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A kind of siRNA drug carrier polymer and its preparation method and application in siRNA targeted delivery

A carrier polymer and drug technology, applied in the fields of polymer chemistry and biomedical engineering, can solve the problems of low drug and lesion binding probability, poor stability of gene drug carrier, and short cycle time, so as to increase biocompatibility, Effects that increase targeting probability and reduce toxicity

Active Publication Date: 2021-05-18
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the problems of poor stability of gene drug carriers in the prior art, short retention time, short circulation time, and low probability of drug and lesion binding, and to provide a siRNA drug carrier polymer

Method used

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  • A kind of siRNA drug carrier polymer and its preparation method and application in siRNA targeted delivery
  • A kind of siRNA drug carrier polymer and its preparation method and application in siRNA targeted delivery
  • A kind of siRNA drug carrier polymer and its preparation method and application in siRNA targeted delivery

Examples

Experimental program
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Effect test

Embodiment 1

[0039] A kind of siRNA drug carrier polymer, its structure is as follows:

[0040]

[0041] (I)

[0042] Wherein, x is 45, m is 8, n is 6, and polyethyleneimine is a linear structure.

[0043] The polymer-loaded gene medicines were nanoscale particles with a particle size of 129.8 ± 23.9 nm.

[0044] Synthesis of siRNA drug carrier polymer shown in formula (I)

[0045] S1. Synthesis of polyethyleneimine: poly(2-ethyl-oxazoline) (PEOX) is synthesized by ring-opening polymerization of 2-ethyl-oxazoline; polyethyleneimine (PEI );

[0046] The synthesis of linear polyethyleneimine (PEI), the reaction mechanism and process are as follows:

[0047]

[0048] Poly(2-ethyl-oxazoline) (PEOX) was first synthesized. Methyl p-toluenesulfonate (2 mmol) was dried in vacuum at normal temperature for 2 h, then dissolved in 15 mL of freshly distilled acetonitrile, and then 2-ethyl-oxazoline (24 mmol) was added to the reaction flask, 85 ○ C reflux for 72 h; after cooling, immerse the r...

Embodiment 2

[0059] A kind of siRNA drug carrier polymer, its structure is as follows:

[0060]

[0061] Wherein, x is 45, m is 12, n is 12, and polyethyleneimine is a linear structure.

[0062] The difference between the synthesis method and Example 1 is that the reflux reaction time at 85° C. in step S1 is 130 h, and the heating and stirring reaction in an oil bath at 35° C. in step S2 is 144 h.

Embodiment 3

[0064] A kind of siRNA drug carrier polymer, its structure is as follows:

[0065]

[0066] Wherein, x is 45, m is 10, n is 10, and polyethyleneimine is a linear structure.

[0067] The difference between the synthesis method and Example 1 is that the reflux reaction time at 85° C. in step S1 is 100 h, and the heating and stirring reaction in an oil bath at 35° C. in step S2 is 100 h.

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Abstract

The invention belongs to the field of polymer chemistry and biomedical engineering, and specifically discloses a siRNA drug carrier polymer, a preparation method thereof and an application in siRNA targeted delivery. The nanomedicine is based on a biocompatible cationic polymer carrier, polyethylene glycol-polyaspartic acid-grafted polyethyleneimine (mPEG-PAsp-(g-PEI)), which uses surface-modified CD36 single-chain Antibody, realize the delivery of targeted siRNA to atherosclerotic plaque foam cells, down-regulate the expression of PAK1 in the plaque, reduce the secretion of inflammatory factors downstream, thereby reducing the course of atherosclerosis and achieving the purpose of treating atherosclerosis .

Description

technical field [0001] The invention relates to the fields of polymer chemistry and biomedical engineering, in particular to a drug carrier polymer and its application in targeted siRNA delivery carriers. Background technique [0002] Atherosclerosis (AS) can lead to myocardial infarction, coronary heart disease, stroke and other diseases such as ischemic cardiovascular and cerebrovascular embolism, and has always been the main cause of death in developed countries. In my country, due to the improvement of people's living standards, the relative and absolute incidence of the disease has increased due to the unhealthy lifestyle produced, resulting in atherosclerosis and its complications have now become the main cause of death in my country. The prevention, diagnosis and treatment of atherosclerosis have always been a hotly concerned issue. With the advancement of science and technology and the attention of relevant government departments and units, significant progress has ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K48/00A61K31/713A61K47/59A61K47/68A61P9/10C08G81/00C08G69/40C08G73/02
CPCA61K31/713A61K47/34C08G69/40C08G73/0206C08G81/00
Inventor 帅心涛吴腾王勇程度
Owner SUN YAT SEN UNIV
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