Method and Technology of Production of Echogenic Microbubbles Combining Properties of Drug Carriers and Ultrasound Contrast Agents

In the present invention, echogenic drug-loaded microbubbles are generated from stable micro- or nanoemulsions of perfluorocarbon upon injection into the body. This invention enables users to control the size of the emulsion droplets and bubbles by changing the concentration of a perfluorocarbon and a type and composition of the diblock copolymer, and allows drug loading and microemulsion formation to proceed in the same step. Upon injection of a mixture of drug-loaded micelles and microemulsion in the body, echogenic microbubbles are produced at the body temperature. In addition, the technique allows precise positioning of the syringe needle in the tumor volume, direct intratumoral injection of encapsulated drug, and acoustic activation of the intracellular drug uptake by the tumor cells triggered by external ultrasonic irradiation. Moreover, this mode of chemotherapy can substantially reduce side effects, allow long residence time of the encapsulated drugs in the tumor volume, increase efficacy, and reduce therapeutic drug doses.

This invention provides methods of generating microbubbles that have properties of drug carriers and ultrasound contrast agents. This technique can be applied in advanced chemotherapy, especially of poorly vascularized tumors for which the direct intratumoral drug injection is the only feasible treatment. It is also beneficial for treating well delineated primary lesions, e.g., colorectal, breast, prostate, and stomach cancers. In addition, depending on the size, stability, and injection mode of in situ generated microbubbles, the invention may also be used as blood pool ultrasound contrast agents and for enhanced ultrasound treatment of vascular thrombosis.

Stage of Development
A PCT provisional patent application is pending.
This technology is available for developmental research support or licensing under either exclusive or non-exclusive terms.

Additional Info

Inventor(s): Zhonggao Gao, Natalya Rapoport

Type of Offer: Licensing

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