Abstract
Abstract The stability of small unilamellar vesicles (SUV) formed by egg phosphatidylcholine has been examined in the presence of four DNA-intercalating drugs—carboxamides of acridine, anthracene, phenylquinoline, and phenylbenzimidazole. The physicochemical stability of the vesicle-membrane changed as the total drug concentration increased and, of the four drugs investigated, the phenylquinolinecarboxamide was the most destructive. The presence of cholesterol in the liposomal bilayer increased resistance to physicochemically induced damage by the drugs except the anthracenecarboxamide. In all cases, coating the liposomes with a polysaccharide made the liposomal surface more hydrophobic and led to the vesicle rupture by the cytotoxic agents. The cytotoxic 9-anilinoacridine derivatives, amsacrine and 9-[2-methoxy-4-(methylsulfonylamino)anilino]-5-methylacridine-4-N-methylcarboxamide (CI-921), were too insoluble to be encapsulated within the aqueous core of liposomes, but the neutral form of CI-921 was intercalated into the liposomal membrane of pullulan-derivative-coated liposomes. In this formulation, CI-921 was more effective against BM 314 carcinoma-cells than the free drug, but an anticarcinoembrionic antigen (anti-CEA) antibody binding liposome provided no additional advantage.
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