US 2003/0211158 A1 · Microgel particles for the delivery of bioactive materials

Abstract

Novel microgels, microparticles and related polymeric materials capable of delivering bioactive materials to cells for use as vaccines or therapeutic agents. The materials are made using a crosslinker molecule that contains a linkage cleavable under mild acidic conditions. The crosslinker molecule is exemplified by a bisacryloyl acetal crosslinker. The new materials have the common characteristic of being able to degrade by acid hydrolysis under conditions commonly found within the endosomal or lysosomal compartments of cells thereby releasing their payload within the cell. The materials can also be used for the delivery of therapeutics to the acidic regions of tumors and sites of inflammation.

Claims26

Dependent claims

An acid hydrolyzable microgel composition for delivering a bioactive molecule, comprising:

(a) a polymer backbone linked by a crosslinker;
(b) the crosslinker having the formula R2CH(OR1)2, wherein
R1 is a crosslinkable, acid hydrolyzable linkage selected from one of compounds (a)-(f) of FIG. 2;
R2 is Ar—X where X is a water solubilizing group selected from hydrogen, methoxy, —O—(CH2—CH2—O)n—CH3 wherein n is from 1 to 10, —O—CH2—CH2—O—C(O)—O—Ph—NO2 and —O—CH2—CH2—CH2—NH—CO-(dextran polysaccharide), said dextran polysaccharaide having a molecular weight from 300 to 100,000 daltons;
and
Ar is a homocyclic aromatic radical, whether or not fused, having 6 to 12 carbon atoms optionally substituted with one to three substituents;
(c) a particle size between 0.1-10 microns;
and
(d) cross linkages between 1 and 20 mole percent, sufficient to physically trap the bioactive molecule within the microgel.

6 more elements

Dependencies are inferred from the claim text.

Microgel particles for the delivery of bioactive materials

Life of this patent

Microgel particles for the delivery of bioactive materials

Life of this patent

Abstract

Claims26