Preferential localization of radiolabeled liposomes in liver

• Published in: Journal of pharmaceutical sciences Vol. 67; no. 6; p. 795
• Main Authors: Hinkle, G H, Born, G S, Kessler, W, Shaw, S M
• Format: Journal Article
• Language: English
• Published: United States 01-06-1978
• Subjects: Animals; Liposomes - metabolism; Liver - metabolism; Male; Mice; Microscopy, Electron; Particle Size; Technetium; Tissue Distribution
• ISSN: 0022-3549
• DOI: 10.1002/jps.2600670617

Liposome formulations were studied to achieve an efficient entrapment procedure for the production of liposomes of 99mTc-pentetic acid. The entrapment efficiency was studied by separation of the product using column chromatography. The particle-size range of the prepared liposomes was evaluated using electron microscopy. Entrapment techniques and separation procedures led to a liposome preparation with particles in the colloidal size range (0.001-0.5 micron). Dramatic differences in the organ distribution of the liposome preparation in mice were produced when different particle-size ranges were injected. Liposomes eluted in the first fraction after the void volume led to a maximum uptake by the liver and spleen 10 min after intravenous injection. Liposomes from pooled fractions provided less than half of the activity in the liver, as did the narrow size range liposome preparation.