Amphiphilic polysaccharide derivative carrier for targeting tumor new blood vessels as well as preparation and application of pharmaceutical composition of amphiphilic polysaccharide derivative carrier

Abstract

The invention relates to an amphiphilic polysaccharide derivative carrier for targeting tumor new blood vessels. According to the derivative, a polysaccharide skeleton is coupled with functional polypeptide targeting E-selectin by virtue of a disulfide bond to ensure that polysaccharide has amphipathy, and is assembled into nano particles for targeting the tumor new blood vessels after carrying an antitumor drug or a tumor new blood vessel inhibitor in an aqueous medium. The nano particles deliver medicines to the tumor new blood vessels in an active targeting manner by virtue of the high affinity between the functional polypeptide targeting the E-selectin and the E-selectin on the surface of the tumor new blood vessels, then a disulfide bond connecting arm can be specifically degraded by a strong reducing environment in endothelial cells of the tumor new blood vessels to cause that the functional polypeptide targeting the E-selectin is separated from polysaccharide, and the medicines are quickly released to treatment target points, so that the concentration of free medicines at tumor new blood vessel parts can be significantly improved and the antitumor curative effect is enhanced. An auxiliary material can be used as a carrier for water-insoluble, indissolvable or amphiphilic antitumor drugs and the tumor new blood vessel inhibitor, and is administrated by injecting into blood vessels or muscles, or is administrated orally or externally. The amphiphilic polysaccharide derivative carrier provided by the invention is simple in preparation method, mature in process and suitable for large-scale production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an amphiphilic polysaccharide derivative targeting neovascularization of tumors as a drug carrier, and also relates to a preparation method and application of the carrier. Background technique [0002] Malignant tumors are an important disease that endangers human health in the world. Although the understanding of tumor cell biology and genetics has reached the level of molecular biology, and new treatment concepts and methods continue to emerge, the overall cure rate of malignant tumors is still low. . American scholar Judah Folkman reported that tumor growth depends on the formation of new blood vessels. During the growth of tumor tissue, new blood vessel formation is often induced, that is, the process of forming new capillaries from existing blood vessels. Studies have shown that the diameter or thickness of the tumor tissue block reaches 1-2mm 3 At this time, if th...

AI Technical Summary

Problems solved by technology

First of all, the tumor blood vessel targeting of the drug is not strong. While acting on tumor blood vessels, it will also have an effect on normal tissues and cells, resulting in serious side effects

Secondly, the drug uptake rate of tumor vascular endothelial cells is low, and the effective therapeutic concentration cannot be maintained locally in tumor blood vessels.

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