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Adriamycin corn starch grafted polymer micelle and preparation method thereof

A technology of grafted polymer and corn starch, which is applied in the field of biomedicine to achieve the effects of low manufacturing cost, good biocompatibility and stable process

Pending Publication Date: 2020-12-25
GUANGXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

After searching, there is currently no patent application or literature report on the preparation of doxorubicin drug-loaded micelles using sulfobetaine and deoxycholic acid grafted corn starch as drug carriers to promote the delivery efficiency of anti-tumor drugs

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  • Adriamycin corn starch grafted polymer micelle and preparation method thereof
  • Adriamycin corn starch grafted polymer micelle and preparation method thereof

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0022] Embodiment 1: the synthesis of cornstarch graft polymer

[0023] S1. Synthesis of zwitterionic starch grafted polymer: Dissolve 1 mmol of corn starch in 3 mL of ultrapure water, add 3 mL of 40 wt % sodium hydroxide solution dropwise to it, and stir and react at 40 ° C for 0.5 h to obtain Alkalized starch suspension: Dissolve 0.2g sulfobetaine in 20mL water, add to the above-mentioned alkalized starch suspension, stir and react at 40°C for 0.5h; neutralize the reaction system to neutral with glacial acetic acid, Precipitate with methanol, obtain precipitate after centrifugation, and freeze-dry to obtain zwitterionic starch graft polymer;

[0024] S2. Synthesis of corn starch graft polymer: 1.2mmol 1-ethyl-(3-dimethylaminopropyl)-carbodiimide hydrochloride, 0.6mmol N-hydroxysuccinimide and 0.1mmol deoxygenated Cholic acid was dissolved in 5mL N,N-dimethylformamide, and activated at room temperature for 15min to obtain carboxyl-activated deoxycholic acid; 200mg of zwitter...

Embodiment 2

[0026] Embodiment 2: the synthesis of corn starch graft polymer

[0027] S1. Synthesis of zwitterionic starch grafted polymer: Dissolve 1 mmol of corn starch in 3 mL of ultrapure water, add 3 mL of 40 wt % sodium hydroxide solution dropwise to it, and stir and react at 50 ° C for 1 h to obtain alkali starch suspension; 0.4g sulfobetaine was dissolved in 3mL water, and added to the above alkalized starch suspension, stirred and reacted at 60°C for 5h; the reaction system was neutralized to neutral with glacial acetic acid, and methanol precipitated analysis, centrifugation to obtain a precipitate, and freeze-drying to obtain a zwitterionic starch grafted polymer;

[0028] S2. Synthesis of corn starch graft polymer: 1.2mmol 1-ethyl-(3-dimethylaminopropyl)-carbodiimide hydrochloride, 0.6mmol N-hydroxyl succinimide and 0.3mmol deoxygenated Cholic acid was dissolved in 5mL N,N-dimethylformamide, and activated at room temperature for 20min to obtain carboxyl-activated deoxycholic a...

Embodiment 3

[0030] Embodiment 3: the synthesis of cornstarch graft polymer

[0031] S1. Synthesis of zwitterionic starch grafted polymer: Dissolve 1 mmol of corn starch in 3 mL of ultrapure water, add 3 mL of 40 wt % sodium hydroxide solution dropwise to it, and stir and react at 70 ° C for 1.5 h to obtain Alkalized starch suspension; dissolve 1.6g sulfobetaine in 3mL water, and add it to the above-mentioned alkalized starch suspension, stir and react at 70°C for 8h; neutralize the reaction system with glacial acetic acid, then methanol Precipitation treatment, centrifugation to obtain a precipitate, freeze-drying to obtain a zwitterionic starch graft polymer;

[0032]S2. Synthesis of corn starch grafted polymer: 1.2mmol 1-ethyl-(3-dimethylaminopropyl)-carbodiimide hydrochloride, 0.6mmol N-hydroxysuccinimide and 1mmol deoxychol The acid was dissolved in 5mL N,N-dimethylformamide, and activated at room temperature for 30min to obtain carboxyl-activated deoxycholic acid; 200mg of zwitterio...

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Abstract

The invention provides an adriamycin starch grafted polymer micelle and a preparation method thereof. A corn starch grafted polymer obtained by grafting zwitterionic sulfobetaine (SB) and deoxycholicacid (DCA) on corn starch (CST) is used as a carrier to encapsulate a hydrophobic antitumor drug adriamycin, and the particle diameter of the obtained adriamycin starch grafted polymer micelle (SB-CST-DCA) is less than 200nm. The drug loading capacity is 5%-16%, and the encapsulation rate is 59%-80%.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a doxorubicin-corn starch-grafted polymer micelle and a preparation method thereof. Background technique [0002] Doxorubicin (DOX) is a drug with strong cell independence, because it contains fat-soluble anthracycline, water-soluble daunosamine, acidic phenolic hydroxyl group and basic amino group, it has extremely strong anti-tumor activity. At present, it has been widely used in the treatment of various cancers such as liver cancer and osteosarcoma. However, doxorubicin is mainly administered by injection, which can easily lead to phlebitis, liver function damage, body inflammation, and in serious cases directly lead to patient death. Its serious toxic and side effects in clinical application limit its development. Therefore, in the treatment of tumors, improving the therapeutic efficiency of doxorubicin and reducing the toxic and side effects is the key. At ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/704A61K47/36A61P35/00C08B31/04
CPCA61K9/1075A61K31/704A61K47/36A61P35/00C08B31/04
Inventor 李坚斌贠琳琦刘灿灿邓立高李凯
Owner GUANGXI UNIV