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Target-selective drug delivery remains a challenge
for various therapeutic applications and particularly
for cancer. Current targeting strategies include formulation
and encapsulation for preferential release in the acidic
tumor environment as well as covalent conjugation via
linkers sensitive to pH, to oxygen levels or to disease-specific
enzymes. These approaches have been limited by:
- stringent requirements on linkable drugs and carriers
- inflexible rates of release and
- insufficient target/tumor-specificity of relevant
enzymes.
A new class of linkers has been developed to address
these limitations. These linkers:
- undergo controlled hydrolysis at physiological
temperature and in mild aqueous, acidic environments,
- can be tuned to hydrolyze with half-lives from 30
minutes to greater than 9 months,
- accommodate a wide range of biocompatible drug
carriers and
- flexibly conjugate to a wide variety of drugs (via
alcohol, amine or imidazole).
These features should prove extremely relevant for
clinical applications, from cancer to ophthalmology,
where increased efficacy and reduce drug toxicity can
enhance the therapeutic profile and/or extend patent
life for promising and useful drugs.
Related Information:
- http://yangserver.ucsd.edu/
- Bioconjugate Chemistry 2007, 18, 293-29
Pending International Application Number:
WO/2007/114946
Case No: SD2006-140
Keywords: tumor, selective delivery,
targeted, targeted delivery, carrier, linker, cancer,
ophthalmology, macular degeneration, retinopathy, sustained
release, controlled release
Inquiries To: invent@ucsd.edu
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