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Polyamino acid sound-sensitive agent and preparation method and application thereof

A technology of polyamino acid and sonosensitizer, applied in the field of biomedicine, can solve the problems of low solubility of sonosensitizers and large toxic and side effects, and achieve the effects of good biocompatibility, high solubility and controllable structure.

Active Publication Date: 2019-03-01
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The technical problem to be solved by the present invention is to overcome the defects and deficiencies of the existing sonosensitizers, such as low solubility and large toxic and side effects, to provide a polyamino acid sonosensitizer, which utilizes polyamino acid sonosensitizers with excellent biocompatibility, stability and ease of modification Polyaspartic acid material modified sound sensitizer protoporphyrin to prepare a highly efficient and low toxicity polyamino acid sound sensitizer

Method used

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  • Polyamino acid sound-sensitive agent and preparation method and application thereof
  • Polyamino acid sound-sensitive agent and preparation method and application thereof
  • Polyamino acid sound-sensitive agent and preparation method and application thereof

Examples

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Embodiment 1

[0047] A polyamino acid sound sensitizer, the structural formula is as follows:

[0048]

[0049] Synthetic pathways such as figure 1 As shown, it is prepared by the following method:

[0050] S1. Preparation of amphiphilic polyamino acid: Weigh 150mg polybenzyl aspartate PEG-PBLA and dissolve it in 5mL NMP, absorb 737.25uL diethylenetriamine (DET) and dissolve it in 5mL NMP, then slowly add the DET solution dropwise to In the PBLA solution, stir and react at room temperature for 6h; after reacting for 6h, add 6.85mL HCl (1M) solution dropwise to the reaction solution under ice bath conditions, and collect it in a 3500D dialysis bag after neutralization in the ice bath for 1h, in 0.01M HCl Dialyzed in the solution for 1 day, then dialyzed in ultrapure water for 1-2 days and freeze-dried to obtain the light yellow powder product PEG-PAsp(DET);

[0051] S2. Synthesis of polyamino acid sound sensitizer PEG-PAsp(DET)-PpIX: Weigh 68mg of PEG-PAsp(DET) and dissolve it in 1.5ml ...

Embodiment 2

[0056] A sonosensitizer nanovesicle is prepared by the following method: Weigh 5 mg of the polymer PEG-PAsp (DET)-PpIX prepared in Example 1 and dissolve it in 1 mL of deionized water (polymer concentration is 5 mg / mL), vortex Rotate and oscillate to completely dissolve the polymer, then place the solution on an ice bath to cool for 5 minutes, then quickly pipette 60uL perfluoro-n-pentane PFP into the pre-cooled polymer solution, and use an ultrasonic cell disruptor to perform probe ultrasonication on the pre-cooled solution Finally, PFP-loaded liquid-gas conversion type sound sensitizer nanovesicles PFP-NDs were obtained.

[0057] The TEM electron microscope image of the prepared sonosensitizer nanovesicle PFP-NDs is as follows Figure 6 As shown, the particle size distribution diagram is shown in Figure 7 As shown, the particle size distribution of the sonosensitizer nanovesicles prepared by the emulsification method is uniform, the particle size is 380-423nm, and the surf...

Embodiment 3

[0061] A target-modified sonosensitizer nanovesicle prepared by the following method:

[0062] Synthetic preparation of polybenzyl aspartate (PEG-PBLA):

[0063] Weigh 500mg of BLA-NCA into a reaction flask, add 4mL of DMF that has been dehydrated, stir to dissolve, then weigh 25mg of polyethylene glycol (PEG-NH 2 ) Dissolve PEG-NH with 1mL DMF 2 Then add it to the BLA-NCA reaction solution; vacuumize first, then feed nitrogen, repeat three times, add anhydrous DCM under nitrogen protection, react at room temperature for 3 days, the solution gradually changes from light yellow to orange; after the reaction, collect the solution to 3500D dialysis bag, dialyzed in DMSO solution in the dark for 1 day, then dialyzed in ultrapure water for 1-2 days and freeze-dried to obtain a white powder product (PEG-PBLA);

[0064] Synthesis of the aminolysis product PEG-PAsp (DET):

[0065] Weigh 100mg PEG-PBLA and dissolve it in 5mL NMP, draw 625uL diethylenetriamine (DET) and dissolve it i...

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Abstract

The invention discloses a polyamino acid sound-sensitive agent and a preparation method and application thereof. A main chain structure of the polyamino acid sound-sensitive agent is aspartic acid grafted with protoporphyrin, the aspartic acid has good biocompatibility, modifying a water-soluble polyaspartic acid side bond with the protoporphyrin greatly improves the solubility of the protoporphyrin, and the blood compatibility in a body and the accumulation quantity on a focus portion of the sound-sensitive agent are improved, so that a good treatment effect is generated, and efficient safe tumor treatment is achieved. The invention further provides a sound-sensitive agent nanovesicle and a targeted modified sound-sensitive agent nanovesicle; the sound-sensitive agent nanovesicle and targeted modified sound-sensitive agent nanovesicle have efficient and low-toxicity effects, a novel sound-sensitive agent material excellent in performance is provided for developing safe and efficient sonodynamic therapy, and by modifying surfaces of the sound-sensitive agent nanovesicle and the targeted modified sound-sensitive agent nanovesicle with specific antibodies or ligands, accumulation ofthe sound-sensitive agent nanovesicle and targeted modified sound-sensitive agent nanovesicle on a targeted portion is improved.

Description

technical field [0001] The invention belongs to the field of biomedicine, and more specifically relates to a polyamino acid sound sensitizer with oxygen-carrying function and its preparation method and application. Background technique [0002] Sonodynamic therapy (SDT) is a new method of tumor treatment developed in recent years. It was first proposed by Umemura and other scholars and put into use in 1989. It is a new therapy based on photodynamic therapy (PDT). . Sonodynamic therapy refers to injecting a sonosensitizer into tumor patients, irradiating the tumor site with low-frequency ultrasound, exciting the sonosensitizer accumulated in the tumor tissue to obtain energy, causing electronic transitions, and the emergence of reactive oxygen species (ROS) that kill target cells. , to promote irreversible damage to tumor cells, so as to achieve the purpose of tumor treatment. The sonosensitizer can selectively accumulate in tumor tissue, and has no cytotoxicity when it is n...

Claims

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Application Information

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IPC IPC(8): A61K49/22A61K41/00A61K9/127A61P35/00
CPCA61K9/1273A61K41/0033A61K49/223A61P35/00
Inventor 刘杰曾强李超
Owner SUN YAT SEN UNIV
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