. Overall, the results demonstrate that the post-insertion technique is a simple, flexible and effective means for preparing targeted liposomal drugs for clinical applications.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal
  • Antigens, CD19 / immunology
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / therapeutic use
  • Burkitt Lymphoma / drug therapy
  • Doxorubicin / administration & dosage
  • Doxorubicin / therapeutic use
  • Drug Carriers
  • Female
  • Ligands
  • Liposomes / chemical synthesis
  • Liposomes / immunology*
  • Liposomes / pharmacokinetics
  • Mice
  • Mice, Inbred BALB C
  • Mice, SCID
  • Micelles
  • Receptors, Cell Surface / immunology
  • Tumor Cells, Cultured


  • Antibodies, Monoclonal
  • Antigens, CD19
  • Antineoplastic Agents
  • Drug Carriers
  • Ligands
  • Liposomes
  • Micelles
  • Receptors, Cell Surface
  • Doxorubicin