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Physical trapping type polymeric micelle drug preparation

  • US 5,510,103 A
  • Filed: 06/05/1995
  • Issued: 04/23/1996
  • Est. Priority Date: 08/14/1992
  • Status: Expired due to Term
First Claim
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1. A method for trapping hydrophobic drugs, which comprises heating, ultrasonication or organic solvent treatment of a hydrophobic drug and a drug carder comprised of a block copolymer of formula I, or II to physically trap said hydrophobic drug in polymeric micelles composed of said drug carrier, wherein formula I and II are represented:

  • ##STR7## wherein;

    R1 is selected from the group consisting of H and methyl;

    R2 is selected from the group consisting of NH, CO and R6 (CH2)q R7 whereR6 is selected from the group consisting of -OC(O)-, -OC(O)N(H)-, -N(H)C(O)-, -N(H)C(O)O-, -N(H)C(O)N(H)-, -C(O)N(H)- and -C(O)O-;

    R7 is NH or CO; and

    q is 1-6;

    R3 is selected from the group consisting of H, -CH3, -CH2 CO2 H, -CH2 CH2 CO2 H, -CH2 CO2 CH2 .O slashed., -CH2 CH2 CO2 CH2 .O slashed., -CH2 CH(CH3)CH3, -CH(CH3)CH2 CH3, -CH(CH3)2, -CH2 .O slashed., -(CH2)P C6 H5, -(CH2)P COOR5 and -CH2 C(O)N(H)R5 ;

    wherep is 1 or 2;

    R5 is selected from the group consisting of benzyl and C1 -C20 alkyl group, said C1 -C20 alkyl group being optionally substituted with a benzyl group; and

    R4 is selected from the group consisting of H, -OH, -C(O)-alkyl, -N(H)-alkyl and -O-alkyl, wherein said alkyl is a C1 -C20 alkyl group;

    m=4-2500; and

    n=2-300.

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