Cedars-Sinai Medical Center

Bong Seop Lee

John S Yu

The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of &#x3b1;-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.

Nanometer-sized prodrugs of NSAIDs

The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.

Antioxidant nanosphere comprising [1,2]-dithiolane moieties

The present invention is directed to antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs and the preparation of nanometer-sized camptothecin prodrugs. Methods of synthesizing the antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant camptothecin nanosphere prodrugs and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these antioxidant camptothecin nanosphere prodrugs for the preparation of delivery devices of other pharmaceuticals and/or drugs. Additionally, methods of treating cancer with the camptothecin and antioxidant derivatives of camptothecin analogs, and nanometer-sized camptothecin prodrugs are also provided.

Antioxidant camptothecin derivatives and antioxidant antineoplastic nanospheres thereof

The present invention describes polymers containing 1,2-dithiolanes capable of acting as scavengers of free radicals, metals and reactive oxygen species. Also described are methods of synthesizing the antioxidant 1,2-dithiolane derivatives and polymerization thereof to produce biodegradable antioxidant polymers. The antioxidant polymers of the present invention may be used to treat diseases or conditions caused by oxidative stress and other free radical mediated conditions. The antioxidant polymers may also be used for the preparation of antioxidant particulate delivery devices of therapeutic agents.

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Torrance, CA, United States of America

Bong Seop Lee