Antitumor activity of a water-insoluble compound entrapped in liposomes on L1210 leukemia in mice.

Abstract

The use of sonicated phospholipid vesicles (liposomes) as carriers of 2-[3'-(methoxycarbonylamino)-phenyl]-3-phenyl-6-methoxycarbonylamino-4-(3H)- quinazolone (NSC-251635), a water-insoluble antimitotic compound, was investigated in mice. NSC-251635 was incorporated in egg yolk lecithin, cholesterol, and stearylamine (4:3:1) liposomes. In vitro, NSC-251635 in suspension or entrapped in liposomes was not toxic for L1210 cells. In vivo, after ip or iv injections to CDF1 mice bearing intraperitoneal or intravenous L1210 leukemia, NSC-251635 was active only when it was incorporated in the liposomes and not when it was given as a suspension in Klucel or in saline. The NSC-251635 liposome preparation induced significantly prolonged survival of the treated animals.

• Authors: C Brassinne, G Atassi, J Frühling, W Penasse, A Coune, J Hildebrand, J M Ruysschaert, C Laduron
• Journal: Journal of the National Cancer Institute (J Natl Cancer Inst) Vol. 70 Issue 6 Pg. 1081-6 (Jun 1983) ISSN: 0027-8874 [Print] United States
• PMID: 6574278 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Liposomes
• Quinazolines
• NSC 251635

Topics

• Animals
• Chromatography, Gel
• Dose-Response Relationship, Drug
• Female
• In Vitro Techniques
• Injections, Intraperitoneal
• Injections, Intravenous
• Leukemia L1210 (drug therapy, pathology)
• Liposomes (administration & dosage, isolation & purification)
• Male
• Mice
• Mice, Inbred Strains
• Neoplasm Transplantation
• Quinazolines (administration & dosage)