Hydroxyalkyl starch conjugate, and preparation method and application thereof

A technology of hydroxyalkyl starch and hydroxyethyl starch, which is applied in the directions of pharmaceutical combinations, pharmaceutical formulations, medical preparations of non-active ingredients, etc.

Active Publication Date: 2018-09-07
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, how to effectively combine this iRGD peptide with a reduction-responsive drug carrier to increase the uptake of the reduction-responsive drug carrier by tumor cells and further enhance the anti-tumor activity has not been reported.

Method used

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  • Hydroxyalkyl starch conjugate, and preparation method and application thereof
  • Hydroxyalkyl starch conjugate, and preparation method and application thereof
  • Hydroxyalkyl starch conjugate, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] The present embodiment provides a hydroxyethyl starch conjugate, comprising the steps of:

[0082] (1) Dissolve 1.00 g of hydroxyethyl starch (sugar ring is 5.6 mmol) in 20 mL of ultrapure water, add 0.85 g (21.2 mmol) of sodium hydroxide to activate the hydroxyl group, and stir at room temperature for 0.5 h to obtain the reaction solution A, and then to the reaction Add 1.00 g (10.6 mmol) of chloroacetic acid to solution A, stir at room temperature to dissolve, then move to 70°C oil bath and stir for 3 hours to obtain reaction solution B;

[0083] (2) Pour the reaction solution B obtained in step (1) into 200 mL of methanol and stir to obtain a suspension C;

[0084] (3) Filtrate the suspension C obtained in step (2) to obtain a white precipitate, wash the precipitate three times with methanol, 50 mL each time, and then vacuum-dry at room temperature to obtain a dry white precipitate;

[0085] (4) Redissolve the dry white precipitate obtained in step (3) in ultrapure ...

Embodiment 2

[0095] The present embodiment provides a hydroxyethyl starch conjugate, comprising the steps of:

[0096] Steps (1)~(6) are identical with embodiment 1

[0097] (7) 195.6 mg (2-pyridyl is 0.11 mmol) of the hydroxyethyl starch-2-(2-pyridyldithio)ethylamine conjugate obtained in step (6) was dissolved in 5 mL dimethyl sulfoxide, Add 17.2mg (0.06mmol) of n-octadecylmercaptan, and stir at room temperature for 24h to obtain reaction solution E;

[0098] (8) Pour the reaction solution E obtained in step (7) into 50 mL of ethanol / ether mixed solvent (1:1, V / V), and stir to obtain a suspension F;

[0099] (9) Filter the suspension F obtained in step (8) to obtain a white precipitate, wash the white precipitate three times with ethanol / ether mixed solvent (1:1, V / V), 10 mL each time, and then vacuum-dry at room temperature , to obtain a dry white precipitate;

[0100] (10) Disperse the dry white precipitate obtained in step (9) in ultrapure water, and dialyze with ultrapure water fo...

Embodiment 3

[0104] The present embodiment provides a hydroxyethyl starch conjugate, comprising the steps of:

[0105] Steps (1)~(6) are identical with embodiment 1

[0106] (7) 195.6 mg (2-pyridyl is 0.11 mmol) of the hydroxyethyl starch-2-(2-pyridyldithio)ethylamine conjugate obtained in step (6) was dissolved in 5 mL dimethyl sulfoxide, Add 22.9mg (0.08mmol) of n-octadecylmercaptan, stir and react at room temperature for 24h to obtain reaction solution E;

[0107] (8) Pour the reaction solution E obtained in step (7) into 50 mL of ethanol / ether mixed solvent (1:1, V / V), and stir to obtain a suspension F;

[0108] (9) Filter the suspension F obtained in step (8) to obtain a white precipitate, wash the white precipitate three times with ethanol / ether mixed solvent (1:1, V / V), 10 mL each time, and then vacuum-dry at room temperature , to obtain a dry white precipitate;

[0109] (10) Disperse the dry white precipitate obtained in step (9) in ultrapure water, and dialyze with ultrapure wa...

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Abstract

The invention provides a hydroxyalkyl starch conjugate, and a preparation method and an application thereof. The hydroxyalkyl starch conjugate is formed by covalently coupling a hydrophobic segment and an iRGD peptide to hydroxyalkyl starch respectively. The hydroxyalkyl starch conjugate provided by the invention can self-assemble in water to form a nano-cluster, and can load drugs, especially doxorubicin, at a high encapsulation rate and a drug loading amount; and a result of in-vitro drug release studies shows that the drug-loaded nano-cluster has a reducing responsive drug release property.

Description

technical field [0001] The invention relates to the technical field of drug-carrying systems, in particular to a hydroxyalkyl starch conjugate and its preparation method and application. Background technique [0002] Chemotherapy is one of the five major means of tumor treatment at present. It mainly uses chemical drugs to kill tumor cells or inhibit the proliferation of tumor cells. reaction. The reduction-responsive nano-drug delivery system based on polymer materials has been extensively studied in recent years for the delivery of anti-tumor drugs. The aggregation of tissues and organs reduces toxic and side effects. These nanocarriers can enter tumor cells through endocytosis, disintegrate under the action of high concentration of reduced glutathione in tumor cells, release the loaded drugs, and exert their efficacy. However, these nanocarriers still have many shortcomings, such as low drug loading and encapsulation efficiency, resulting in high drug loading costs; low...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B31/12A61K47/61A61K47/64A61K31/704A61P35/00
CPCA61K31/704A61K47/61A61K47/64A61P35/00C08B31/125
Inventor 李子福杨祥良徐辉碧胡航
Owner HUAZHONG UNIV OF SCI & TECH
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