Nanoconjugates and nanoconjugate formulations

摘要

The invention provides a drug-polymer nanoconjugate that includes a drug covalently bonded to a polymer. The nanoconjugate can include a block copolymer coating and/or an albumin coating. The drug of the drug-polymer nanoconjugate can be one or more of a variety of therapeutic agents linked to the polymer through ether or thioether linkages formed from hydroxyl or thiol groups of the drug. The albumin coating can substantially or completely retard or prevent aggregation of the nanoconjugates in solid form or in solution. The invention further provides compositions that include a plurality of drug-polymer nanoconjugates, as well as methods for using the drug-polymer nanoconjugates, such as in therapeutic or diagnostic applications.

主权项

1. A drug-polymer nanoconjugate composition comprising drug-polymer nanoconjugate particles having a block copolymer coating, and an albumin coating;
wherein the drug-polymer nanoconjugate particles comprise one or more drugs and one or more polymers, and the one or more drugs of the drug-polymer nanoconjugate particles are individually covalently bonded to initiation points of individual polymers of the drug-polymer nanoconjugate particles through ether or thioether moieties; the one or more polymers of the drug-polymer nanoconjugate particles comprise polyester, polycarbonate, polyphosphate, polysiloxane, polyphosphazane, polypeptide, or amino acid oligomers segments, or a combination thereof; the block copolymer coating comprises PEG and lactide blocks; and the block copolymer coating is coated with an amount of albumin effective to at least substantially prevent aggregation of the drug-polymer nanoconjugate particles when in contact with other drug-polymer nanoconjugates particles, wherein the ratio of the mass of albumin coating to the total mass of the drug-polymer nanoconjugate particles is about 2:1 to about 20:1; and wherein the composition has a diameter of about 2 nm to about 300 nm and a mass of less than 2 wt. % of total drugs that are not covalently bonded to the polymer.