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Modified polyrotaxane, medicine carrier micelle based on polyrotaxane and preparation method and application of micelle

A technology of drug-loaded micelles and polyrotaxanes, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, antineoplastic drugs, etc., can solve the problem of low encapsulation efficiency of drugs, achieve clear hydrophilic and hydrophobic structures, and improve encapsulation. terminal efficiency and mild reaction conditions

Active Publication Date: 2018-08-14
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In terms of drug application, people usually self-assemble PEG / α-cyclodextrin host and guest into a polyrotaxane supramolecular system, and use α-cyclodextrin to graft drugs. The sealing rate is not high, and only drugs that can react with cyclodextrin can be grafted

Method used

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  • Modified polyrotaxane, medicine carrier micelle based on polyrotaxane and preparation method and application of micelle
  • Modified polyrotaxane, medicine carrier micelle based on polyrotaxane and preparation method and application of micelle
  • Modified polyrotaxane, medicine carrier micelle based on polyrotaxane and preparation method and application of micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] (1) Preparation of pseudopolyrotaxane: Dissolve activated ester modified polyethylene glycol (1g, 0.43mmol) (molecular weight: 2330, molar mass of activated ester unit: 0.86mmol) in 5mL deionized water, and add Added to a saturated aqueous solution of α-cyclodextrin (8.35g, 8.56mmol), a white precipitate formed after a few minutes, sonicated for 1.5h (ultrasonic frequency: 40kHz, power: 100W), stirred at room temperature (speed: 400rpm) for 12h, and collected by centrifugation Precipitate, freeze-dried to obtain quasi-polyrotaxane PPR;

[0065] (2) Preparation of polyrotaxane: Dissolve amino-modified cholic acid (0.32g, 0.71mmol) (molecular weight: 450) in 4mL DMF, and add dropwise to pseudopolyrotaxane PPR (4g, 0.236mmol, activated ester unit The molar weight is 0.47mmol) powder, stir until a yellow viscous liquid is formed, add triethylamine (10μL, 0.072mmol) dropwise to catalyze, ultrasonically treat for 1.5h (ultrasonic frequency: 40kHz, power: 100W), and react at 5...

Embodiment 2

[0074] (1) Preparation of pseudopolyrotaxanes: Dissolve activated ester modified polyethylene glycol (1g, 0.43mmol) in 5mL deionized water, and add dropwise to α-cyclodextrin (7.52g, 7.73mmol) In the saturated solution, a white precipitate formed after a few minutes, sonicated for 1h (ultrasonic frequency: 40kHz, power: 200W), stirred at room temperature (speed: 400rpm) for 18h, centrifuged to collect the precipitate, and freeze-dried to obtain PPR;

[0075] (2) Preparation of polyrotaxane: Dissolve amino-modified cholic acid (0.43g, 0.96mmol) in 4mL DMF, and add dropwise to pseudopolyrotaxane PPR (4g, 0.27mmol, molar mass of activated ester unit is 0.54 mmol) powder, stirred until a yellow viscous solution was formed, triethylamine (8 μL, 0.054 mmol) was added dropwise to catalyze, ultrasonic treatment was performed for 1 h (ultrasonic frequency: 40 kHz, power: 200 W), reaction was carried out at 40°C for 36 h, and ether precipitated. The precipitate was dissolved in a small ...

Embodiment 3

[0080] (1) Preparation of pseudopolyrotaxanes: Dissolve activated ester-modified polyethylene glycol (1 g, 0.43 mmol) in 5 mL of deionized water, and add dropwise to α-cyclodextrin (10.44 g, 10.73 mmol) In the saturated solution, a white precipitate formed after a few minutes, sonicated for 2h (ultrasonic frequency: 40kHz, power: 100W), stirred at room temperature (speed: 300rpm) for 24h, centrifuged to collect the precipitate, and freeze-dried to obtain PPR;

[0081] (2) Preparation of polyrotaxane: Dissolve amino-modified cholic acid (0.41g, 0.9mmol) in 4mL DMF, and add dropwise to pseudopolyrotaxane PPR (4g, 0.18mmol, molar mass of activated ester unit is 0.36mmol ) powder, stirred until a yellow viscous solution was formed, triethylamine (8 μL, 0.054 mmol) was added dropwise to catalyze, ultrasonic treatment was performed for 2 h (ultrasonic frequency: 40 kHz, power: 100 W), reaction was carried out at 50 °C for 24 h, and ether precipitated. The precipitate was dissolved i...

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Abstract

The invention belongs to the technical field of biological medicine and discloses modified polyrotaxane, a medicine carrier micelle based on polyrotaxane and a preparation method and application of the micelle. The preparation method of the micelle includes the steps of (1) preparing hydrophilic modified polyrotaxane, wherein hydroxide radical of epoxy dextrin units in polyrotaxane is subjected toa reaction with a modifier, and the modifier is dicarboxylic anhydride; (2) making hydrophilic modified polyrotaxane subjected to amidation with a tumor-targeted ligand unit in water to obtain an amphipathic grafting product; (3) making hydrophobic antitumor medicine buried in the amphipathic grafting product to form and obtain the polyrotaxane medicine carrier micelle. Polyrotaxane is obtained after end capping is conducted by an end-capping reagent on quasi-polyrotaxane prepared by mixing active-ester-modified polyethylene glycol and cyclodextrin. The micelle is stable in structure, capableof carrying hydrophobic medicine, excellent in medicine encapsulating capability and high in encapsulation efficiency and has a targeting property. Meanwhile, the micelle has extremely low cytotoxicity and excellent blood compatibility.

Description

technical field [0001] The invention belongs to the technical field of biomedical materials, and specifically relates to a modified polyrotaxane, a targeted drug-loaded micelle based on the polyrotaxane, a preparation method and application thereof. Background technique [0002] Malignant tumors are one of the major diseases that seriously endanger human life and health. According to statistics, the number of new cases and deaths of malignant tumors is increasing year by year, and the situation is grim. The main methods of tumor treatment include surgery, radiotherapy, chemotherapy, etc., among which chemotherapy is the most widely used. However, as a systemic treatment, chemotherapy lacks targeting and selectivity in the course of treatment, leading to serious side effects. In addition, some chemotherapeutic drugs also have problems such as low solubility and poor stability, which seriously limit their clinical application. At present, nanomicelles with core-shell structu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G83/00A61K9/107A61K47/40A61K31/704A61P35/00
CPCA61K9/1075A61K31/704A61K47/40A61P35/00C08G83/007
Inventor 任力刘卅贾永光金家宏
Owner SOUTH CHINA UNIV OF TECH
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