Distribution and pharmacology of intravenous 99mTc-labeled multilamellar liposomes in rats and mice

Leela P. Kasi, Gabriel Lopez-Berestein, Kapil Mehta, Michael Rosenblum, Howard J. Glenn, Thomas P. Haynie, Giora Mavligit, Evan M. Hersh

Research output: Contribution to journalArticle

19 Scopus citations

Abstract

The use of liposomes for the delivery of macrophage activators offers a new approach for the selective targeting of antitumor therapy. We have investigated the distribution, retention, and pharmacology of multilamellar liposomes (phosphatidylserine (PS): phosphatidylcholine (PC) 3:7) on i.v. injection in normal rats. Sprague-Dawley rats were injected with doses varying from 300 to 1000 mg/kg of 99mTc-liposomes. The organ distribution of doses ranging from 300 to 500 mg/kg showed 45% mean uptake by liver, 25% by spleen, and 4% by lung. At higher doses of 800-1000 mg/kg, uptake in the lung increased significantly to 9 ± 3%. Whole body retention at 24 h after i.v. injection in Hale Stoner mice was 70%. The blood disappearance curve was biphasic and compared with the free isotope, a decrease was observed in the initial a phase t 1 2 while the terminal phase t 1 2 increased by 100%. These data suggest that encapsulation prolongs the initial distribution to the peripheral compartments and that higher doses may increase uptake by organs other than the liver.

Original languageEnglish (US)
Pages (from-to)35-37
Number of pages3
JournalInternational Journal of Nuclear Medicine and Biology
Volume11
Issue number1
DOIs
StatePublished - 1984

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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