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 language | English (US) |
|---|---|
| Pages (from-to) | 35-37 |
| Number of pages | 3 |
| Journal | International Journal of Nuclear Medicine and Biology |
| Volume | 11 |
| Issue number | 1 |
| DOIs | |
| State | Published - 1984 |
| Externally published | Yes |
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ASJC Scopus subject areas
- Radiology Nuclear Medicine and imaging
Cite this
Distribution and pharmacology of intravenous 99mTc-labeled multilamellar liposomes in rats and mice. / Kasi, Leela P.; Lopez-Berestein, Gabriel; Mehta, Kapil; Rosenblum, Michael; Glenn, Howard J.; Haynie, Thomas P.; Mavligit, Giora; Hersh, Evan M.
In: International Journal of Nuclear Medicine and Biology, Vol. 11, No. 1, 1984, p. 35-37.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Distribution and pharmacology of intravenous 99mTc-labeled multilamellar liposomes in rats and mice
AU - Kasi, Leela P.
AU - Lopez-Berestein, Gabriel
AU - Mehta, Kapil
AU - Rosenblum, Michael
AU - Glenn, Howard J.
AU - Haynie, Thomas P.
AU - Mavligit, Giora
AU - Hersh, Evan M
PY - 1984
Y1 - 1984
N2 - 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.
AB - 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.
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UR - http://www.scopus.com/inward/citedby.url?scp=0021271439&partnerID=8YFLogxK
U2 - 10.1016/0047-0740(84)90028-7
DO - 10.1016/0047-0740(84)90028-7
M3 - Article
C2 - 6735607
AN - SCOPUS:0021271439
VL - 11
SP - 35
EP - 37
JO - Nuclear Medicine and Biology
JF - Nuclear Medicine and Biology
SN - 0969-8051
IS - 1
ER -