Decorated macromolecular scaffolds

摘要

The present invention relates to a method for preparing decorated macromolecular scaffolds. The method of the invention is useful for the generation of bioactive nanoparticles for use in clinical applications. Such applications include drag and gene delivery, tumour targeting, bioimaging, tissue remodelling, generation of antiviral products and vaccines delivery.

主权项

1. A method for preparing a decorated macromolecular scaffold comprising the step of reacting the surface groups of a macromolecular scaffold with ligands to form oxime or hydrazone bonds between the surface groups of the macromolecular scaffold and the ligands, wherein the reaction is carried out in the presence of an aniline or substituted aniline catalyst and
(i) the surface groups on the macromolecular scaffold comprise groups -E1-L1; and (ii) the ligands each comprise group -E2-L2; wherein E1 and E2 are independently each optional linkers; wherein one of -L1 or -L2 is —C(O)—Z1—C(O)R1 and the other of -L1 and -L2 is —C(O)—Z2—X—NH2; wherein Z1 is selected from (CH2)nor wherein Z2 is selected from (CH2)n,  or —NH—NHC(O)—; n is 0, 1, 2 or 3; R1 is H or CH3;
X is NH or O; andwherein -L1 and -L2 react to form —C(O)—Z1—C(R1)═N—X—Z2—C(O)—; and further comprising the step of(iii) reacting a macromolecular scaffold to introduce group -E1-L1; and/or(iv) reacting ligands to introduce groups -E2-L2; wherein step (iii) comprises reacting a macromolecular scaffold with and step (iv) comprises reacting ligands with