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Liposome-entrapped topoisomerase inhibitors

  • US 7,244,449 B2
  • Filed: 08/29/2002
  • Issued: 07/17/2007
  • Est. Priority Date: 09/16/1998
  • Status: Expired due to Term
First Claim
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1. A composition for treating a tumor in a subject, comprising liposomes composed of a vesicle-forming lipid and between about 1–

  • 20 mole percent of a vesicle-forming lipid derivatized with polyethyleneglycol having a molecular weight between 500–

    5,000 Daltons, said polymer being distributed on both sides of the liposomes'"'"' bilayer membranes; and

    entrapped in the liposomes, a topoisomerase inhibitor at a concentration of at least about 0.10 μ

    mole drug per μ

    mole lipid, said liposomes having an inside/outside ion gradient sufficient to retain the topoisomerase inhibitor within the liposomes at the specified concentration, and wherein the topoisomerase inhibitor is selected from the group consisting of MPE-camptothecin, topotecan, and (7-(2-N-isopropylamino)ethyl)-(20S)-camptothecin.

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