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Preparation method of boron-containing nano targeted drug

A drug and nanotechnology, which is applied in the field of preparation of boron-containing nano-targeted drugs, can solve the problems of difficulty in preparing boron-containing drug composite systems, reduced radiotherapy effect, etc. easy effect

Active Publication Date: 2020-06-16
四川瑶天纳米科技有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

②Traditional radiotherapy requires oxygen to enhance the effect of biological radiation. However, due to the rapid and aggressive growth of malignant tumors, the blood supply of tumor tissue is often insufficient, resulting in local hypoxia, which reduces the effect of radiotherapy
However, due to the structural characteristics of boron-containing drugs, it is actually difficult to prepare a composite system containing boron-containing drugs. At present, there are few reports on the composite system containing boron-containing drugs with high swollen blood ratio.

Method used

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  • Preparation method of boron-containing nano targeted drug
  • Preparation method of boron-containing nano targeted drug

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1 Preparation of boron-containing nano-targeted drug of the present invention

[0043] 1. Synthesis of cRGD-PEG-PCL amphiphilic copolymer

[0044] refer to figure 1 Described flowchart, synthetic amphiphilic copolymer cRGD-PEG-PCL of the present invention, specific operation process is as follows:

[0045] (1) Use a 250mL three-necked flask to build a reaction device. Under nitrogen protection, N-hydroxysuccinimide-modified polyethylene glycol (ie NHS-PEG-OH, 0.5g, 0.1mmol) and ε-hexane Lactone (5 g, 43.86 mmol) was put into a three-necked flask, stirred magnetically under an oil bath, and the catalyst stannous octoate was added dropwise. Keep the temperature of the reaction system at about 130° C., and react for 6 hours. After the reaction, the reaction system was cooled to room temperature, and the final product was washed out with dichloromethane, transferred to a beaker, and then the product was precipitated with petroleum ether overnight. The next da...

experiment example 1

[0054] Experimental example 1 The swelling and blood ratio test of boron-containing nano-targeted drug of the present invention

[0055] (1) Experimental method:

[0056] Taking the boron-containing nano-targeted drug prepared in Example 1 as the object, the tumor-to-blood ratio was tested by inductively coupled plasma atomic emission spectrometry (ICP-AES).

[0057] (2) Experimental results:

[0058] The results show that the tumor-to-blood ratio of the boron-containing nano-targeted drug prepared in Example 1 of the present invention is 4.1:1, which is much higher than that of free BPA.

[0059] In summary, the present invention provides a method for preparing boron-containing nano-targeted drugs, which is simple in process, mild in synthesis conditions, and conducive to expanded production. Compared with free BPA, the tumor-to-blood ratio of the boron-containing nano-targeted drug prepared by the method of the present invention is significantly improved, up to 4.1:1, indi...

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Abstract

The invention relates to a preparation method of a boron-containing nano targeted drug, which comprises the following steps: (1) dissolving an amphiphilic polymer in an organic solvent to obtain an organic solution; adding a boron-containing drug into an aqueous solution containing an emulsifier, uniformly mixing, dropwise adding the obtained system into the above organic solution, and stirring toobtain a w / o emulsion; (2) dropwise adding the w / o emulsion into another aqueous solution containing the emulsifier, stirring, and then removing the organic solvent to obtain a w / o / w double emulsion;and freeze-drying the w / o / w double emulsion to obtain the boron-containing nano targeted drug. The preparation process of the boron-containing nano targeted drug is simple and convenient, the synthesis condition is mild, and expanded production is facilitated. Compared with free BPA, the prepared nano targeted drug has the advantages that the hematoma ratio is remarkably increased and reaches upto 4.1: 1, the tumor treatment effect can be remarkably improved, and the nano targeted drug has very good application prospects when being independently used as an anti-tumor drug and being combinedwith paclitaxel and other anti-tumor drugs for use.

Description

technical field [0001] The invention belongs to the field of drug delivery systems, and in particular relates to a preparation method of a boron-containing nano-targeted drug. Background technique [0002] Due to the difficulty of surgery and drug treatment, sensitive lesion site, easy to cause complications, low cure rate but high morbidity and mortality, the treatment of malignant tumors has become a major problem in the world. Recently, researchers found that compared with traditional treatment methods, boron neutron capture therapy (BNCT) showed excellent effect on malignant tumors. [0003] Neutron capture therapy is to make corresponding pro-tumor drugs from nuclides with large neutron reaction cross-sections, and inject the drugs into the body of tumor patients. The ion capture reaction uses the secondary radiation and recoil particles produced by the nuclear reaction to kill cancer cells. Its main advantages are as follows: ① Neutron capture therapy drugs (usually ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/113A61K31/337A61K31/513A61K31/704A61K33/243A61K47/62A61K47/34A61P35/00
CPCA61K9/113A61K47/62A61K41/0095A61K31/337A61K31/704A61K31/513A61K33/243A61K47/34A61P35/00A61K2300/00
Inventor 巩长旸周长庚
Owner 四川瑶天纳米科技有限责任公司
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