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A nano-targeted drug carrier, preparation method and application thereof

A targeting and carrier technology, applied in pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems that anti-tumor drugs do not have tumor tissue-targeting effects, affect drug bioavailability, and cannot achieve anti-tumor effects

Active Publication Date: 2020-06-19
合肥仟金草生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Antineoplastic drugs are usually hydrophobic small molecular organic substances, which need to be solubilized by organic solvents when administered, which will cause toxic and side effects on the body and seriously affect the bioavailability of the drug. While killing tumor cells, it will also produce toxicity to normal cells, causing serious side effects and failing to achieve a good anti-tumor effect

Method used

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  • A nano-targeted drug carrier, preparation method and application thereof
  • A nano-targeted drug carrier, preparation method and application thereof
  • A nano-targeted drug carrier, preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Experimental principle such as figure 1 , the specific preparation method is as follows:

[0032] a) Reaction step: get 3.0g soluble starch (polymerization degree is 400-800, relative molecular weight is 10 4 -10 6 g / mol), 1.5g biotin and 0.75g 18-β glycyrrhetinic acid were dissolved in 150mL dimethyl sulfoxide and stirred to dissolve, then 0.5g N,N'-dicyclohexylcarbodiimide and 0.25g 4- After dimethylaminopyridine was reacted at room temperature at a stirring speed of 150 rpm for 48 hours, the initial product was obtained;

[0033] b) Dialysis process: put the initial product prepared in the reaction step a) into a dialysis bag (MW8000-14000) and put it into deionized water for dialysis, change the deionized water every 4 hours, continue dialysis for 24 hours, and suction filter. And wash with anhydrous ether and deionized water 3 times respectively to obtain the washings, repeat the above steps 3 times, vacuum freeze-dry the washings for the third time at -50°C to ...

Embodiment 2

[0043] a) Reaction step: get 2.75g soluble starch (degree of polymerization is 400-800, relative molecular weight is 10 4 -10 6 g / mol), 1.25g biotin and 0.63g 18-β glycyrrhetinic acid were dissolved in 150mL DMSO and stirred to dissolve, then 0.6g N,N'-dicyclohexylcarbodiimide and 0.25g 4- After dimethylaminopyridine was reacted at room temperature at a stirring speed of 150 rpm for 48 hours, the initial product was obtained;

[0044] b) Dialysis process: put the initial product prepared in the reaction step a) into a dialysis bag (MW8000-14000) and put it into deionized water for dialysis, change the deionized water every 4 hours, continue dialysis for 24 hours, and suction filter. And wash with anhydrous ether and deionized water 3 times respectively to obtain the washings, repeat the above steps 3 times, vacuum freeze-dry the washings for the third time at -50°C to constant weight, and obtain glycyrrhetinic acid-modified biotin hydrophobic Modified soluble starch;

[004...

Embodiment 3

[0047] a) Reaction step: get 2.5g soluble starch (polymerization degree is 400-800, relative molecular weight is 10 4 -10 6 g / mol), 1.75g ​​biotin and 0.87g 18-β glycyrrhetinic acid were dissolved in 150mL dimethyl sulfoxide and stirred to dissolve, then added 0.75g N,N'-dicyclohexylcarbodiimide and 0.25g 4- After dimethylaminopyridine was reacted at room temperature at a stirring speed of 150 rpm for 48 hours, the initial product was obtained;

[0048] b) Dialysis process: put the initial product prepared in the reaction step a) into a dialysis bag (MW8000-14000) and put it into deionized water for dialysis, change the deionized water every 4 hours, continue dialysis for 24 hours, and suction filter. And wash with anhydrous ether and deionized water 3 times respectively to obtain the washings, repeat the above steps 3 times, vacuum freeze-dry the washings for the third time at -50°C to constant weight, and obtain glycyrrhetinic acid-modified biotin hydrophobic Modified solu...

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Abstract

The invention discloses a nano targeted drug carrier, a preparation method and an application of carrier. The structural formula of the drug carrier is as shown in the specification. Compared with the prior art, the drug carrier has a stable morphological structure and can effectively entrap hydrophobic anti-tumor drugs, selectivity of the anti-tumor drugs is enhanced by the targeting function of a targeting group in the drug carrier, anti-tumor effects are enhanced, toxic and side effects on normal tissues are decreased, and drug-loaded nanoparticles can retain tumor tissues for a long time and release drugs for a long time to enhance efficacy.

Description

technical field [0001] The invention relates to a drug carrier, a preparation method and an application thereof, in particular to a nano-targeted drug carrier, a preparation method and an application thereof. Background technique [0002] Antineoplastic drugs are usually hydrophobic small molecular organic substances, which need to be solubilized by organic solvents when administered, which will cause toxic and side effects on the body and seriously affect the bioavailability of the drug. While killing tumor cells, it also produces toxicity to normal cells, causing serious side effects and failing to achieve a good anti-tumor effect. Contents of the invention [0003] The first technical problem to be solved by the present invention is to prepare nano-drug carriers capable of carrying hydrophobic anti-tumor drugs and targeting tumor tissues, so as to increase the water solubility of anti-tumor drugs and reduce the side effects on normal cells. [0004] The second technica...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K31/704A61K47/54A61P35/00
CPCA61K31/704
Inventor 龚仁敏许桐杨倩倩桂黎明
Owner 合肥仟金草生物科技有限公司
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