Nanometer medicine-loaded micelle, nanometer anticancer medicine, methods for preparing nanometer medicine-loaded micelle and nanometer anticancer medicine and application of nanometer medicine-loaded micelle and nanometer anticancer medicine

A technology of nano-drug loading and anti-cancer drugs, which is applied in drug combination, drug delivery, and pharmaceutical formulations. Enhanced thermal effect, increased water solubility, enhanced therapeutic effect

Inactive Publication Date: 2017-05-17
SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] IR808 is a heptamethine dye, which has good absorption in the near-infrared region. When the IR808 dyes gather together, they can quickly generate a large amount of heat under 808nm excitation, so they are suitabl

Method used

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  • Nanometer medicine-loaded micelle, nanometer anticancer medicine, methods for preparing nanometer medicine-loaded micelle and nanometer anticancer medicine and application of nanometer medicine-loaded micelle and nanometer anticancer medicine
  • Nanometer medicine-loaded micelle, nanometer anticancer medicine, methods for preparing nanometer medicine-loaded micelle and nanometer anticancer medicine and application of nanometer medicine-loaded micelle and nanometer anticancer medicine
  • Nanometer medicine-loaded micelle, nanometer anticancer medicine, methods for preparing nanometer medicine-loaded micelle and nanometer anticancer medicine and application of nanometer medicine-loaded micelle and nanometer anticancer medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] In this example, nano drug-loaded micelles were prepared by the following method, as follows:

[0060] (1) 15g hyaluronic acid (HA, M W 5K) was dissolved in 5 L of deionized water, 25 g of adipic dihydrazide (ADH) was added to the aqueous solution, and the pH value was adjusted to 4.5 with 0.1 M hydrochloric acid solution under rapid stirring. 15 g of EDC was added to the above reaction solution, and the pH value was adjusted to 4.5 with 0.1 M hydrochloric acid solution, and then reacted at 25° C. for 1 h to obtain a white solid HA-ADH.

[0061] (2) Dissolve 8g HA-ADH in 2L formamide, activate 25g heptamethine cyanine dye (IR808) with EDC and NHS and dissolve it in a mixed solution of tetrahydrofuran and water, and add the mixed solution dropwise to the above In the formamide solution of HA-ADH, react at 25°C for 24h after the dropwise addition.

[0062] (3) The reaction solution is filtered under reduced pressure to remove large insoluble matter. The filtrate was pl...

Embodiment 2

[0064] In this example, nano drug-loaded micelles were prepared by the following method, as follows:

[0065] (1) 15g hyaluronic acid (HA, M W 10K) was dissolved in 5 L of deionized water, 45 g of adipic dihydrazide (ADH) was added to the aqueous solution, and the pH value was adjusted to 4.8 with 0.1 M hydrochloric acid solution under rapid stirring. Add 25 g of EDC to the above reaction solution, adjust the pH value to 4.8 with 0.1 M hydrochloric acid solution, and react at 30° C. for 0.5 h to obtain HA-ADH as a white solid.

[0066] (2) Dissolve 10g HA-ADH in 2L formamide, activate 40g heptamethine cyanine dye (IR808) with EDC and NHS and dissolve it in a mixed solution of tetrahydrofuran and water, and add the mixed solution dropwise to the above In the formamide solution of HA-ADH, react at 30°C for 24h after the dropwise addition.

[0067] (3) The reaction solution is filtered under reduced pressure to remove large insoluble matter. The filtrate was placed in a cellul...

Embodiment 3

[0069] In this example, nano drug-loaded micelles were prepared by the following method, as follows:

[0070] (1) 15g hyaluronic acid solution (HA, M W 10K) in 5L of deionized water, add 60g of adipic dihydrazide (adipate dihydrazide ADH) to its aqueous solution, and adjust the pH value to 4.6 with 0.1M hydrochloric acid solution under rapid stirring. Add 35 g of EDC to the above reaction solution, adjust the pH value to 4.6 with 0.1 M hydrochloric acid solution, and react at 18° C. for 5 h to obtain white solid HA-ADH.

[0071] (2) Dissolve 10g HA-ADH in 2L formamide, activate 60g heptamethine cyanine dye (IR808) with EDC and NHS, dissolve it in the formamide solution, and add the mixture dropwise to the above HA-ADH In the formamide solution, react at 20°C for 30h after the dropwise addition is complete.

[0072] (3) The reaction solution is filtered under reduced pressure to remove large insoluble matter. The filtrate was placed in a cellulose dialysis bag, and dialyzed ...

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Abstract

The invention provides nanometer medicine-loaded micelle, a nanometer anticancer medicine, methods for preparing the nanometer medicine-loaded micelle and the nanometer anticancer medicine and application of the nanometer medicine-loaded micelle and the nanometer anticancer medicine. The nanometer medicine-loaded micelle comprises hyaluronic acid and dye IR808. The dye IR808 is connected onto the hyaluronic acid by adipic dihydrazide groups. The hyaluronic acid is used as a hydrophilic shell for the nanometer medicine-loaded micelle, and the dye IR808 is used as a hydrophobic core for the nanometer medicine-loaded micelle, so that a shell-core structure can be formed. The nanometer medicine-loaded micelle, the nanometer anticancer medicine, the methods and the application have the advantages that tumor cell targeting, imaging and photothermal therapy effects can be realized by the nanometer medicine-loaded micelle; the nanometer medicine-loaded micelle can be used as a medicine carrier and can wrap hydrophobic anticancer medicines, so that the nanometer anticancer medicine can be formed, joint therapy effects of chemical medicine therapy and photothermal therapy can be realized, and curative effects can be improved for tumor; the methods for preparing the nanometer medicine-loaded micelle and the nanometer anticancer medicine are simple, and accordingly operation and popularization can be facilitated.

Description

technical field [0001] The invention belongs to the technical field of drug-loaded materials, and relates to a nano drug-loaded micelle, a nano anticancer drug and a preparation method and application thereof. Background technique [0002] Hyaluronic acid (HA) is a high-molecular polymer, which is an advanced straight-chain mucopolysaccharide composed of D-glucuronic acid and N-acetylglucosamine. It has unique physical and chemical properties and physiological functions. It has been used in medicine, Biomaterials have been widely used. There are various cell surface receptors, and selecting the appropriate receptor and its ligand is the key to realize the active targeting of drugs. CD44 is a widely studied cell surface receptor, which plays an important role in the occurrence and development of tumors. [0003] Current studies use high-molecular-weight hyaluronic acid as an active targeting factor, which binds to the CD44-specific receptor CD44 on the surface of tumor cells...

Claims

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Application Information

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IPC IPC(8): A61K47/61A61K47/69A61K41/00A61K49/00A61K49/22A61P35/00
CPCA61K41/0052A61K49/0002A61K49/0032A61K49/0082A61K49/227
Inventor 蔡林涛龚萍李三朋李文军孟晓青孙枝红邓冠军倪大鹏张佳丽朱婷
Owner SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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