主权项 |
1. A nucleic acid delivery composition for delivering a nucleic acid to a target cell or tissue, comprising: a block copolymer having an uncharged hydrophilic polymer segment and a cationic polymer segment; a second cationic polymer; and a nucleic acid,
wherein the uncharged hydrophilic polymer segment of the block copolymer is a polyalkylene glycol segment, the cationic polymer segment of the block copolymer is a segment made of poly(amino acid) having amino groups at its side chains, and the second cationic polymer is poly(amino acid) having amino groups at its side chains, wherein the mol percentage (B/H ratio) of the cationic groups of the block copolymer to the total cationic groups of the block copolymer and the second cationic polymer is between 25% and 90%, wherein said block copolymer is selected from the group consisting of formulae (I) to (IV): wherein, in formulae (I) and (II), R1 represents a hydrogen atom or unsubstituted or substituted, linear or branched C1-12 alkyl group, R2 represents a methylene group or ethylene group, R3 represents a hydrogen atom, protecting group, hydrophobic group or polymerizable group, R4 is either the same as R5 or represents an initiator residue, R5 respectively and independently represent a hydroxyl group, oxybenzyl group or —NH—(CH2)a—X group, X respectively and independently represents a bulky amine compound residue having a pKa value of 7.4 or less, an amine compound residue containing one type or two or more types of a primary, secondary, tertiary or quaternary amine, or a non-amine compound residue, L1 and L2 respectively and independently represent a linking group, a represents an integer of 1 to 5, m represents an integer of 5 to 20,000, n represents an integer of 2 to 5,000, and x represents an integer of 0 to 5,000, provided that x is not greater than n; wherein, in formulae (III) and (IV), R1 represents a hydrogen atom or unsubstituted or substituted, linear or branched C1-12 alkyl group, R2 represents a methylene group or ethylene group, R3 represents a hydrogen atom, protecting group, hydrophobic group or polymerizable group, R4 is either the same as R5 or represents an initiator residue, R5 respectively and independently represent a hydroxyl group, oxybenzyl group or —NH—(CH2)a—X group, provided that 85% or more of R5 are —NH—(CH2)a—X groups, X respectively and independently represents a bulky amine compound residue having a pKa value of 7.4 or less, an amine compound residue containing one type or two or more types of a primary, secondary, tertiary or quaternary amine, or a non-amine compound residue, L1 and L2 respectively and independently represent a linking group, a represents an integer of 1 to 5, R6 respectively and independently represents a hydrogen atom or protecting group, m represents an integer of 5 to 20,000, n represents an integer of 2 to 5,000, y represents an integer of 0 to 5,000 and z represents an integer of 0 to 5,000, provided that y+z is not greater than n; and wherein said second cationic polymer is selected from the group consisting of formulae (I′) to (IV′): wherein, in formulae (I′) and (II′), R2, R3, R4, R5, n and x have the same meanings as defined in formulae (I) and (II); wherein, in formulae (III′) and (IV′), R2, R3, R4, R5, R6, n, x, y and z have the same meanings as defined in formulae (III) and (IV). |