Crossref journal-article
Proceedings of the National Academy of Sciences
Proceedings of the National Academy of Sciences (341)
Abstract

Human serum albumin (HSA) derivatized with cis -aconitic anhydride was covalently coupled to liposomes with a size of approximately 100 nm [polyaconitylated HSA (Aco-HSA) liposomes]. Within 30 min after injection into a rat, Aco-HSA liposomes were completely cleared from the blood and almost exclusively taken up by the liver, whereas in control liposomes 80% was still present in the blood at that time. Endothelial cells were shown to account for almost two-thirds of the hepatic uptake of the Aco-HSA liposomes, the remainder being recovered mainly in the liver macrophages (Kupffer cells). With fluorescently labeled liposomes it was shown that the Aco-HSA liposomes target a vast majority (>85%) of the cells in the endothelial cell population. Control liposomes were not taken up to a significant extent by the endothelial cells. Uptake of Aco-HSA liposomes by both endothelial and Kupffer cells was inhibited by preinjection with polyinosinic acid, indicating the involvement of scavenger receptors in the uptake process. The uptake of Aco-HSA liposomes by liver endothelial cells was dependent on liposome size; with increasing liposome diameter endothelial cell uptake decreased in favor of Kupffer cell uptake. We have demonstrated that massive in vivo targeting of liposomes to a defined cell population other than macrophages is possible. Aco-HSA liposomes thus may represent an attractive drug carrier system for treatment of various liver or liver endothelium-associated disorders.

Bibliography

Kamps, J. A. A. M., Morselt, H. W. M., Swart, P. J., Meijer, D. K. F., & Scherphof, G. L. (1997). Massive targeting of liposomes, surface-modified with anionized albumins, to hepatic endothelial cells. Proceedings of the National Academy of Sciences, 94(21), 11681–11685.

Authors 5
  1. Jan A. A. M. Kamps (first)
  2. Henriëtte W. M. Morselt (additional)
  3. Pieter J. Swart (additional)
  4. Dick K. F. Meijer (additional)
  5. Gerrit L. Scherphof (additional)
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Dates
Type When
Created 23 years, 1 month ago (July 26, 2002, 10:31 a.m.)
Deposited 3 years, 4 months ago (April 13, 2022, 2:22 p.m.)
Indexed 1 month ago (Aug. 2, 2025, 12:50 a.m.)
Issued 27 years, 10 months ago (Oct. 14, 1997)
Published 27 years, 10 months ago (Oct. 14, 1997)
Published Online 27 years, 10 months ago (Oct. 14, 1997)
Published Print 27 years, 10 months ago (Oct. 14, 1997)
Funders 0

None

@article{Kamps_1997, title={Massive targeting of liposomes, surface-modified with anionized albumins, to hepatic endothelial cells}, volume={94}, ISSN={1091-6490}, url={http://dx.doi.org/10.1073/pnas.94.21.11681}, DOI={10.1073/pnas.94.21.11681}, number={21}, journal={Proceedings of the National Academy of Sciences}, publisher={Proceedings of the National Academy of Sciences}, author={Kamps, Jan A. A. M. and Morselt, Henriëtte W. M. and Swart, Pieter J. and Meijer, Dick K. F. and Scherphof, Gerrit L.}, year={1997}, month=oct, pages={11681–11685} }