Targeted drug delivery: a two-compartment growth inhibition assay demonstrates that fluorodeoxyuridine and fluorodeoxyuridine monophosphate are liposome-independent drugs.
The targeted delivery to cells by liposomes and leakage under delivery conditions of fluorodeoxyuridine (FdUR) and fluorodeoxyuridine monophosphate (FdUMP) have been evaluated using a two-compartment growth inhibition assay. Under cell culture conditions, FdUR leaks 100% from all liposomes regardless of charge or phase transition temperature. Under the same conditions, FdUMP leaks 100% from egg yolk phosphatidylglycerol liposomes, 47% from distearoylphosphatidylglycerol liposomes, 44% from egg yolk phosphatidylcholine liposomes, and 10% from distearoylphosphatidylcholine liposomes. All liposomes were prepared from a 67:33 mixture of phospholipid and cholesterol. The two-compartment assay demonstrates directly that neither of these drugs is delivered selectively to the target cells by the liposomes, suggesting that they are liposome independent drugs.
Heath
T D
TD
University of Wisconsin, School of Pharmacy, Madison.
Brown
C S
CS
D001702:Biopharmaceutics; D003856:Deoxyuracil Nucleotides / Q000493:pharmacokinetics*; D004337:Drug Carriers; D005467:Floxuridine / Q000493:pharmacokinetics*; D005468:Fluorodeoxyuridylate / Q000493:pharmacokinetics*; D008081:Liposomes
D003856:Deoxyuracil Nucleotides; D004337:Drug Carriers; D008081:Liposomes; D005467:Floxuridine; D005468:Fluorodeoxyuridylate