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Degradable polymer with pH sensitivity of tumor tissues and preparation method for degradable polymer and application of degradable polymer

A technology for degrading polymers and tumor tissues, which is applied in the field of degradable polymers, can solve the problems of small adjustable range of pKa value, and achieve the effects of reducing treatment costs, large drug loading, and less drug resistance

Inactive Publication Date: 2015-11-04
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Relatively speaking, there are few types of suitable polyionic pH-sensitive block polymers, mainly with amine groups and carboxyl groups as the response groups, and the pKa value can be adjusted in a small range

Method used

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  • Degradable polymer with pH sensitivity of tumor tissues and preparation method for degradable polymer and application of degradable polymer
  • Degradable polymer with pH sensitivity of tumor tissues and preparation method for degradable polymer and application of degradable polymer
  • Degradable polymer with pH sensitivity of tumor tissues and preparation method for degradable polymer and application of degradable polymer

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Embodiment 1

[0030] A degradable polymer with tumor tissue pH sensitivity, the polymer is a compound of the following structure:

[0031] 150≤n≤420, and n is an integer.

[0032] The synthetic route of described polymkeric substance is as follows:

[0033]

[0034]Add 10.0g of polyethylene glycol monomethyl ether (Mn=5000, 2mmol) into a 250mL round bottom flask, then add 100mL of toluene, dissolve 1.2g of potassium tert-butoxide in 15mL of tert-butanol, and then add polyethylene glycol monomethyl ether In ether / toluene solution, under nitrogen protection, react at 50°C for 20min. Dissolve 2.22mL of ethyl bromoacetate in 20mL of tert-butanol and add dropwise to the above reaction solution under nitrogen protection. Precipitation occurs immediately, and the temperature is kept at 50°C for 36h. After the reaction, the precipitate was removed by centrifugation, most of the solvent was removed by rotary evaporation of the supernatant, glacial ether (-4°C, 50mL) was precipitated, and th...

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Abstract

A degradable polymer with pH sensitivity of tumor tissues is a compound in the structure in the formula, wherein the formula is shown in the description, n is greater than or equal to 150 but less than or equal to 420, and n is an integer. The pH sensitive polymer provided by the invention as a drug-loading micelle has the characteristics that (1) the polymer is truly nanoscale (less than 200 nm) and is very uniform and stable; (2) multi-target technology (which overcomes the deficiencies of single targeting) comprises natural targeting of a long-circulating nanoparticle and pH sensitive physical and chemical targeting, so that tumor targeting is sufficiently obtained; (3) the polymer is large drug loading capacity and good in stability, and the treatment cost is lowered and the side effects generated by free drug release; (4) the drug is quickly released in a tumor tissue to obtain a local high concentration so as to quickly kill the cancer cells, and drug resistance is not easily generated; and (5) the polymer is less in distribution in normal tissues and few in side effects as a result of high tumor targeting; even if a small amount of polymer reaches the non-tumor parts, the drug is nearly not released or the release rate is less as a result of pH sensitivity, so that the polymer is few in side effects.

Description

technical field [0001] The invention belongs to the fields of medicinal polymer materials and biomedicine, and specifically relates to a degradable polymer with pH sensitivity of tumor tissue, its preparation method and application. Background technique [0002] In recent years, polymeric micelles have attracted more and more attention as one of the most promising drug delivery materials. A large number of new dosage forms of polymer micellar anticancer drugs have been developed, and some have entered the preclinical application stage, such as NK911 ? , SP1049C ? , NK105 ? and Genexol-PM ? Wait. The size of the polymer micelle drug-loading system is generally below 200 nanometers, and it can be selectively enriched around cancerous cells through the EPR (enhanced permeability and retention) effect. With the continuous progress of polymer synthesis chemistry, flexible molecular design endows polymer micelles with rich and diverse microstructures and continuously optimi...

Claims

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Application Information

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IPC IPC(8): C08G63/08C08G65/48A61K47/34A61K9/107A61K31/704A61P35/00
Inventor 刘蕾徐靖栾树娟秦本凯李稳稳徐惠平
Owner HENAN UNIVERSITY
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