The application relates to a polymeric prodrug which comprises a hydrogel, a biologically active moiety and a reversible prodrug linker. The prodrug linker covalently links the hydrogel and the biologically active moiety at a position and the hydrogel has a plurality of pores with openings on the surface of the hydrogel. The diameter of the pores is larger than that of the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety.
The present invention relates to a polymeric prodrug comprising a hydrogel having cross-linkers and a non-biodegradable backbone, a biologically active moiety to be released as drug and a reversible prodrug linker, wherein the prodrug linker covalently links the hydrogel and the biologically active moiety at a position and wherein the prodrug linker is attached to the non-biodegradable backbone of the hydrogel; and the hydrogel has a plurality of pores with openings on the surface of the hydrogel, wherein the diameter of the pores is larger than the biologically active moiety at least at all points of the pore between at least one of the openings and the position of the biologically active moiety and wherein the cross-linkers of the hydrogel further comprise bio-degradable bonds selected from the group of chemically cleavable bonds consisting of phosphate, phosphonate, carbonate, carbamate, disulfide and ester bonds, wherein the number of crosslinks and the halflife of the bio-degradable bonds are adjusted in that almost all drug can be released before a significant amount of release of backbone can take place.
The present invention also relates to respective hydrogels and methods for the manufacture of a mesoporous hydrogel-biologically active moiety conjugate.
This invention relates to polymer particles for solid phase oligonucleotide synthesis. The oligonucleotide may be linked to the particle via a linker having an amide-oligoethyleneglycol-amine structure. The particles may be considered to act as a solid support during the oligonucleotide synthesis. Also disclosed are processes for preparing such polymer particles, compositions and systems comprising such particles, and uses thereof.
Compact Biocompatible Quantum Dots via RAFT-Mediated Synthesis of Imidazole-Based Random Copolymer Ligand
作者:Wenhao Liu、Andrew B. Greytak、Jungmin Lee、Cliff R. Wong、Jongnam Park、Lisa F. Marshall、Wen Jiang、Peter N. Curtin、Alice Y. Ting、Daniel G. Nocera、Dai Fukumura、Rakesh K. Jain、Moungi G. Bawendi
DOI:10.1021/ja908137d
日期:2010.1.20
We present a new class of polymeric ligands for quantum dot (OD) water solubilization to yield biocompatible and derivatizable QDs with compact size (similar to 10-12 nm diameter), high quantum yields (>50%), excellent stability across a large pH range (pH 5-10.5), and low nonspecific binding. To address the fundamental problem of thiol instability in traditional ligand exchange systems, the polymers here employ a stable multidentate imidazole binding motif to the OD surface. The polymers are synthesized via reversible addition-fragmentation chain transfer-mediated polymerization to produce molecular weight controlled monodisperse random copolymers from three types of monomers that feature imidazole groups for CID binding, polyethylene glycol (PEG) groups for water solubilization, and either primary amines or biotin groups for derivatization. The polymer architecture can be tuned by the monomer ratios to yield aqueous QDs with targeted surface functionalities. By incorporating amino-PEG monomers, we demonstrate covalent conjugation of a dye to form a highly efficient QD-dye energy transfer pair as well as covalent conjugation to streptavidin for high-affinity single molecule imaging of biotinylated receptors on live cells with minimal nonspecific binding. The small size and low serum binding of these polymer-coated QDs also allow us to demonstrate their utility for in vivo imaging of the tumor microenvironment in live mice.