A gold nano-assembly with enhanced tumor radiotherapy and its preparation method and application
A technology of tumor radiotherapy and gold nanotechnology, which is applied in the field of biomedicine, can solve the problems that nanoparticles are not easy to clear the viscera, and it is difficult to reach the deep part of the tumor, and achieve excellent radiosensitivity and stability, small size, and improved cycle time. Effect
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Embodiment 1
[0055] The synthesis of embodiment 1, block copolymer PAEMA-b-PEAL:
[0056] (1) First prepare 2-(hexamethyleneimine) ethyl methacrylate, namely AEMA:
[0057] Specifically, 6.4 g of acryloyl chloride was added dropwise to a mixed THF solution of 10.1 g of 2-(hexamethylenediimine) ethanol and 7.0 g of triethylamine in an ice bath environment, and reacted overnight. After the reaction, the triethylamine salt produced in the reaction system was removed by filtration, then concentrated by rotary evaporation, and vacuumed overnight to obtain a colorless transparent liquid product with a yield of 65.7%.
[0058] (2) Second, synthesize lipoic acid hydroxyethyl methacrylate, namely EAL:
[0059] Under room temperature, 2g lipoic acid and 1.6g hydroxyethyl methacrylate were dissolved in dichloromethane, and 0.5g lutidine and 3.9g 1-(3-dimethylaminopropyl)-3-ethyl Carbodiimide, reaction 48h. After the reaction, it was washed successively with hydrochloric acid, saturated sodium bica...
Embodiment 2
[0068] The synthesis of embodiment 2 block copolymer PAEMA-b-mPEG:
[0069] (1) First prepare mPEG-CPAD, polyethylene glycol-4-cyano-4-(thiobenzoyl)valerate:
[0070] Specifically, dicyclohexylcarbodiimide, 4-dimethylaminopyridine, and 4-cyano-4-(thiobenzoyl)valeric acid were dissolved in dichloromethane. After stirring and reacting for 12 hours, it was precipitated with glacial ether to obtain a pink solid with a grafting rate of 75%.
[0071] (2) Preparation of PAEMA-b-mPEG:
[0072] Specifically, 0.051g mPEG-CPAD, 3.2g 2-(hexamethyleneimine) ethyl methacrylate, and 0.003g azobisisobutylcyanide were dissolved in dioxane, and reacted at 75°C under nitrogen atmosphere 12h. After the reaction was completed, it was concentrated under reduced pressure, precipitated with n-hexane, and vacuumed overnight to obtain a pink solid with a yield of 62.6% and a degree of polymerization of 97.
[0073]
[0074] The prepared compound was characterized by proton nuclear magnetic reson...
Embodiment 3
[0075] Example 3, the synthesis of poly 2-cyclohexyl methacrylate block lipoic acid hydroxyethyl methacrylate, namely PCMA-b-PEAL:
[0076] (1) at first prepare 2-cyclohexyl methacrylate, i.e. CMA,:
[0077] Specifically, under the condition of 0° C., methacryloyl chloride was added dropwise into a tetrahydrofuran solution of triethylamine and 2-cyclohexyl ethanol. After reacting overnight, after the reaction was completed, it was filtered, concentrated by rotary evaporation, and then purified by distillation under reduced pressure to finally obtain a colorless transparent liquid with a yield of 53.2%.
[0078] (2) secondly prepare poly 2-cyclohexyl methacrylate, i.e. PCMA:
[0079] Specifically, 0.034 g of cyanomethyl dodecyl trithiocarbonate, 1.95 g of 2-cyclohexyl methacrylate and 0.005 g of azobisisobutylcyanide are uniformly mixed in a dioxane solvent. Under freezing pumping and nitrogen atmosphere, react at 75°C for 12h. After the reaction, it was concentrated under r...
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