Dendritic high-molecular-weight polymer drug carriers and their conjugates with drugs especially for treatment of solid tumours

摘要

The present invention relates to water-soluble high-molecular-weight polymer drug carriers and their conjugates with drugs, derived from dendrimers of the amidoamine and 2,2-bis(hydroxymethyl)propanoic types, the amino and hydroxy end groups of which are attached to semitelechelic copolymers of N-(2 hydroxypropyl)methacrylamide (HPMA) through biodegradable spacers. The polymer carriers and conjugates enable targeted transport notably of anticancer drugs into solid tumors in which biodegradation, the associated controlled drug release and subsequent elimination of polymer carrier from the organism are provided. The polymer carrier conjugated with a cancerostatic for use in targeted therapy of human tumors.

主权项

1. A dendritic high-molecular-weight polymer drug carrier characterized in that it consists of a central dendritic part of zero to sixth generation of dendrimer selected from the group consisting of amidoamine- and 2,2-bis(hydroxymethyl)propanoic units, the amino or hydroxy end groups of which are grafted with semitelechelic copolymers of N-(2-hydroxypropyl) methacrylamide (HPMA) through amide or ester bond and biodegradable spacers.