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Imitated virus-structured high-polymer vesicle with target function and preparation and application thereof

A technology of polymer vesicles and functions, which can be used in anti-tumor drugs, liposome delivery, drug combination, etc., can solve the problem that polymer vesicles have not been publicly reported, and achieve good targeting and good application prospects. , good repeatability

Inactive Publication Date: 2017-09-08
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there are no public reports on polymer vesicles with tumor cell targeting function and virus-like structure

Method used

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  • Imitated virus-structured high-polymer vesicle with target function and preparation and application thereof
  • Imitated virus-structured high-polymer vesicle with target function and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] (1) Add 1.0g hyaluronic acid (M w =5000, 0.2mmol) dissolved in 30mL acetate buffer (pH = 5.6, acetic acid / sodium acetate), after complete dissolution, add 1.0mL 1,4-butanediamine (0.4mmol), 50 ℃ constant temperature Under the conditions, magnetic stirring for 24 hours; then, while keeping the temperature and stirring conditions unchanged, add 0.2g of sodium boron cyanide every day for three times. Use a dialysis bag to dialyze in deionized water for 1 day. Freeze drying at ℃ to obtain amino-terminated hyaluronic acid;

[0051] (2) Weigh 1.0g of PCL-COOH (PCL with carboxyl end, M w =10,000, 0.1mmol), dissolved in 10mL of methanol, add 0.2mmol of EDC and 0.2mmol of NHS, stir at room temperature for 24h, use 10mL of methanol / ether (75 / 25v / v) to precipitate the product, and vacuum dry at 70°C for 3h , To obtain NHS / carboxyl active intermediate ester, which is the product of carboxyl activation;

[0052] (3) Weigh 0.5g of amino-terminated hyaluronic acid and NHS / carboxyl active ...

Embodiment 2

[0055] (1) Put 2.0g hyaluronic acid (M w =5,000, 0.4mmol) dissolved in 30mL acetate buffer (pH = 5.6, acetic acid / sodium acetate), after complete dissolution, add 1.0mL 1,4-butanediamine (0.4mmol), 50 ℃ constant temperature conditions Under the condition of magnetic stirring for 24 hours; then, while keeping the temperature and stirring conditions unchanged, add 0.2g of sodium boron cyanide every day for a total of three times. Use a dialysis bag to dialyze in deionized water for 1 day. Freeze-drying under conditions to obtain amino-terminated hyaluronic acid;

[0056] (2) Weigh 1.0g of PCL-COOH (PCL with carboxyl end, M w =10,000, 0.1mmol), dissolved in 10mL of methanol, add 0.2mmol of EDC and 0.2mmol of NHS, stir at room temperature for 24h, use 10mL of methanol / ether (75 / 25v / v) to precipitate the product, and vacuum dry at 70°C for 3h , To obtain NHS / carboxyl active intermediate ester;

[0057] (3) Weigh 0.5g of amino-terminated hyaluronic acid and NHS / carboxyl active intermedi...

Embodiment 3

[0060] (1) Add 1.0g hyaluronic acid (M w =5000, 0.2mmol) dissolved in 30mL acetate buffer (pH=5.6, acetic acid / sodium acetate), after complete dissolution, add 1.0mL 1,4-butanediamine (0.4mmol), 50℃ constant temperature conditions Under the condition of magnetic stirring for 24 hours; then, while keeping the temperature and stirring conditions unchanged, add 0.2g of sodium borocyanide every day for a total of three times. Use a dialysis bag to dialyze the bag in deionized water for 1 day. Freeze drying at ℃ to obtain amino-terminated hyaluronic acid;

[0061] (2) Weigh 2.0g of PVP-COOH (carboxy-terminated PVP, M w =10,000, 0.2mmol), dissolved in 10mL of methanol, add 0.4mmol of EDC and 0.4mmol of NHS, stir at room temperature for 24h, use 10mL of methanol / ether (75 / 25v / v) to precipitate the product, and vacuum dry at 70°C for 3h , To obtain NHS / carboxyl active intermediate ester;

[0062] (3) Weigh 0.5g of amino-terminated hyaluronic acid and NHS / carboxyl active intermediate ester...

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Abstract

The invention belongs to the field of high-polymer materials and discloses an imitated virus-structured high-polymer vesicle with a target function and preparation and application thereof. The preparation method of the imitated virus-structured high-polymer vesicle with the target function comprises, S1, performing amide reaction on hyaluronic acid containing amino and hydrophobic polymers containing carboxyl to obtain hyaluronic acid grafted amphiphilic block copolymers, wherein the hydrophobic polymers containing carboxyl requires carboxyl activation before reaction are performed, and the hyaluronic acid containing amino are obtained through reaction between diamine and hyaluronic acid; S2, reacting the hyaluronic acid grafted amphiphilic block copolymers with other amphiphilic block copolymers through a solvent exchange method or a hydration method to obtain the imitated virus-structured high-polymer vesicle with the target function. The preparation method of the imitated virus-structured high-polymer vesicle with the target function is simple in operation, flexible in modification, high in production efficiency and good in repeatability; the prepared imitated virus-structured high-polymer vesicle achieves the target function and can be applied to the biomedical fields such as drug carriers.

Description

Technical field [0001] The invention belongs to the field of polymer materials, and relates to a polymer vesicle with a virus-like structure with a targeting function and a preparation method thereof, in particular to an amphiphilic block copolymer grafted with hyaluronic acid and other amphiphilic The block copolymer is mixed and self-assembled into a polymer vesicle with a virus-like surface synapse structure, and a preparation method and application thereof. [0002] technical background [0003] Malignant tumor is a serious disease that endangers human life and health. Its prevention and treatment is still a difficult point in the field of life science research today. Conventional chemotherapy is a systemic therapy, which is the first choice among related treatment methods, and is suitable for most solid tumors or hematological tumors. However, the known chemotherapeutic drugs still generally have the problems of strong toxicity and poor tumor target recognition. While killing...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08J3/03C08J3/07C08G81/00C08G81/02C08L67/04C08L87/00A61K9/127A61K47/36A61K47/34A61P35/00
CPCC08J3/03A61K9/1273A61K47/34A61K47/36C08G81/00C08G81/02C08J3/07C08J2367/04C08J2487/00C08L67/04C08L87/00
Inventor 王林格司自卫李卫昌
Owner SOUTH CHINA UNIV OF TECH
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