A kind of polyamino acid sound sensitizer and its preparation method and application
A polyamino acid and sonosensitizer technology, applied in the field of biomedicine, can solve the problems of high toxicity and low solubility of sonosensitizers, and achieve the effects of improving solubility, good biocompatibility, and improving aggregation
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Embodiment 1
[0046] A polyamino acid sound activator, the structural formula is as follows:
[0047]
[0048] Synthetic route figure 1 As shown, it is prepared from the following method:
[0049] S1. Preparation of two-pro - polyamino acid: It is called 150 mg of polyteenine benzyl pelelate PEG-PBLA to dissolve in 5 ml NMP, and 737.25 ul Diethine (DET) is dissolved in 5 ml NMP, and then the DET solution slowly added In the PBL solution, the reaction was stirred at room temperature for 6 h; after 6 h, 6.85 ml of HCl (1 m) solution was added dropwise to the reaction solution, and the ice bath was collected until 3500d dialysis bag after 1 h, at 0.01m Dialysis in the HCl solution was dialyzed in ultrapure water for 1 to 2 days and lyophilized to give a pale yellow powder PEG-PASP (DET);
[0050] S2. Synthesis Polyamino Acid Sensitizer PEG-PASP (DET) - PPIX: It is called PEG-PASP (DET) 68 mg to dissolve in 1.5 ml of pure water, PPIX weigh 8 mg dissolved in 1 ml dimethyl sulfoxide (DMSO), EDC, NH...
Embodiment 2
[0055] A sensual agent nano vesicle was prepared from the following method: a polymer PEG-PASP (DET) -PPIX prepared by 5 mg Example 1 was soluble in 1 ml deionized water (polymer concentration of 5 mg / ml), vortex The spin oscillation allows the polymer to completely dissolve 5 min on an ice bath, and then quickly remove 60 ul of all fluoropentane PFP to a pre-cooling polymer solution, using ultrasonic cell crusher to probe the pre-cooling solution The liquid gas conversion-type sensitive agent nanocarbon PFP-NDS was obtained from the load PFP.
[0056] Preparation of sensitive agent nano vesicles PFP-NDS TEM electron microscopy Image 6 As shown, the particle size distribution is like Figure 7 As shown, it is known that the sensitive agent nano-vesicle particle size of such emulsification method can be seen by dynamic light scattering DLS, and the particle size is 380 to 423 nm, and the surface potential is 30 to 45 mV.
[0057] Figure 8 The release curve of the contrast water i...
Embodiment 3
[0059] A targeted resolved sensitive agent nano vesicles, prepared by the following method:
[0060] Synthesis Preparation of PEG-PBLAs:
[0061] Weigh 500 mg BLA-NCA in the reaction flask, add DMF 4ml having a water, stir the dissolution, and then weigh 25 mg of polyethylene glycol (PEG-NH) 2 1 ml DMF to dissolve PEG-NH 2 After adding to the BLA-NCA reaction solution; first vacuum, then enter nitrogen, and then add anhydrous DCM under nitrogen, and the reaction is 3 days at room temperature, and the solution is gradually yellowing. The 3500D dialysis bag was dialyzed in DMSO solution for 1 day, and then dialyzed in ultrapure water for 1 to 2 days and lyophilized to give a white powder product (PEG-PBLA);
[0062] Synthesis of amine solution PEG-PASP (DET):
[0063] It is weighing 100 mg PEG-PBLA dissolved in 5 mL NMP, and 625 ul of divinisin (DET) was dissolved in 5 ml NMP, and then the DET solution was slowly added dropwise to the PBLA solution, and the reaction was stirred at a...
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