title: Kupffer cell depletion by liposome-delivered drugs: comparative activity of intracellular clodronate, propamidine, and ethylenediaminetetraacetic acid.
abstract: Macrophages such as Kupffer cells in the liver are multifunctional cells. They are involved in host defense mechanisms and have a regulatory role in many biomedical processes. Their selective depletion, using liposome-encapsulated drugs, forms a widely accepted approach to studying their functional aspects in vivo. We have compared the Kupffer cell-depleting activities of liposome-encapsulated clodronate, propamidine, and ethylenediaminetetraacetic acid (EDTA) for this purpose. These molecules represent the drug families of bisphosphonates, diamidines (or aromatic polyamidines), and polyaminopolycarboxylic acid-chelating agents, respectively. The Kupffer cell-depleting activity of the liposome-encapsulated antimicrobial drug propamidine exceeded that of clodronate by about a factor of 10. EDTA appeared to be inefficacious for depletion of Kupffer cells in the rat.
authors.affiliation: Department of Cell Biology and Immunology, Faculty of Medicine, Vrije Universiteit Van der Boechorststraat 7, Amsterdam, The Netherlands.
authors.forename: N
authors.initials: N
authors.lastname: Van Rooijen
authors.forename: A
authors.initials: A
authors.lastname: Sanders
mesh_terms: D000818:Animals; D001550:Benzamidines / Q000008:administration & dosage / Q000494:pharmacology*; D002469:Cell Separation; D004002:Clodronic Acid / Q000008:administration & dosage / Q000494:pharmacology*; D004337:Drug Carriers; D004492:Edetic Acid / Q000008:administration & dosage / Q000494:pharmacology*; D007728:Kupffer Cells / Q000166:cytology / Q000187:drug effects*; D008081:Liposomes; D008099:Liver / Q000166:cytology / Q000187:drug effects*; D008297:Male; D051381:Rats; D011922:Rats, Mutant Strains
chemical_list: D001550:Benzamidines; D004337:Drug Carriers; D008081:Liposomes; D004002:Clodronic Acid; D004492:Edetic Acid; C005555:propamidine