| 摘要 |
A pharmaceutical composition comprising a liposome having a lipid component which comprises: (i) an N-acyl phosphatidylethanolamine having the formula: CH2-O-R1 ]CH-O-R2 ]CH2-O-P(O)2-O-CH2CH2NH-R3 ; and, (ii) an additional lipid wherein: each of R1, R2 and R3 is independently a group having the formula: C(O)(CH2)n1(CH=CH)n2(CH2)n3(CH=CH)n4(CH2)n5(CH=CH)n6(CH2)n7(CH=CH)n8(CH2)n9CH3; n1 is zero or an integer equal to from 1 to 22; n3 is zero or an integer equal to from 1 to 19; n5 is zero or an integer equal to from 1 to 16; n7 is zero or an integer equal to from 1 to 13; n9 is zero or an integer equal to from 1 to 10; for each of R1 and R2 independently the sum of n1 + 2n2 + n3 + 2n4 + n5 + 2n6 + n7 + 2n8 + n9 is an integer equal to from 12 to 22; for R3 the sum of n1 + 2n2 + n3 + 2n4 + n5 + 2n6 + n7 + 2n8 + n9 is an integer equal to from 2 to 22; each of n2, n4, n6 and n8 is independently equal to 0 or 1; at least one of n2, n4, n6 and n8 is equal to 1; the lipid component comprises a destabilization-effective amount of the N-acyl phosphatidylethanolamine of at least about 25 mole%; and, the liposome is a multilamellar or is a large unilamellar liposome. The use of the composition in the manufacture of a medicament for localised delivery of a bioactive agent to a target cell is also provided. |
