CPC A61K 39/001 (2013.01) [A61K 38/28 (2013.01); A61K 38/38 (2013.01); A61K 39/0002 (2013.01); A61K 39/0005 (2013.01); A61K 39/35 (2013.01); A61K 39/385 (2013.01); A61K 47/549 (2017.08); A61K 47/555 (2017.08); A61K 38/00 (2013.01); A61K 2039/555 (2013.01); A61K 2039/577 (2013.01); A61K 2039/60 (2013.01); A61K 2039/6093 (2013.01); A61K 2039/627 (2013.01); C07K 2319/01 (2013.01)] | 20 Claims |
1. A composition for the induction of antigen-specific immune tolerance in a subject, the composition comprising:
an antigen to which tolerance is desired;
wherein the antigen to which tolerance is desired is capable of inducing an unwanted immune response in the subject;
a polymeric linker;
wherein the polymeric linker is coupled to the antigen to which tolerance is desired via a disulfide bond or a disulfanyl ethyl ester;
wherein the disulfide bond or the disulfanyl ethyl ester are each configured to be cleaved after administration of the composition to the subject and to release the antigen to which tolerance is desired from the polymeric linker;
a liver-targeting moiety;
wherein the polymeric linker comprises the following structure:
where
the right bracket “)” indicates a bond between the linker and a corresponding reversible addition-fragmentation chain transfer (RAFT) polymerization agent;
the bottom bracket “” indicates a bond between the linker and the liver targeting moiety;
Y′ comprises a remaining portion of the polymeric linker:
n is an integer from 1 to 100;
p is an integer from 2 to 150;
R9 comprises —C(O)—NH—CH2—CH2—;
the left bracket “(” indicates the bond between the antigen and linker;
the bottom bracket “” indicates the bond between the linker and the liver targeting moiety; and
wherein the liver-targeting moiety comprises a galactosylating moiety or glucosylating moiety.
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