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

Active Publication Date: 2021-09-28
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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  • A kind of polyamino acid sound sensitizer and its preparation method and application
  • A kind of polyamino acid sound sensitizer and its preparation method and application
  • A kind of polyamino acid sound sensitizer and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

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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Abstract

The invention discloses a polyamino acid sound sensitizer as well as its preparation method and application. The main chain structure of the polyamino acid sonosensitizer of the present invention is aspartic acid grafted with protoporphyrin, which has good biocompatibility, and the side bond of protoporphyrin modified on the water-soluble polyaspartic acid greatly improves The solubility of protoporphyrin is improved, the blood compatibility of the sonosensitizer in the body and the accumulation amount of the lesion are increased, so as to produce a better therapeutic effect and realize efficient and safe tumor treatment. The present invention also provides a sound sensitizer nanovesicle and its target-modified sound sensitizer nanovesicle, which has the effect of high efficiency and low toxicity, and provides a new type of sound sensitizer with excellent performance for the development of safe and efficient sonodynamic therapy. Sensitizer materials, and by modifying specific antibodies or ligands on their surface, improve their aggregation at the target site.

Description

Technical field [0001] The present invention is in the field of biomedicine and, more specifically, the acoustic method for its preparation and application of the oxygen-carrying function relates to a polyamino acid. Background technique [0002] SDT (sonodynamic therapy, SDT) is a tumor developed in recent years a new treatment method, originally proposed by Umemura and other scholars, and put into use in 1989, is a new therapy based on photodynamic therapy (PDT) developed . SDT refers to the injection of cancer patients acoustic agents, low-frequency ultrasonic irradiation of the tumor, tumor tissue accumulated in the excitation of the acoustic agent for energy, thereby causing the electronic transition, reactive oxygen species (ROS) appear to kill target cells promote irreversible damage tumor cells, so as to achieve the purpose of cancer treatment, the acoustic agent is selectively accumulated in the tumor tissue, non-cytotoxic when unactuated, once activated can cause damage...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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