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Anti-tumor macromolecule bonding drug with multidrug synergistic effect and preparation method thereof

A synergistic, anti-tumor drug technology, applied in the direction of anti-tumor drugs, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of poor anti-cancer activity and low bioavailability of drugs, Achieve less side effects, inhibit tumor cell growth, and improve therapeutic effect

Active Publication Date: 2016-12-07
XIANGTAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] For traditional tumor chemotherapy, a single chemotherapy drug is used, or some drug carriers for combined administration are mostly non-degradable polymers, and their bonding methods are all physically encapsulated, resulting in low bioavailability of the drug to the human body , poor anti-cancer activity and other defects; the purpose of the present invention is to provide a polymer-bonded drug composed of a biodegradable polymer as a carrier and loaded with multiple anti-tumor drugs at the same time. The synergistic effect improves the anticancer activity while reducing the side effects of chemotherapy, and the polymer bonded drug has good biocompatibility, high and controllable drug loading, and can be applied to clinical research

Method used

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  • Anti-tumor macromolecule bonding drug with multidrug synergistic effect and preparation method thereof
  • Anti-tumor macromolecule bonding drug with multidrug synergistic effect and preparation method thereof
  • Anti-tumor macromolecule bonding drug with multidrug synergistic effect and preparation method thereof

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Embodiment 1

[0054] 1. Preparation of polyethylene glycol monomethyl ether-b-polylactide-b-polyα-bromocaprolactone copolymer:

[0055] First, 0.80 g of lactide of norbornene pendant group and 1.00 g of polyethylene glycol monomethyl ether (mPEG) were added to an ampoule that had been vacuum-baked three times under nitrogen protection, and then 1 mL of purified DCM to make it completely dissolved, inject 1 mL of TBD solution containing initiator prepared from purified DCM, react at room temperature for 48 h, settle with anhydrous ether for 3 times, centrifuge and vacuum dry to obtain polyethylene glycol monomethyl ether-b- Polylactide diblock polymer, structurally characterized as figure 1 As shown, the molecular weight distribution is image 3 . Then, use it as a macromolecular initiator to initiate the polymerization of α-bromocaprolactone under the same polymerization conditions to obtain a polyethylene glycol monomethyl ether-b-polylactide-b-polyα-bromocaprolactone copolymer , whose ...

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Abstract

The invention discloses an anti-tumor macromolecule bonding drug with a multidrug synergistic effect and a preparation method thereof. The preparation method comprises the steps of sequentially triggering the polymerization of lactide containing norbornene and alpha bromination caprolactone through methoxy polyethylene glycol so as to obtain a triblock copolymer; modifying a p-nitrophenyl formic ether lateral group and a carboxyl lateral group on the triblock copolymer so as to obtain a polymeric carrier; bonding the polymeric carrier, an anti-tumor drug containing hydroxyl and an anti-tumor drug containing amino so as to obtain the anti-tumor macromolecule bonding drug. The preparation method is simple to operate, moderate in reaction conditions, less in side reaction, high in yield, large in drug loading capacity, controllable, and high in product purity; according to the prepared anti-tumor macromolecule bonding drug, the anti-tumor activity is improved through a various signal channel effect (the synergistic effect), and meanwhile, due to the joint action of various drugs, the dosage of each drug can be reduced, so that a toxic and side effect of chemotherapy is reduced.

Description

technical field [0001] The invention relates to an anti-tumor drug, in particular to an anti-tumor polymer bonded drug with multi-drug synergy and a preparation method thereof, and belongs to the field of biomedical polymer materials. Background technique [0002] Cancer is a global public health problem. In the past three decades, the incidence of cancer in the world has increased at a rate of 3-5% per year. In the 21st century, tumors have become the number one cause of human death. Chemotherapy is one of the three major treatment methods for tumors, and it is an important method in current tumor treatment. Although chemotherapy has made great progress in the treatment of tumors, there are still some obstacles in its clinical application. For example, traditional tumor chemotherapy uses a single chemotherapeutic drug, and its main drawback is that the treatment of a single drug often activates and strengthens the survival pathways of other aspects of tumor cells, resulti...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/337A61K31/407A61K31/4745A61K31/7048A61P35/00A61K31/704C08G63/08C08G63/78C08G63/91
CPCA61K31/337A61K31/407A61K31/4745A61K31/704A61K31/7048C08G63/08C08G63/78C08G63/912
Inventor 张雪飞赵碧云
Owner XIANGTAN UNIV
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