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Enzyme-sensitive and redox-sensitive dual response type copolymer as well as preparation method and application thereof

A dual-response, enzyme-sensitive technology, applied in the fields of polymer chemistry and pharmaceutical preparations, can solve problems such as lack of pertinence, worsening side effects, and limited effects, and achieve good biocompatibility, reduce toxic side effects, and improve environmental sensitivity. Effect

Inactive Publication Date: 2018-11-06
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the use of BSO has limited and untargeted effects, and the drug will also reduce the content of GSH in normal cells, which further worsens the side effects caused by radiotherapy and chemotherapy

Method used

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  • Enzyme-sensitive and redox-sensitive dual response type copolymer as well as preparation method and application thereof
  • Enzyme-sensitive and redox-sensitive dual response type copolymer as well as preparation method and application thereof
  • Enzyme-sensitive and redox-sensitive dual response type copolymer as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Polyacrylic acid-VC-SS-vitamin E succinate copolymer PAA-VC-SS-VES

[0035]

[0036] (1) The preparation method is as follows:

[0037] 1. Vitamin E succinate derivative VES-SS-NH 2 (Intermediate A) synthetic, concrete steps are as follows:

[0038]

[0039] Dissolve vitamin E succinate (VES) (5.30g, 10mmol) in 100mL of dichloromethane, stir in a 250mL round-bottomed flask until completely dissolved, add EDC (13mmol) and HOBT (13mmol) in an ice bath, and store in room temperature. Stir overnight, add cystamine dihydrochloride (6.75g, 30mmol) to the reaction solution, add 30mL of methanol to aid dissolution, add triethylamine to adjust the pH to 7-8, stir for 24h, the obtained product is treated with 1mol / L NaHCO 3 Wash with aqueous solution, dry the organic layer by adding anhydrous magnesium sulfate, filter, remove dichloromethane by rotary evaporation under reduced pressure at 40°C, and dry in vacuum to obtain 4.72g vitamin E succinate derivative VE...

Embodiment 2

[0051] Embodiment 2 PAA-VC-SS-VES micelles and drug-loaded nano micelles

[0052] (1) Determination of appearance, particle size and potential of PAA-VC-SS-VES micelles

[0053] Get 10mg PAA-VC-SS-VES copolymer and dissolve in 10mL distilled water, stir at room temperature for ten minutes, the appearance of the preparation is clear and transparent, as Figure 2a It shows that the solubility of the copolymer is excellent. Irradiating the preparation with a beam of light showed a bright path, indicating that the PAA-VC-SS-VES copolymer can spontaneously form nanomicelles in water (such as Figure 2b shown). Detect with the Malvern laser particle size scanner, record that this nano-micelle particle size is 147.7nm (as Figure 2c shown), the potential is -23.2mV (such as Figure 2d shown), indicating that the nano-micelle has a small particle size, can be enriched at the tumor site, and has good stability and dispersion.

[0054] (2) Preparation of PAA-VC-SS-VES drug-loaded n...

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Abstract

The invention discloses an enzyme-sensitive and redox-sensitive dual response type copolymer as well as a preparation method and application thereof and belongs to the fields of high polymer chemistryand pharmaceutical preparations. The preparation method in the invention comprises the following steps: binding polyacrylic acid and vitamin E succinate by utilizing valine-citrulline (Val-Cit, VC) fragments capable of being specifically hydrolyzed by cathepsin B and disulfide bonds capable of being reduced by glutathione, thereby obtaining the dual sensitive type copolymer polyacrylic acid-VC-SS-vitamin E succinate (PAA-VC-SS-VES). The copolymer is excellent in biocompatibility and high in sensitivity, can be self-assembled to form nano-micelles in water, can be coated with hydrophobic drugs, is mainly applied to treating tumor related diseases and has an effect of intelligently releasing the drugs.

Description

technical field [0001] The present invention relates to the fields of pharmaceutical preparations and polymer chemistry, in particular to a dual sensitive copolymer with enzyme sensitivity and redox sensitivity: polyacrylic acid-VC-SS-vitamin E succinate (PAA-VC-SS-VES ) and its preparation method and application. Background technique [0002] Cancer is the number one disease threatening human life today. The purpose of tumor treatment is to kill cancer cells. Since tumor cells are highly similar to normal cells and have higher vitality, existing non-surgical therapies need to continue to improve the specificity of tumor cells, which requires anticancer drugs It has higher targeting, which is also the challenge that the pharmaceutical industry and scientists have been facing. Targeted therapy for tumors is to selectively concentrate drugs on tumor tissues, thereby improving the efficacy of drugs while reducing side effects on normal tissues. The nano-drug delivery system ...

Claims

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Application Information

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IPC IPC(8): C08F8/34C08F120/06C07D311/72A61K9/107A61K47/32A61K31/337A61P35/00
CPCA61K9/1075A61K31/337A61K47/32A61P35/00C07D311/72C08F8/34C08F120/06Y02P20/55
Inventor 陈立江宋柯王欣梁啸
Owner LIAONING UNIVERSITY
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