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Degradable organic silicon nanocapsule drug carrier as well as preparation method and application thereof

A nanocapsule and organosilicon technology, applied in the field of biomedicine, can solve the problems of difficulty in co-carrying multiple drugs and refractory degradation, and achieve the effects of reducing multidrug resistance of tumor cells, simple operation and low equipment requirements.

Inactive Publication Date: 2015-12-02
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the defects that the existing silicon material drug carriers are difficult to realize multiple drug co-carrying and refractory to degradation, the present invention provides an organic compound with redox sensitivity, degradability, multiple drug co-carrying function and excellent biocompatibility. Silicon nanocapsule drug carrier and its preparation method and application

Method used

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  • Degradable organic silicon nanocapsule drug carrier as well as preparation method and application thereof
  • Degradable organic silicon nanocapsule drug carrier as well as preparation method and application thereof
  • Degradable organic silicon nanocapsule drug carrier as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] (1) Fluorescent labeling of chitosan

[0028] Rhodamine B was used as the labeling dye, and the weight-average molecular weight was 4 × 10 using amide condensation.5 Chitosan labeling of Da. The specific preparation process is as follows: Weigh 0.479g of Rhodamine B, dissolve it in 10mL of anhydrous N-dimethylformamide (DMF), add 0.247g of N,N'-dicyclohexylcarbodiimide (DCC), N -Hydroxysuccinimide (NHS) 0.138g, reacted at 0°C for 24h in the dark. Filter and take the filtrate.

[0029] Weigh M w =4×10 5 Da chitosan 0.805g, add 80mL of water and 5mL of 1mol / L hydrochloric acid to dissolve, add the filtrate, avoid light and react at 50°C for 48h.

[0030] Add NaOH solution to adjust the pH to alkaline, precipitate chitosan, collect the precipitate by centrifugation, wash with secondary water, and centrifuge, repeating 3 times. Add 100mL of water and 5mL of 1mol / L hydrochloric acid to dissolve the chitosan after the reaction, using a molecular weight cut-off of 1.4×10 ...

Embodiment 2

[0045] (1) Fluorescent labeling of chitosan

[0046] Rhodamine B was used as the labeling dye, and the weight-average molecular weight was 2 × 10 using amide condensation. 5 Chitosan labeling of Da. The specific preparation process is as follows: Weigh 0.479g of Rhodamine B, dissolve it in 10mL of anhydrous DMF, add 0.247g of DCC and 0.138g of N-NHS, and react in the dark at 0°C for 24h. Filter and take the filtrate.

[0047] Weigh M w =2×10 5 Da chitosan 0.805g, add 80mL of water and 5mL of 1mol / L hydrochloric acid to dissolve, add the filtrate, avoid light and react at 50°C for 48h.

[0048] Add NaOH solution to adjust the pH to alkaline, precipitate chitosan, collect the precipitate by centrifugation, wash with secondary water, and centrifuge, repeating 3 times. Add 100mL of water and 5mL of 1mol / L hydrochloric acid to dissolve the chitosan after the reaction, using a molecular weight cut-off of 1.4×10 4 The dialysis bag of Da was dialyzed until the external solution ...

Embodiment 3

[0063] (1) Fluorescent labeling of chitosan

[0064] Rhodamine B was used as the labeling dye, and the weight-average molecular weight was 4 × 10 using amide condensation. 5 Chitosan labeling of Da. The specific preparation process is as follows: Weigh 0.479g of Rhodamine B, dissolve it in 10mL of anhydrous N-dimethylformamide (DMF), add 0.247g of N,N'-dicyclohexylcarbodiimide (DCC), N -Hydroxysuccinimide (NHS) 0.138g, reacted at 0°C for 24h in the dark. Filter and take the filtrate.

[0065] Weigh M w =4×10 5 Da chitosan 0.805g, add 80mL of water and 5mL of 1mol / L hydrochloric acid to dissolve, add the filtrate, avoid light and react at 50°C for 48h.

[0066] Add NaOH solution to adjust the pH to alkaline, precipitate chitosan, collect the precipitate by centrifugation, wash with secondary water, and centrifuge, repeating 3 times. Add 100mL of water and 5mL of 1mol / L hydrochloric acid to dissolve the chitosan after the reaction, using a molecular weight cut-off of 1.4×1...

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Abstract

The invention discloses a degradable organic silicon nanocapsule drug carrier as well as a preparation method and application thereof. The carrier has a core-shell structure, wherein the core is a nano particle drug; the shell is a degradable organic silicon nanocapsule layer containing a large amount of disulfide bonds; the degradable organic silicon nanocapsule layer wraps small molecule drugs; the shell contains disulfide bonds, disulfide bonds can be in oxidation-reduction reaction with glutathione that excessively expresses in cancer cells, therefore the shells of capsules are disintegrated, drugs wrapped in the shells can be slowly released, while disulfide bonds cannot be disintegrated due to the fact that the content of glutathione outside cells is inadequate, the internal drugs can be prevented from being influenced by the external environment, the in vivo circulation time can be prolonged, and the purpose of releasing drugs in the tumor cells can be achieved. According to the degradable organic silicon nanocapsule drug carrier as well as the preparation method and application thereof, provided by the invention, the disadvantages that the conventional silicone drug carrier cannot be degraded and has difficulty in metabolism in biological bodies are overcome, an excellent dual drug carrying and tumor specificity transferring ability and a good biocompatibility are achieved, and a broad application prospect in the field of cancer treatment is further achieved.

Description

technical field [0001] The invention relates to a degradable organosilicon nanocapsule drug carrier and a preparation method and application thereof, belonging to the field of biomedicine. Background technique [0002] There are more than 32 million surviving cancer patients in the world, more than 14 million new cancer cases are added every year, and more than 8 million cancer patients die. Cancer has become one of the main causes of human death. Conventional treatment methods mainly include surgery, chemotherapy and radiotherapy. Chemotherapy is also called drug therapy. Commonly used drugs cannot distinguish between normal cells and cancer cells. The half-life of drugs is short, so patients must use drugs in large doses and frequently, and their side effects are relatively large. The development of new drug carriers is one of the focuses of cancer treatment research. Drug carriers can carry the drug to the target area for sustained release, which can reduce the dosage o...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/48A61K47/24A61P35/00
Inventor 张先正李江蓝曾旋
Owner WUHAN UNIV
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