Double-drug skeleton polymer as well as preparation method and application thereof

一种聚合物、骨架的技术，应用在双药骨架聚合物及其制备和应用领域，能够解决药物比难以掌控等问题

Active Publication Date: 2020-11-13
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the current multi-drug carriers can rarely maintain a constant drug ratio in the complex systemic circulation, which is due to the different hydrophilicity and hydrophobicity of different drugs, which have different effects in the process of entrapment, administration, systemic circulation, and reaching the target. The pharmacokinetic characteristics will eventually lead to the difficulty of controlling the ratio of drugs acting on the target, which has become a major limiting factor in the development of combination chemotherapy

Method used

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Examples

Experimental program
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Embodiment

[0054] A kind of double-drug skeleton polymer, its preparation method comprises the following steps (synthetic route such as figure 1 shown):

[0055] 1) Disperse 0.5g of mitoxantrone (MTO) and 5mL of triethylamine in 100mL of methanol, then disperse 1.0g of di-tert-butyl dicarbonate in 10mL of tetrahydrofuran and add dropwise to the reaction system, dropwise After the addition was completed, react at 25°C for 16 hours, remove methanol by rotary evaporation, redissolve the solid obtained by rotary evaporation with 200 mL of ethyl acetate and transfer it to a separatory funnel, then wash the organic phase with saturated potassium carbonate solution 3 times, and then use silica gel chromatography After purification (the mobile phase is composed of n-hexane, ethyl acetate and methanol according to the volume ratio of 10:5:1) and vacuum-dried, the mitoxantrone ((Boc) 2 -MTO);

[0056] 2) Disperse 100mg (0.65mmol) of 2,2'-dithiodiethanol and 282mg (2.3mmol) of 4-dimethylaminopyri...

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Abstract

The invention discloses a double-drug skeleton polymer as well as a preparation method and application thereof. The double-drug skeleton polymer can be self-assembled in a water phase to form nano-micelles and is used as a double-drug transport carrier, specific response drug release can be realized on a reductive microenvironment of tumor tissues, and two drugs can be released in a stable and accurate proportion.

Description

technical field [0001] The invention relates to a double-drug skeleton polymer and its preparation method and application. Background technique [0002] Chemotherapy is the abbreviation of chemical drug therapy. It is a treatment method that uses chemical drugs to prevent the proliferation, invasion, and metastasis of cancer cells until it finally kills cancer cells. Together with surgery and radiotherapy, it is called the three major treatment methods for cancer. However, due to the multidrug resistance of the tumor and the strong side effects of the drug itself, the use of a single chemotherapy drug has considerable limitations. Combination chemotherapy is a common means to improve the therapeutic effect and overcome multidrug resistance. The study found that the combination of drugs with different mechanisms of action can produce synergistic effects, which can improve target selectivity and prevent the occurrence of tumor drug resistance, and the use of drugs with non-ov...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/334A61K47/69A61K47/59A61K31/12A61K31/136A61P35/00
CPCA61K31/12A61K31/136A61K47/59A61K47/6907A61P35/00C08G65/3348A61K2300/00
Inventor 袁友永俞方舟涂雅兰肖炫姜茂麟
Owner SOUTH CHINA UNIV OF TECH
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