ROS and esterase dual-responsive nano-preparation, and preparation method and application thereof

Abstract

This invention relates to a ROS- and esterase-responsive nano-formulation, its preparation method, and its application, belonging to the field of nano-formulation technology. The nano-formulation of this invention uses itaconic acid as a hyperbranched polymer backbone after modification. Upon reaching the inflammatory site, the hyperbranched polymer first disintegrates in response to ROS stimulation, and then releases the active pharmaceutical ingredient of itaconic acid under the further action of esterases. This significantly improves the cell membrane permeability and bioavailability of exogenous itaconic acid. Secondly, compared with nano-formulations encapsulating therapeutic agents, the nano-formulation of this invention has an almost pure drug core, thus exhibiting higher drug loading capacity and lower toxicity. Furthermore, by using the therapeutic agent as the nanocarrier backbone, the nano-formulation of this invention effectively avoids premature leakage of the therapeutic agent and the problem of clearing foreign substances after the parent drug is released.

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