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Amphipathy hydroxyethyl-starch-coupled-polylactic-acid copolymer and preparing method and application thereof

A polylactic acid copolymer and hydroxyethyl starch technology, which is applied in the multidisciplinary field, can solve the problems of low drug loading, large size, unstable structure, etc., and achieve the effects of uniform chain length, high degree of polymerization, and stable structure.

Active Publication Date: 2017-02-22
HUAZHONG UNIV OF SCI & TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Aiming at the above defects or improvement needs of the prior art, the present invention provides an amphiphilic hydroxyethyl starch-coupled polylactic acid copolymer, its nano-drug loading system, its preparation method and application. An amphiphilic hydroxyethyl starch-coupled polylactic acid copolymer was obtained through esterification reaction between starch and carboxyl-terminated polylactic acid, in which hydroxyethyl starch was the hydrophilic segment and polylactic acid was the hydrophobic segment. The amphiphilic block copolymer was prepared by emulsification and high-pressure homogenization technology to obtain a nano drug-loading system of amphiphilic hydroxyethyl starch-coupled polylactic acid copolymer loaded with anti-tumor drug doxorubicin, thus solving the existing problem Technical issues of low drug loading, oversized and structurally unstable amphiphilic copolymers

Method used

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  • Amphipathy hydroxyethyl-starch-coupled-polylactic-acid copolymer and preparing method and application thereof
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  • Amphipathy hydroxyethyl-starch-coupled-polylactic-acid copolymer and preparing method and application thereof

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preparation example Construction

[0040] The preparation method, such as figure 1 As shown, it specifically includes the following steps:

[0041] (1) Dissolving polylactic acid and activating its terminal carboxyl group: Add catalyst N-N'-dicyclohexylcarbodiimide and 4-dimethylaminopyridine to carboxyl-terminated polylactic acid, and use anhydrous dimethyl sulfoxide as a solvent , react at 50-70°C for 25-45 minutes, make it dissolve completely, and obtain polylactic acid activated by the carboxyl-terminated group; said polylactic acid, N-N'-dicyclohexylcarbodiimide and 4-dimethylaminopyridine The feeding molar ratio is 1:4:2;

[0042] (2) Dissolving hydroxyethyl starch: under the condition of nitrogen protection, fully dissolve the hydroxyethyl starch in anhydrous dimethyl sulfoxide at 50-70° C. to obtain a dimethyl sulfoxide solution of hydroxyethyl starch;

[0043] (3) Esterification reaction: the polylactic acid activated by the carboxyl end group obtained in step (1) is mixed with the dimethyl sulfoxide...

Embodiment 1

[0055] A kind of amphiphilic block polymer hydroxyethyl starch-polylactic acid (HES-g-PLA), is synthesized according to the following steps:

[0056] (1) Dissolve the polylactic acid and activate the terminal carboxyl group: 0.565g carboxyl-terminated polylactic acid (PLA-COOH), N-N'-dicyclohexylcarbodiimide (DCC), 4-dimethylaminopyridine (DMAP ), wherein the molar ratio of PLA, DCC, and DMAP is 1:4:2 and placed in a 100mL dry round bottom flask, the system is replaced with nitrogen, and a nitrogen balloon is connected. At the same time, 15 mL of anhydrous dimethyl sulfoxide (DMSO) solvent under nitrogen protection was added, and stirred at 60° C. for 30 min to completely dissolve the reactant and activate its terminal carboxyl group.

[0057] (2) Dissolving hydroxyethyl starch: Dissolve 0.5 g of hydroxyethyl starch in 10 mL of anhydrous DMSO solvent while performing step (1). The whole reaction process uses nitrogen as a protective gas, and the reaction temperature is set to ...

Embodiment 2

[0065] A kind of amphiphilic block polymer hydroxyethyl starch-polylactic acid (HES-g-PLA), is synthesized according to the following steps:

[0066] (1) Dissolve polylactic acid and activate the terminal carboxyl group: 0.323g carboxyl-terminated polylactic acid (PLA-COOH), N-N'-dicyclohexylcarbodiimide (DCC), 4-dimethylaminopyridine (DMAP ), wherein the molar ratio of PLA, DCC, and DMAP is 1:4:2 and placed in a 100mL dry round bottom flask, the system is replaced with nitrogen, and a nitrogen balloon is connected. At the same time, 15 mL of anhydrous dimethyl sulfoxide (DMSO) solvent under nitrogen protection was added, and stirred at 50° C. for 25 min to completely dissolve the reactant and activate its terminal carboxyl group.

[0067] (2) Dissolving hydroxyethyl starch: Dissolve 0.5 g of hydroxyethyl starch in 10 mL of anhydrous DMSO solvent while performing step (1). The whole reaction process uses nitrogen as a protective gas, and the reaction temperature is set at 50 ...

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Abstract

The invention discloses an amphipathy block-polymer hydroxyethyl-starch-olylactic-acid copolymer and a preparing method and nanometer medicine loading system thereof. The method includes the steps that 4-dimethylaminopyridine serves as a catalyst, N-N'-dicyclohexylcarbodiimide serves as a dehydrating agent, carboxyl at the tail end of polylactic acid and hydroxyl on hydroxyethyl-starch sugar ring are subjected o an esterification reaction, hydrophobic polylactic acid is coupled on hydrophilic hydroxyethyl starch accordingly, and the amphipathy hydroxyethyl-starch-polylactic-acid block polymer is synthesized. Debydrochlorination adriamycin amycin is loaded to a hydrophobic core with the emulsified solvent evaporation method and the high pressure homogenization technology, evenly-distributed medicine loading polymer nanometer particles with the particle-size of about 140 nm are formed, and are applied in preparing antitumor medicine, the medicine in-vivo cycling time is prolonged, the toxic and side effects of the medicine are reduced, and the good antitumor effect is achieved.

Description

technical field [0001] The invention belongs to the interdisciplinary fields of chemistry, pharmacy, medicine, etc., and specifically relates to a preparation technology of an amphiphilic block polymer nano drug carrier with good biocompatibility and degradability, and more specifically relates to a two- The hydrophilic hydroxyethyl starch polylactic acid coupling copolymer, its nano-drug loading system, its preparation method and application. Background technique [0002] Cancer is one of the major diseases threatening human health. Surgical treatment, chemotherapy and radiotherapy are the three most commonly used methods for cancer treatment, among which chemotherapy plays an important role in cancer treatment. However, many chemotherapeutic drugs currently developed have the problems of poor water solubility and short circulation in the body. In addition, although many common chemotherapeutic drugs have significant therapeutic effects, their bioavailability is low due t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K47/36A61K47/34A61K31/704A61P35/00
CPCA61K31/704A61K47/34A61K47/36C08G81/00
Inventor 杨祥良李子福万影徐辉碧余婵周庆
Owner HUAZHONG UNIV OF SCI & TECH
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