Acid response nano-micelle based on Cherenkov effect as well as preparation method and application of acid response nano-micelle
A nano-micelle and effect technology, applied in the field of biomedicine, can solve the problems of normal tissue side effects, phototoxicity, etc., and achieve the effect of improving selective lethality, improving specificity, and reducing side effects
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Embodiment 1
[0070] The synthesis routes of sPS and sPS-2 are respectively shown below, and the synthesis method includes the following steps:
[0071] (1) Modification of acid-responsive groups: take 468.6mg (1.0mmol) of N-Alpha-fluorenylmethoxycarbonyl-N-Epsilon-tert-butoxycarbonyl-L-lysine (CAS number: 71989-26-9) and 570.3 mg (1.5 mmol) of 2-(7-azabenzotriazole)-N,N,N',N'-tetramethyluronium hexafluorophosphate (HATU) were dissolved in 20 mL of dry dichloromethane , stirred at room temperature for 1 h under nitrogen protection. Then add 144.2mg (1.0mmol) N,N-diisopropylethylenediamine (DPA) and 193.9mg (1.5mmol) N,N-diisopropylethylamine (DIPEA) under nitrogen protection conditions, react overnight at room temperature . The progress of the reaction was detected by thin-layer chromatography, and the reaction was completed when the raw material spots on the chromatographic plate disappeared. NaHCO 3 The solution was washed three times with saturated brine, dried and purified by column...
Embodiment 2
[0090]Assembly and pH response of sPS NPs nanomicelles.
[0091] Method: Dissolve sPS in chloroform to make a 15mg / mL mother solution. Subsequently, the mother liquor was slowly added to the PBS buffer solution of pH 7.4, the volume ratio of the mother liquor and the buffer solution was controlled to be 1:15, and the open door was vigorously stirred overnight, that is, a 1 mg / mL sPS NPs nanomicelle solution was self-assembled, which could realize The assembled particle size is between 100-200nm. Adjust the pH of the assembled micellar solution to 5.4, scan the sPS NPs under two pH conditions by transmission electron microscopy, and observe the morphology.
[0092] Result: see Figure 4 A, at pH 7.4, sPS can form stable spherical micelles; Figure 4 B, The micelles were disrupted and dispersed at pH 5.4. It shows that the micelles have acid response properties and can be disassembled and dispersed under acidic conditions.
[0093] Replace the above sPS with sPS-2, and the ...
Embodiment 3
[0095] Labeling of sPS NPs nanomicelles 131 I.
[0096] Method: The sPS NPs nanomicelles prepared in Example 2 were prepared into a 50 μg / mL sPS NPs micellar solution using PBS buffer solution with pH 7.4, and 1 mL was placed on the tube wall to attach iodogen (CAS number: 51592-06- 4) in the EP tube. Then add 200 μCi Na 131 I solution (volume controlled at 100 μL), seal the EP tube, and vortex at room temperature for 10 min. Use a PD-10 separation column for desalting. Specifically, add the solution after the reaction to the PD-10 column, then rinse the desalting column with 50mL deionized water, and use 2mL EP tubes under the column to collect samples in sequence and collect samples with radioactive activity. Then all the samples were concentrated with a 30000Da ultrafiltration centrifuge tube, the rotation speed was set to 3000r / min, and the time was 20min. The radioactivity was measured, and finally about 150μCi was obtained. 131 I-sPS NPs nanomaterials.
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