Increased therapeutic efficiency of a lipid-soluble alkylating agent incorporated in liposomes

A highly hydrophobic alkylating agent, 1-N,N-bis(beta-bromoethyl) amino-3-methylnaphthalene, given as the free drug in oil, cured a substantial proportion of mice bearing the PC6 myeloma in the dose range 2-7 mg/kg. However, these doses were toxic, and the LD50 was 6-7 mg/kg. When incorporated in li...

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Bibliographic Details
Published inBritish journal of cancer Vol. 45; no. 6; pp. 830 - 834
Main Authors Babbage, J W, Berenbaum, M C
Format Journal Article
LanguageEnglish
Published England Nature Publishing Group 01.06.1982
Subjects
1-Naphthylamine - analogs & derivatives
1-Naphthylamine - therapeutic use
1-Naphthylamine - toxicity
Alkylating Agents - therapeutic use
Alkylating Agents - toxicity
Animals
Dose-Response Relationship, Drug
Liposomes - administration & dosage
Male
Mice
Mice, Inbred BALB C
Multiple Myeloma - drug therapy
Naphthalenes - therapeutic use
Neoplasms, Experimental - drug therapy
Oils - administration & dosage
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Summary:A highly hydrophobic alkylating agent, 1-N,N-bis(beta-bromoethyl) amino-3-methylnaphthalene, given as the free drug in oil, cured a substantial proportion of mice bearing the PC6 myeloma in the dose range 2-7 mg/kg. However, these doses were toxic, and the LD50 was 6-7 mg/kg. When incorporated in liposomes, similar curative effects were obtained at doses of 10-41 mg/kg without material toxicity, even at the highest dose. Liposome entrapment therefore greatly increases the therapeutic efficiency of this agent.
ISSN:0007-0920
1532-1827
DOI:10.1038/bjc.1982.134