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
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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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