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A drug-carrying system capable of specific drug release at tumor sites and its preparation method

A drug-carrying system and specific technology, which can be used in anti-tumor drugs, pharmaceutical formulations, medical preparations with inactive ingredients, etc. problems, to achieve the effect of improving bioavailability, obvious toxicity, and high drug loading

Active Publication Date: 2019-01-01
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the stability of polymer micelles is poor after dilution, especially after highly diluted blood, the drug will be released in advance in the systemic circulation, resulting in low bioavailability of the drug
In order to solve the problem of micelles stability, some scholars carry out chemical cross-linking on the surface of micelles. Although this method can increase the stability of micelles, it will reduce the drug release of micelles at the tumor site, resulting in multi-drug production of tumors. drug resistance

Method used

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  • A drug-carrying system capable of specific drug release at tumor sites and its preparation method
  • A drug-carrying system capable of specific drug release at tumor sites and its preparation method
  • A drug-carrying system capable of specific drug release at tumor sites and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] 1. Preparation of cystamine-modified hyaluronic acid:

[0044] Dissolve 0.5 mmol of hyaluronic acid (HA) in 50 mL of 0.01 M, pH 7.4 phosphate buffered saline (PBS), then add 2 mmol of 1-ethyl-(3-dimethylaminopropyl)carbodiimide (EDC) and 0.4mmol N-hydroxysuccinimide (NHS), reacted at room temperature for 15 minutes; then added 5mmol cystamine (CYS), and continued to react at room temperature for 4 hours; In the bag, dialyze in 0.1M sodium chloride solution and deionized water for 1 day and 2 days respectively, and freeze-dry to obtain the cystamine-modified hyaluronic acid intermediate.

[0045] 2. Preparation of deoxycholic acid activated ester:

[0046] 1mmol of deoxycholic acid, 1.2mmol of dicyclohexylcarbodiimide (DDC), and 1.2mmol of N-hydroxysuccinimide (NHS) were dissolved in tetrahydrofuran (THF), reacted for 30 minutes under ice-cooling, and then React at room temperature for 12 hours; remove the precipitate by suction filtration, precipitate with excess ice ...

Embodiment 2

[0084] 1. Preparation of cystamine-modified hyaluronic acid:

[0085] As described in Example 1.

[0086] 2. Preparation of deoxycholic acid activated ester:

[0087] As described in Example 1.

[0088] 3. Preparation of deoxycholic acid-cystamine-hyaluronic acid graft copolymer:

[0089] As described in Example 1.

[0090] 4. Preparation of drug-loaded polymer micelles (paclitaxel (PTX)-deoxycholic acid-cystamine-hyaluronic acid micelles):

[0091] As described in Example 1.

[0092] 5. Preparation of the drug-loading system (calcium carbonate nanoshell-PTX-deoxycholic acid-cystamine-hyaluronic acid micelles):

[0093] Measure 10 mL of drug-loaded polymer micelles (paclitaxel (PTX)-deoxycholic acid-cystamine-hyaluronic acid micelles), adjust the pH of the drug-loaded micelles to 7.0, and then stir at room temperature at 400 rpm ;

[0094] According to the molar weight of carboxyl groups on the surface of the micelles (the total molar weight of carboxyl groups on hyalur...

Embodiment 3

[0097] 1. Preparation of cystamine-modified hyaluronic acid:

[0098] As described in Example 1.

[0099] 2. Preparation of octanoic acid-cystamine-hyaluronic acid graft copolymer:

[0100] According to the molar ratio of octanoic acid to 1-ethyl-(3-dimethylaminopropyl) carbodiimide and hyaluronic acid modified by cystamine as 5:5:1, feed into formamide and react at room temperature After 24 hours, the reaction was terminated, dialyzed in a mixed solution of ethanol and water with a volume ratio of 1:1, and in deionized water for 1 day and 2 days respectively, and freeze-dried to obtain octanoic acid-cystamine-hyaluronic acid grafted branch copolymers.

[0101] 3. Preparation of drug-loaded polymer micelles (paclitaxel (PTX)-octanoic acid-cystamine-hyaluronic acid micelles):

[0102] Dissolve 60 mg of caprylic acid-cystamine-hyaluronic acid graft copolymer in 10 mL of deionized water and stir at room temperature for 15 minutes to obtain polymer micelles (caprylic acid-cysta...

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Abstract

The invention discloses a drug loading system capable of specifically releasing drugs at tumor parts and a preparation method of the drug loading system. The drug loading system refers to that a layer of acid-sensitive inorganic salt nano shell is arranged at a hydrophilic end of drug loading polymeric micelle; antitumor drugs are wrapped and loaded in the drug loading polymeric micelle; the drug loading polymeric micelle has disulfide bonds; the hydrophilic end of the drug loading polymeric micelle is carboxylated. Tests show that by adopting the drug loading system disclosed by the invention, reduction and dual response characteristics of acids can be simultaneously achieved, drugs can be only specifically released at the tumor parts, remarkable targeting properties can be achieved, the solubility of antitumor drugs is improved, moreover the bioavailability of the antitumor drugs can be remarkably improved, and the drug loading system is remarkable in toxic function on tumor cells and low in toxic and side effect on other normal tissue and organs, and has remarkable values for treatment on tumor diseases.

Description

technical field [0001] The invention relates to a drug-carrying system capable of specifically releasing drugs at tumor sites and a preparation method thereof, belonging to the technical field of targeted drug delivery. Background technique [0002] Tumor has become one of the most important diseases that threaten human life and health. At present, the methods for treating tumor mainly include radiation therapy, surgical resection and drug chemotherapy. Among them, drug chemotherapy is the most commonly used method to treat tumors, but there are many deficiencies in the traditional way of drug delivery. For example: the half-life of most anticancer drugs in the body is short, and the concentration of the drug in the tumor site is insufficient, resulting in insignificant therapeutic effect; giving the dose to achieve the therapeutic effect will cause serious toxic side effects to normal tissues and organs; anticancer drugs are water insoluble Features, vascular drug deliver...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/36A61K47/34A61K47/02A61K31/337A61P35/00
CPCA61K9/1075A61K31/337A61K47/02A61K47/34
Inventor 谢燕邓冰夏梦欣李瑞李国文刘名玉辛雷李璐佳韩晓乐任淑珍
Owner SHANGHAI UNIV OF T C M
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