Preparation method and application of permeable membrane brush polymer capable of entering cells through hole formation mediated direct translocation mode

Abstract

The invention relates to a preparation method and application of a permeable membrane brush-like polymer capable of entering cells in a hole-mediated direct translocation mode. In order to solve the problem that drug molecules entering cells are bound in vesicles and cannot exert actual functions, permeable membrane brush polymers PTn-R2-C6, PT15-R2-C2 and PT15-R4-C6 rich in arginine are synthesized, and the polymers can enter the cells in a mediated direct translocation mode through holes, so that the problem of binding of the vesicles is fundamentally solved. Through structure-function relationship screening, PTn-R2-C6 can form a mediated non-endocytosis pathway through holes to effectively enter cells. The PTn-R2-C6 shows that the transfection efficiency is higher than that of the PEI 25K, and the cytotoxicity is lower than that of the PEI 25K. The invention of the PTn-R2-C6 polymer provides a valuable platform for efficient and rapid drug delivery in cytoplasm. The preparation method is simple in process, easy to operate, low in cost and easy to popularize and apply.

Description

A transmembrane brush polymer that enters cells by direct translocation mediated by pore formation Preparation method and application of compound technical field The invention belongs to the field of macromolecular biomaterials, and relates to a direct translocation method mediated by pore formation into Preparation method and application of novel arginine-rich transmembrane brush polymers for cells. Background technique [0002] Intracellular transduction of drug molecules is a very important part of drug delivery systems. Biomacromolecules or Hydrophilic Drugs Transmembrane delivery of drugs remains a major challenge. An efficient transport vehicle will meet this challenge at some level. thin Cell penetrating peptides (CPPs) are a class of cationic short peptides that can effectively penetrate the cell membrane And carry biologically active substances into cells. It is generally believed that CPPs can enter cells through one or more pathways, and most In some...

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Problems solved by technology

[0004] The purpose of the present invention is to solve the problem that the existing delivery vectors will cause the drug molecules entering cells to be bound in vesicles, unable to perform actual functions or even be degraded and inactivated, and to provide a direct translocation method mediated by pore formation to enter cells Preparation method and application of novel arginine-rich transmembrane brush polymer

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