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A kind of carrier-free hyperbranched macromolecular polymer and its preparation method

A macromolecular polymer and carrier-free technology, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problem of cumbersome synthetic routes, unsimple synthetic methods, and system drug loading rate. Not high problem, to solve the effect of low drug loading

Active Publication Date: 2021-12-07
NORTHWESTERN POLYTECHNICAL UNIV
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0003] Document 1 "Xiujuan Xi, Shiqi Hu, Zhuxian Zhou and Youqing Shen et al.Dendrimers with the protocatechuic acid building block for anticancer drugdelivery[J].Journal of Materials Chemistry B,2016,4,5236-5245." A single protocatechuic acid drug is used as a unit to construct a polymer drug with a dendritic morphology. However, the synthetic route of this method is cumbersome and the synthetic method is not simple enough.
[0004] Document 2 "Yajun Huang, Xiaokang Ding, Yu Qi, Bingran Yu and Fu-JianXu. Reduction-responsive multifunctional hyperbranched polyaminoglycosides with excellent antibacterial activity, biocompatibility and gene transfectioncapability [J]. Biomaterials, 2016, 104:13 published" A polymer drug with a dendritic morphology is constructed using a single drug of the antibiotic gentamicin, tobramycin or neomycin, combined with a disulfide bond. to the role of combined treatment of disease
[0005] Document 3 "Xiaopin Duan, Jisheng Xiao, Qi Yin and Yaping Li et al.Smart pH-Sensitive and Temporal-Controlled Polymeric Micelles for Effective Combination Therapy of Doxorubicin and Disulfiram[J].ACS Nano,2013,7(7):5858- 5869." discloses a combined anti-cancer strategy using two drugs, doxorubicin and disulfiram, but the traditional method of physical coating with carriers leads to the disadvantages of low drug loading rate and unstable drug delivery.

Method used

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  • A kind of carrier-free hyperbranched macromolecular polymer and its preparation method
  • A kind of carrier-free hyperbranched macromolecular polymer and its preparation method
  • A kind of carrier-free hyperbranched macromolecular polymer and its preparation method

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Experimental program
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Effect test

Embodiment 1

[0042] Weigh 250mg of cystamine dihydrochloride and place it in a dry 100ml single-necked flask, add 5ml of methanol and 350mg of triethylamine, and stir for 30min under ice-bath conditions. Weigh 88 mg of di-tert-butyl dicarbonate into a beaker and dissolve it with 10 ml of methanol, and add it dropwise into a single-necked flask with a constant pressure dropping funnel. After reacting for 5 hours, add 10 ml of deionized water to terminate the reaction. The reaction solvent was removed by rotary evaporation under reduced pressure, then 30 ml of saturated sodium chloride solution was added, extracted three times with 50 ml of dichloromethane, and the organic phase was dried over anhydrous sodium sulfate. The resulting solid was directly applied to a silica gel column for separation. The solvent was evaporated to dryness with a rotary evaporator, and dried in a vacuum oven for 2 days to obtain 123 mg of cystamine with a single-tert-butoxycarbonyl-protected amino group as a pale...

Embodiment 2

[0050] Weigh 400mg of cystamine dihydrochloride and place it in a dry 100ml single-necked flask, add 8ml of methanol and 560mg of triethylamine, and stir for 30min under ice-bath conditions. Weigh 140 mg of di-tert-butyl dicarbonate into a beaker and dissolve it with 12 ml of methanol, and add it dropwise into a single-necked flask with a constant pressure dropping funnel. After reacting for 5 hours, add 10 ml of deionized water to terminate the reaction. The reaction solvent was removed by rotary evaporation under reduced pressure, then 30 ml of saturated sodium chloride solution was added, extracted three times with 50 ml of dichloromethane, and the organic phase was dried over anhydrous sodium sulfate. The resulting solid was directly applied to a silica gel column for separation. The solvent was evaporated to dryness with a rotary evaporator, and dried in a vacuum oven for 2 days to obtain 196 mg of cystamine with a single-tert-butoxycarbonyl-protected amino group as a pal...

Embodiment 3

[0057] Weigh 500mg of cystamine dihydrochloride and place it in a dry 100ml single-necked flask, add 10ml of methanol and 700mg of triethylamine, and stir for 30min under ice-bath conditions. Weigh 175 mg of di-tert-butyl dicarbonate into a beaker and dissolve it with 15 ml of methanol, and add it dropwise into a single-necked flask with a constant pressure dropping funnel. After reacting for 5 hours, add 10 ml of deionized water to terminate the reaction. The reaction solvent was removed by rotary evaporation under reduced pressure, then 30 ml of saturated sodium chloride solution was added, extracted three times with 50 ml of dichloromethane, and the organic phase was dried over anhydrous sodium sulfate. The obtained solid was directly applied to a silica gel column for separation, the solvent was evaporated to dryness with a rotary evaporator, and dried in a vacuum oven for 2 days to obtain 257 mg of cystamine with a single-terminal tert-butoxycarbonyl-protected amino group ...

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Abstract

The invention relates to a carrier-free hyperbranched macromolecular polymer and a preparation method. Two common hydrophobic drugs, methotrexate and chlorambucil, are used as basic elements to modify the structures of these two hydrophobic drugs. Modification, so that the structure contains dynamic covalent bonds "disulfide bond" and "ester bond", and then "A 2 +B 3 "method polymerization into hyperbranched macromolecular polymers, and finally self-assembled into a hyperbranched macromolecular drug-type carrier-free nano-drug self-delivery system, which provides a new idea for the construction of carrier-free nano-drug delivery systems and solves the current problem. There are problems such as low drug loading, high cytotoxicity, large toxic side effects on kidneys and other organs, and insufficient responsiveness in the drug loading of hyperbranched polymers.

Description

technical field [0001] The invention belongs to the field of polymer material synthesis and a preparation method of functional medicine, and relates to a carrier-free hyperbranched macromolecular polymer and a preparation method. Background technique [0002] Carrier-free nano-drug delivery system has the advantages of high drug loading, simple preparation strategy, precise structure, stable drug release, etc., and has become the main trend in the development of nano-drugs. Complete removal of inert excipients can not only increase the drug loading to 100%, greatly improving the therapeutic effect, but also effectively avoid the toxicity and immune response caused by the carrier. [0003] Document 1 "Xiujuan Xi, Shiqi Hu, Zhuxian Zhou and Youqing Shen et al.Dendrimers with the protocatechuic acid building block for anticancer drugdelivery[J].Journal of Materials Chemistry B,2016,4,5236-5245." A single protocatechuic acid drug is used as a unit to construct a polymer drug wi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G69/42A61K47/59A61K31/519A61K31/196A61P35/00
CPCA61K31/196A61K31/519A61K47/595A61P35/00C08G69/42A61K2300/00
Inventor 田威刘程飞庞俊李鹏翔李慧鑫
Owner NORTHWESTERN POLYTECHNICAL UNIV
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