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N-acyl phosphatidylethanolamine-mediated liposomal drug delivery

  • US 6,294,191 B1
  • Filed: 01/19/2000
  • Issued: 09/25/2001
  • Est. Priority Date: 10/15/1996
  • Status: Expired due to Fees
First Claim
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1. A pharmaceutical composition comprising:

  • (a) a pharmaceutically acceptable carrier; and

    (b) a liposome having a lipid component which comprises;

    (i) an N-acyl phosphatidylethanolamine (NAPE) having the formula;

    (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, at least one of n2, n4, n6 and n8 is equal to 1;

    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;

    the lipid component comprises a destabilization-effective amount of the N-acyl phosphatidylethanolamine of at least about 25 mole %;

    wherein the liposome is multilamellar or is a large unilamellar liposome wherein the destabilization-effective amount of the NAPE is that amount of NAPE which renders the liposome fusogenic when the liposome is admixed with a target, in the presence of divalent cations or at a pH of about 4.9 to about 6.0.

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