Dual-Action Polymer Nanocarriers That Release a COX Inhibitor While Co-Delivering a Second Therapeutic
This invention is an amphiphilic polymer that carries a COX-inhibitor drug as a releasable side group and binds a second therapeutic agent through ionic interaction. It delivers two drugs together in a single, nano-sized carrier, which makes it a promising platform for combination therapy.
Description
Unmet Need - Small-molecule drugs and COX inhibitors are often limited by poor solubility and the high doses needed for efficacy, and this technology addresses that by co-delivering a COX inhibitor and a second drug in one carrier.The polymer has a water-repelling (hydrophobic) backbone with two kinds of side groups. The first kind carries a COX-inhibitor drug attached through a bond that breaks inside the body, so the polymer acts as a prodrug that releases the active COX inhibitor. This group also contains a chemical feature that interacts ionically (through opposite electrical charges) with a second therapeutic compound. The second kind of side group is a water-loving (hydrophilic) polymer, which gives the polymer both water-loving and water-repelling character.
Because of this design, multiple polymer chains can come together to form tiny micelles. These are nano-sized spheres that can hold the second drug, and the micelles can be under 100 nm in diameter. The release bond can be tuned to respond to specific conditions in the body, such as reductive, pH, ROS, hypoxia or protease-sensitive environments. An optional third side group, such as folate, can steer the carrier toward a region of interest in vivo.
Applications
- Combination cancer therapy platforms pairing a COX inhibitor with chemotherapeutic or targeted agents- Targeted delivery systems for tumors, using folate or other targeting groups
- Nanocarrier formulations for small-molecule drugs (under about 1.5 kDa) that are hard to formulate
- Delivery of anti-inflammatory, antiviral, antibiotic, antifungal or immunomodulating compounds
- Co-delivery systems for COX-inhibitor drugs such as 5-aminosalicylic acid, diclofenac and sulfasalazine
Advantages
- Delivers two different therapeutic compounds from a single carrier- Releases the COX inhibitor in vivo through a bond designed to cleave under chosen biological conditions
- Binds the second drug through ionic interaction, which supports loading of small-molecule therapeutics
- Forms micelles under 100 nm in diameter, a size range suited to systemic delivery
- Can include a targeting group such as folate to direct the carrier to a region of interest in vivo