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Non-linear multiblock copolymer-drug conjugates for the delivery of active agents

  • US 10,159,743 B2
  • Filed: 03/12/2013
  • Issued: 12/25/2018
  • Est. Priority Date: 03/16/2012
  • Status: Active Grant
First Claim
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1. A polymer conjugate defined by the following formula
(A-Xprivate use character ParenclosestmYprivate use character ParenopenstZ)n whereinA is an ophthalmic drug for treatment of the posterior segment of the eye selected from the group consisting of brimonidine, apraclonidine, brinzolamide, acetazolamine, and dorzolamide;

  • Z represents, independently for each occurrence, a hydrophilic polymer segment selected from the group consisting of a poly(ethylene glycol) segment, a poly(propylene glycol) segment, and a copolymer thereof segment;

    Y represents a multivalent branch point that is an organic, inorganic, or organometallic moiety;

    X represents a hydrophobic polymer segment selected from the group consisting of a poly(lactic acid) segment, a poly(glycolic acid) segment, and a poly(lactic-co-glycolic acid) segment; and

    m and n are independently 1, 2, 3, 4, or 5, and m+n is greater than 2.

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