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5‐Fluoroorotate: a new liposome‐dependent cytotoxic agent
Author(s) -
Heath Timothy D.,
Lopez Ninfa G.,
Stem Walter H.,
Papahadjopoulos Demetrios
Publication year - 1985
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(85)81217-5
Subject(s) - liposome , chemistry , potency , drug delivery , cytotoxicity , cholesterol , cytotoxic t cell , pharmacology , biophysics , biochemistry , in vitro , biology , organic chemistry
The potency of 5‐fluoroorotate for inhibition of L929 or CV1‐P cell growth is increased by encapsulation in negatively charged liposomes. The optimal liposome composition is dipalmitoylphosphatidylglycerol: cholesterol, 67:33. Unextruded large unilamellar liposomes are the optimal size for delivery. This compound is the second transport‐negative drug which we have found to exhibit liposome‐dependent delivery.