Patent ID: 7629003

Claim:
A method of intracellular delivery into tumor cells of taxol or a camptothecin derivative of formula wherein: R 7 is a —C(R 11 )═N—O (n) R 10 group, wherein R 10 is hydrogen or a C 1 -C 5 alkyl or C 2 -C 5 alkenyl group, linear or branched or C 3 -C 10 cycloalkyl, group or a linear or branched (C 3 -C 10 ) cycloalkyl-(C 1 -C 5 ) alkyl group, or C 6 -C 14 aryl, or a linear or branched (C 6 -C 14 ) aryl-(C 1 -C 5 ) alkyl group, or a heterocyclic or linear or branched heterocyclo-(C 1 -C 5 ) alkyl group, said heterocyclic group containing at least a heteroatom selected from the group consisting of nitrogen atom, optionally substituted with a (C 1 -C 5 ) alkyl group, and/or oxygen and/or sulfur; said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aryl-alkyl, heterocyclic or heterocyclo-alkyl groups, being optionally substituted with other groups selected from the group consisting of: halogen, hydroxy, C 1 -C 5 alkyl, C 1 -C 5 alkoxy, phenyl, cyano, nitro, —NR 12 R 13 , wherein R 12 and R 13 , which may be the same or different, are hydrogen, linear or branched (C 1 -C 5 ) alkyl; a pharmaceutically acceptable ester of the —COOH group; or the —CONR 14 R 15 group, wherein R 14 and R 15 , which may be the same or different, are hydrogen or linear or branched (C 1 -C 5 ) alkyl; or R 10 is a (C 6 -C 10 ) aroyl residue optionally substituted by one or more groups selected from the group consisting of: halogen, hydroxy, linear or branched (C 1 -C 5 ) alkyl, C 1 -C 5 alkoxy, phenyl, cyano, nitro, —NR 16 R 17 , wherein R 16 and R 17 , which may be the same or different, is hydrogen, linear or branched (C 1 -C 8 ) alkyl; n is the number 0 or 1; R 11 is hydrogen, linear or branched C 1 -C 5 alkyl, linear or branched C 2 -C 5 alkenyl, C 3 -C 10 cycloalkyl, (C 3 -C 10 ) cycloalkyl-linear or branched (C 1 -C 5 ) alkyl, C 6 -C 14 aryl, (C 6 -C 14 ) aryl-linear or branched alkyl (C 1 -C 5 ); R 8 and R 9 , which may be the same or different are hydrogen, hydroxy, linear or branched C 1 -C 5 alkoxy; their N 1 -oxides, their single isomers, in particular the syn and anti isomers of the —C(R 11 )═N—O (n) R 10 group, their enantiomers, diastereoisomers and admixtures, the pharmaceutically acceptable salts thereof; using a liposome comprising a compound of formula (II) where: R 3 is an acyl chain selected from the group consisting of palmitoyl and stearoyl; R 4 is undecyl; the molar ratio between the compound of the formula (II) and the taxol or the camptothecin is 40:1; and X − is the anion of a pharmacologically acceptable acid.