<> "The repository administrator has not yet configured an RDF license."^^ . <> . . . "Receptor-mediated endocytosis of macromolecular conjugates in selective drug delivery."^^ . "In the present investigation we have described a method of enhancing the uptake of methotrexate by macrophages. This enhanced uptake was mediated by endocytosis through the \"scavenger receptor\" system which recognized maleylated bovine serum albumin. Experimental evidence showed that macrophages internalized methotrexate coupled to maleylated bovine serum albumin through a saturable process at 37OC leading to an eightfold higher concentration of cell-associated methotrexate compared to the free drug. Following uptake, the drug conjugate\r\nwas degraded in the lysosomes leading to intracellular release of a pharmacologically active form\r\nof methotrexate. When administered to macrophages infected with Leishmania mexicana amazonensis,\r\nthe drug conjugate could eliminate the intracellular amastigotes more efficiently than\r\nthe free drug. The leishmanicidal effect of the drug conjugate was inhibited in the presence of\r\nexcess maleylated bovine serum albumin and lysosomal inhibitors such as chloroquine and\r\nmonensin. Addition of folinic acid to the medium also prevented the elimination ofthe amastigotes\r\nby the drug conjugate. These results suggested that the scavenger receptor-mediated endocytosis\r\nof the drug conjugate led to enhanced transport and intracellular release of a pharmacologically\r\nactive form of methotrexate resulting in more efficient killing of the amastigotes compared\r\nto the free drug. This modality ofdelivering drugs selectively to macrophages might have\r\nutility in the chemotherapy of macrophage-associated disorders in general."^^ . "1990-11-01" . . "40" . "9" . . "Portland Press Ltd."^^ . . . "Biochemical pharmacology"^^ . . . "00062952" . . . . . . . "S K"^^ . "Basu"^^ . "S K Basu"^^ . . . . . . "Receptor-mediated endocytosis of macromolecular conjugates in selective drug delivery. (PDF)"^^ . . . . "HTML Summary of #430 \n\nReceptor-mediated endocytosis of macromolecular conjugates in selective drug delivery.\n\n" . "text/html" . . . "QD Chemistry"@en . .