High-molecular polymer for treating tumors and preparation method and application thereof

Abstract

The invention relates to a high-molecular polymer for treating tumors and a preparation method and application thereof, and belongs to the technical field of medicines. The preparation method comprises the following steps: synthesizing PEGMA-(RAFT); synthesizing PEGMA-b-PDPA-(RAFT); synthesizing PEGMA-b-PDPA-b-PDMAEMA-(RAFT); desulfurization reaction; and synthesizing the high-molecular polymer ma< 1 >-PMDM. The invention also discloses the high-molecular polymer prepared by the preparation method and used for treating tumors and application of the high-molecular polymer. According to the preparation method, the high-molecular polymer for treating tumors can be prepared very efficiently; the high-molecular polymer can improve the stability of the carrier, improve the cellular uptake capacity and improve the transfection capacity, the composition and the structure of the carrier have the capacity of overcoming the lysosome biological barrier, and the high-molecular polymer can be applied to a targeting drug carrier for treating tumors.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a high molecular polymer for treating tumors, a preparation method and application thereof. Background technique [0002] It was first reported in 1998 that the suppression of specific gene expression caused by double-stranded RNA (dsRNA) is called RNA interference (RNA interference, RNAi). This opened the prelude to small interfering siRNA (small interfering RNA, or short interfering RNAs, siRNA) research, especially in 2004, the first case of reagents based on siRNA entered clinical trials, which undoubtedly brought a new era to the development of siRNA. A new drive and hope. Since the use of RNAi technology can specifically knock out or shut down the expression of specific genes, small interfering siRNA has been widely used in the exploration of gene function and the treatment of infectious diseases and malignant tumors. [0003] When small interfering siRNA is...

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Problems solved by technology

[0005] However, for the current polymer nano-gene carrier, after the polymer is loaded with siRNA to form the gene carrier, after endocytosis into the cell, it is difficult to escape from the endosome and lysosome on the one hand and there is a risk of being degraded by RNase. On the other hand, endosomes or lysosomes containing gene carrier are easily transformed into vesicles, which are excreted through efflux, resulting in a low effective concentration of siRNA in cells, which is a key problem to be solved in siRNA delivery.

Another concern is that due to the heterogeneity of tumor tissue and high interstitial pressure, nanocarriers in tumor tissue tend to stay near blood vessels, making it difficult to penetrate deep into tumor tissue.

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