Micromolecular conjugate based on RGD polypeptide-chemotherapy drug and nanometer prodrug system thereof

Abstract

The invention relates to a micromolecular conjugate based on RGD polypeptide-chemotherapy drug and a self-assembly nanometer prodrug system thereof, and belongs to the technical field of biological medicine and nanometer medicine. The nanometer prodrug system has the main advantages that (1) the system is formed by RGD polypeptide and an anti-tumor drug through direct covalent connection via micromolecular connecting arms, and the drug loading capacity of the system is improved; (2) the conjugate is self-assembled into a nanometer prodrug using the drug as a hydrophobic inner core and the RGD polypeptide as a hydrophilic outer shell, the active targeting on tumor cells and tumor new vessels is realized through the ligand-receptor mutual action, and the endocytosis is promoted; (3) the stability of the nanometer prodrug system in the body circulation can be ensured through thioether bonds, reduction sensitive bonds and cathepsin B sensitive bonds, and the cytotoxic drug is released when the nanometer prodrug system reaches the tumor microenvironment; and (4) the micromolecular conjugate instead of a macromolecular material is used as a carrier, so that the nanometer prodrug system can favorably and better penetrate into the tumor tissues and cells to achieve better anti-tumor effects.

Description

A class of small molecule conjugates and nano-prodrug systems based on RGD polypeptide-chemotherapy drugs technical field The invention relates to a class of small molecule conjugates based on RGD polypeptide-chemotherapy drugs and a nano-prodrug system thereof, belonging to the technical field of biomedicine and nano-medicine. The invention provides a composition and preparation method of a small molecular conjugate of RGD polypeptide-chemotherapy drug and its nanometer prodrug system. Background technique Malignant tumor is one of the major diseases that seriously threaten human life and health. According to the statistics of the World Health Organization (WHO), the number of cancer patients is increasing year by year. Nearly 1 million people are diagnosed with cancer every year in the world. However, cancer treatment is still a worldwide problem. In the treatment of cancer, chemotherapy is the main treatment for tumors, especially for advanced tumors. However, the most...

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Problems solved by technology

The object of the present invention is to provide a class of small molecule conjugates based on RGD polypeptide-chemotherapy drugs and its nano-prodrug system (Peptide-drug conjugate nanoparticles, PDCNPs), especially the structure and composition of the anti-tumor nano-prodrug system and its Preparation method to overcome problems in the prior art such as poor biocompatibility of macromolecular targets and carriers, low drug loading, low permeability, etc.

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