SSTR-TARGETED CONJUGATES ENCAPSULATED IN PARTICLES AND FORMULATIONS THEREOF

摘要

Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.

主权项

1. A polymeric controlled release nanoparticle comprising a conjugate of a chemotherapeutic agent bound via a linker to a targeting moiety, said targeting moiety binds to cells of solid tumors to which the chemotherapeutic agent is to be delivered, wherein the polymeric nanoparticle is synthesized as a solid polymeric nanoparticle having a diameter of between about 10 nm to about 500 nm and wherein the conjugate is distributed in the solid polymeric nanoparticle and wherein, upon administration, the solid nanoparticle preferentially accumulates at sites of said solid tumors.