Therapeutic and diagnostic use of modified polymeric...

A - Human Necessities – 61 – K

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A61K 47/32 (2006.01) A61K 9/16 (2006.01) A61K 9/50 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) A61K 49/04 (2006.01) A61K 51/12 (2006.01) B01J 13/02 (2006.01) B01J 13/20 (2006.01)

Patent

CA 2140333

2140333 9402106 PCTABS00030 The present invention relates to a highly efficient method of preparing modified microcapsules exhibiting selective targeting. These microcapsules are suitable for encapsulation or surface attachment of therapeutic and diagnostic agents. In one aspect of the invention, surface charge of the polymeric material is altered by conjugation of an amino acid ester to the polymer, providing improved targeting of encapsulated agents to specific tissue cells. Examples include encapsulation of hydrophilic radiodiagnostic agents in 1 µm capsules to provide improved opacification and encapsulation of cytotoxic agents in 100 µm capsules for chemoembolization procedures. The microcapsules are suitable for attachment of a wide range of targeting agents, including antibodies, steroids and drugs, which may be attached to the microcapsule polymer before or after formation of suitably sized microcapsules. The invention also includes hydrophilic microcapsules surface modified with hydroxyl groups. Various agents such as estrone may be attached to the microcapsules and effectively targeted to selected organs.

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