Liposomes and Local Hyperthermia: Selective Delivery of Methotrexate to Heated Tumors

Liposomes with phase transitions a few degrees above physiological temperature delivered more than four times as much methotrexate to murine tumors heated to 42°C as to unheated control tumors. Most of the accumulated drug appeared to be intracellular and bound to dihydrofolate reductase, the enzyme...

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Bibliographic Details
Published in:	Science (American Association for the Advancement of Science) Vol. 204; no. 4389; pp. 188 - 191
Main Authors:	Weinstein, J. N., Magin, R. L., Yatvin, M. B., Zaharko, D. S.
Format:	Journal Article
Language:	English
Published:	United States American Association for the Advancement of Science 13-04-1979
Subjects:	Animals Antineoplastics Blood Dosage Hot Temperature Hyperthermia Induced hyperthermia Lipids Liposomes Liposomes - therapeutic use Lungs Male Metabolic Clearance Rate Methotrexate - administration & dosage Methotrexate - metabolism Mice Neoplasms, Experimental - drug therapy Phospholipids Structure-Activity Relationship Transition temperature Tumors
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Summary:	Liposomes with phase transitions a few degrees above physiological temperature delivered more than four times as much methotrexate to murine tumors heated to 42°C as to unheated control tumors. Most of the accumulated drug appeared to be intracellular and bound to dihydrofolate reductase, the enzyme blocked by methotrexate in its role as an antineoplastic agent.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0036-8075 1095-9203
DOI:	10.1126/science.432641