• D L Iden and T M Allen.
• Department of Pharmacology, University of Alberta, Edmonton, AB, Canada T6G 2H7.
• Biochim. Biophys. Acta. 2001 Aug 6; 1513 (2): 207-16.

AbstractLigand-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.

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