EGFRTargeted Liposomes

Acridine is a WS, DNA-intercalator. Its boronated derivative WSA was incorporated into liposomes composed of EGF-conjugated lipids. Their surface contained approximately 5 mol% PEG and 10-15 molecules of EGF, and 104-105 of WSA molecules were encapsulated. These liposomes had EGFR-specific cellular binding to cultured human glioma cells130,140 and were internalized following specific binding to the receptor. Following internalization, WSA primarily was localized in the cytoplasm, and had high cellular retention with 80% of the boron remaining cell-associated after 48 h.141

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