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siRNA drug carrier polymer, preparation method thereof and application in targeted siRNA delivery

A carrier polymer and drug technology, applied in the fields of polymer chemistry and biomedical engineering, can solve the problems of low probability of combining drugs with lesions, poor stability of gene drug carriers, short cycle time, etc., to increase biocompatibility, Increases the chance of targeting and reduces the effect of toxicity

Active Publication Date: 2017-06-27
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology describes how certain types of chemicals called drugs are able to be delivered into cells through specific ways that make them easier for other molecules like DNA or proteins inside their body. These techniques involve modifying these substance with special materials made from synthetic resin material (poly ethyleneglycols) instead of traditional plastic). By adding this modified version of matter on top of it's own design, they become more effective when delivered within tissues where there may have been damage caused by surgery or disease.

Problems solved by technology

This patented technical solution described in the patents relates to improving the efficiency or accuracy of delivering small nucleic acid agents into cells called ASFISCs during medical procedures like angioplasties. Current techniques involve administering chemical substances directly inside patients without any knowledge about how they develop symptoms related to inflammations caused by plaque buildup on vessel walls. To address this challenge, there was proposed a technique involving targeted administration of specific types of nanopartides containing certain functional groups along with chemotherapeutants to enhance antiinflammatory effects while minimizing side reactions associated with traditional approaches.

Method used

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  • siRNA drug carrier polymer, preparation method thereof and application in targeted siRNA delivery
  • siRNA drug carrier polymer, preparation method thereof and application in targeted siRNA delivery
  • siRNA drug carrier polymer, preparation method thereof and application in targeted siRNA delivery

Examples

Experimental program
Comparison scheme
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 high-polymer chemical and biomedical medical engineering, and particularly discloses an siRNA drug carrier polymer, a preparation method thereof and application in targeted siRNA delivery. The nano drug is based on a biocompatible cationic polymer carrier, polyethylene glycol-polyaspartic acid is grafted with polyethyleneimine (mPEG-PAsp-(g-PEI)), the surface is utilized to modify a CD36 single-chain antibody, targeted siRNA delivery of atherosclerotic plaque foam cells is achieved, PAK1 expressions in plaques are lowered, secretion of inflammatory factors in its downstream is reduced, accordingly disease course of atherosclerosis is shortened, and the purpose of treating the atherosclerosis is achieved.

Description

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Claims

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Application Information

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Owner SUN YAT SEN UNIV
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