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Enhanced intracellular delivery of doxorubicin by scavenger receptor‐mediated endocytosis for preferential killing of histiocytic lymphoma cells in culture
Author(s) -
Basu Sunanda,
Mukhopadhyay Bratati,
Basu Sandip K.,
Mukhopadhyay Amitabha
Publication year - 1994
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(94)80511-3
Subject(s) - endocytosis , intracellular , doxorubicin , cytotoxicity , scavenger receptor , conjugate , chemistry , u937 cell , receptor mediated endocytosis , cell culture , pharmacology , drug delivery , drug , biochemistry , receptor , biology , apoptosis , chemotherapy , in vitro , lipoprotein , mathematical analysis , mathematics , organic chemistry , cholesterol , genetics
A conjugate of the antineoplastic drug doxorubicin (DXR) with maleylated bovine serum albumin (MBSA) was taken up by a human histiocytic lymphoma cell line (U937) through the high efficiency process of scavenger receptor‐mediated endocytosis resulting in a sixfold higher intracellular concentration of the drug compared to that obtained when the free drug was administered. Compared to the free drug, the drug conjugate showed significantly higher cytotoxicity towards U937 cells presumably because of intracellular availability of a pharmacologically active form of the drug. The intracellular product released after lysosomal degradation of the drug conjugate was chromatographically identical to free DXR. These findings merit serious consideration in the development of new chemotherapeutic agents for the treatment of histiocytic malignancies.