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Block polymer, drug carrier containing same, and preparation method and application of block polymer

A technology of block polymers and polymers, which is applied in the direction of medical preparations, drug combinations, and pharmaceutical formulations of non-active ingredients, and can solve the problems of EPR effect drug release, wide molecular weight distribution, and uncontrollable polymer molecular weight, etc.

Active Publication Date: 2017-10-27
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since ordinary free radical polymerization is commonly used in the preparation of PHPMA carriers at present, the molecular weight of the prepared polymers is uncontrollable and the molecular weight distribution is very wide, which will have a serious impact on the EPR effect of the carrier and the release of drugs, and further affect the drug release. Therapeutic Effects on Tumors

Method used

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  • Block polymer, drug carrier containing same, and preparation method and application of block polymer
  • Block polymer, drug carrier containing same, and preparation method and application of block polymer
  • Block polymer, drug carrier containing same, and preparation method and application of block polymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] The synthesis of embodiment 1,4-dodecyl trithioester group-4-cyanopentanol (CTA-OH)

[0065]

[0066] Take a 1000mL round bottom flask, add 14.6gKOH into 450mL water, then slowly add 40.4g (48mL) dodecyl mercaptan to obtain an emulsified liquid solution, and slowly add 0.8g methyl trioctylammonium chloride and 14.4g ( 12.06mL) CS 2The mixed solution was observed to change from earthy yellow to yellow and finally to orange. After reacting at room temperature for 1 hour, cool to -5°C in an ice-salt bath (NaCl), slowly add 20 g of p-toluenesulfonyl chloride, keep the reaction at -5°C for 2 hours, then react in a water bath at 45°C for 45 minutes to form an orange oily product. Cool in an ice-water bath for 1 hour to form a solid product, which was filtered with suction and washed several times with ice water to remove water-soluble impurities. Then recrystallize and purify in acetone: gradually add acetone in a water bath at 61°C, and stir continuously until the solut...

Embodiment 2

[0069] Embodiment 2, the synthesis of ethylene glycol single 4-dodecyl trithioester group-4-cyanovalerate

[0070]

[0071] Take 5 g of didodecyl bis-trithiocarbonate prepared in Example 1 and 5 g of 4,4′-azobis(4-cyanovaleric acid) and dissolve them in 150 mL of ethyl acetate, reflux and react in the dark for 24 hours , the reaction temperature was 95° C., and the obtained final product was separated, purified and recovered by column chromatography again, and the mobile phase was petroleum ether: ethyl acetate = 2:1. Gained product 4.03g and 3.1g ethylene glycol are dissolved in 50mL anhydrous dichloromethane, add 4.5g dicyclohexylcarbodiimide (DCC) and 0.2g4-dimethylaminopyridine (DMAP) to catalyze and carry out esterification reaction, reaction After 48 hours, the produced by-product dicyclohexylurea was removed by filtration, and the obtained final product was separated, purified and recovered by column chromatography again, and the mobile phase was petroleum ether:ethy...

Embodiment 3

[0072] Embodiment 3, the synthesis of ethylene glycol mono-2-bromoisobutyrate

[0073]

[0074] Dissolve 9.3g of ethylene glycol and 2.02g of triethylamine in 100mL of dichloromethane, use an ice-water bath to lower the temperature of the system to 5°C, and slowly add 4.6g of 2-bromoisobutyryl bromide dropwise using a constant pressure dropping funnel. React for 24 hours after completion. After the reaction was completed, the generated triethylamine hydrobromide was removed by filtration, and the filtrate was washed three times with 1% sodium bicarbonate aqueous solution and pure water respectively. The collected organic phase was dried by adding anhydrous sodium sulfate, and then concentrated by rotary evaporation to remove the organic solvent to obtain a pure product.

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Abstract

The invention discloses a block polymer, a drug carrier containing the same, and a preparation method and application of the block polymer. According to the block polymer, a copolymer with controllable copolymerization components, controllable molecular weight and narrow molecular weight distribution (the molecular weight distribution d<1.2) are obtained by adopting ring-opening polymerization (ROP) and reversible addition fragmentation chain transfer (RAFT) or atom transfer radical polymerization (ATRP) method. The drug carrier prepared from the polymer has relatively good slow release and tumor passive targeting effects, so that the polymer can be applied to targeting transportation of anti-tumor drugs; and the polymer has a high targeting property and good biocompatibility and is an anti-tumor targeting drug carrier with good performance.

Description

technical field [0001] The invention relates to a drug carrier, in particular to a block polymer, a drug carrier containing it, a preparation method and application thereof. Background technique [0002] Cancer is a malignant tumor. It is due to the destruction of the normal proliferation mechanism of human cells, resulting in malignant proliferation of cells, imbalance of human metabolism, damage to the structure and function of tissues and organs, and eventually patients will die due to organ failure. With economic and social development and population aging, cancer has become the number one killer of human health in developed and developing countries, among which breast cancer, lung cancer and rectal cancer have the highest incidence rates in developing countries. At present, the prevention and treatment of cancer are mainly through early diagnosis and treatment, tobacco control, and the use of vaccines (liver cancer, cervical cancer), etc. economic and social burdens. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F293/00C08G63/08A61K47/34A61K49/00A61P35/00
Inventor 甘志华喻青松杜楠管书丽
Owner BEIJING UNIV OF CHEM TECH
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