Soluble, degradable poly (ethylene glycol) derivatives for controllable release of bound molecules into solution
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United States of America Patent
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Feb 4, 2003
Grant Date -
Sep 13, 2001
app pub date -
Apr 2, 2001
filing date -
Sep 26, 1996
priority date (Note) -
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Abstract
PEG and related polymer derivatives having weak, hydrolytically unstable linkages near the reactive end of the polymer are provided for conjugation to drugs, including proteins, enzymes, small molecules, and others. These derivatives provide a sufficient circulation period for a drug-PEG conjugate and then for hydrolytic breakdown of the conjugate and release of the bound molecule. In some cases, drugs that previously had reduced activity when permanently coupled to PEG can have therapeutically suitable activity when coupled to a degradable PEG in accordance with the invention. The PEG of the invention can be used to impart water solubility, size, slow rate of kidney clearance, and reduced immunogenicity to the conjugate. Controlled hydrolytic release of the bound molecule in the aqueous environment can then enhance the drug delivery system.
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