Abstract
Liposomes are of interest as drug delivery tools for therapy of cancer and infectious diseases. We investigated conjugation of epidermal growth factor, EGF, to liposomes using the micelle-transfer method. EGF was conjugated to the distal end of PEG-DSPE lipid molecules in a micellar solution and the EGF-PEG-DSPE lipids were then transferred to preformed liposomes, either empty or containing the DNA-binding compound, water soluble acridine, WSA. We found that the optimal transfer conditions were a 1-h incubation at 60 degrees C. The final conjugate, (125)I-EGF-liposome-WSA, contained approximately 5 mol % PEG, 10-15 EGF molecules at the liposome surface, and 10(4) to 10(5) encapsulated WSA molecules could be loaded. The conjugate was shown to have EGF-receptor-specific cellular binding in cultured human glioma cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Acridines / chemistry
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Acridines / therapeutic use
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Animals
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Boron Compounds / chemistry
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Boron Compounds / therapeutic use
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Boron Neutron Capture Therapy / methods*
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Drug Delivery Systems / methods*
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Drug Stability
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Epidermal Growth Factor / metabolism*
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Epidermal Growth Factor / therapeutic use
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Glioma / chemistry
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Glioma / pathology
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Humans
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Intercalating Agents / chemistry
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Intercalating Agents / therapeutic use
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Liposomes / chemistry
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Liposomes / therapeutic use
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Mice
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Neoplasm Proteins / metabolism
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Phosphatidylethanolamines / chemistry
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Phosphatidylethanolamines / therapeutic use
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Polyethylene Glycols / chemistry
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Polyethylene Glycols / therapeutic use
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Radioligand Assay
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Sensitivity and Specificity
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Tumor Cells, Cultured
Substances
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Acridines
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Boron Compounds
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Intercalating Agents
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Liposomes
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Neoplasm Proteins
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Phosphatidylethanolamines
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polyethylene glycol-distearoylphosphatidylethanolamine
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Polyethylene Glycols
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Epidermal Growth Factor