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Antineoplastic activity of sterically stabilized alkylphosphocholine liposomes in human breast carcinomas

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Abstract

New sterically stabilized liposomes derived from the antitumoragent hexadecylphosphocholine with reduced uptake by the mononuclearphagocyte system and improved antitumor activities were developedand tested. The bilayer of such sterically stabilizedliposomes consists of hexadecylphosphocholine, cholesterol and polyethylene glycol-linkedphosphoethanolamine. The measurement of carbon clearance in miceshows that these stabilized liposomes, in contrast toconventional alkylphosphocholine liposomes, are not largely engulfed bythe mononuclear phagocyte system. Their therapeutic activity onexperimental human breast carcinomas MaTu, MT-1 and MT-3was tested in nude mice. Especially in theMaTu models the sterically stabilized hexadecylphosphocholine liposomes resultedin significantly reduced tumor growth in comparison toconventional hexadecylphosphocholine liposomes or free hexadecylphosphocholine. The enhancedtherapeutic efficacy of sterically stabilized hexadecylphosphocholine liposomes isprobably related to the extended circulation time ofthe formulation and its accumulation in tumors.

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Authors and Affiliations

  1. Institute for Ultrastructure Research Friedrich-Schiller-University Jena, Germany

    D. Arndt, R. Zeisig, I. Eue & I. Fichtner

  2. Max-Delbrück-Center of Molecular Medicine, 13122, Berlin-Buch, Germany

    B. Sternberg

Authors
  1. D. Arndt
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  2. R. Zeisig
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  3. I. Eue
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  4. B. Sternberg
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  5. I. Fichtner
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Arndt, D., Zeisig, R., Eue, I. et al. Antineoplastic activity of sterically stabilized alkylphosphocholine liposomes in human breast carcinomas. Breast Cancer Res Treat 43, 237–246 (1997). https://doi.org/10.1023/A:1005798715192

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