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Poly spermine polymer-contained nano-particle, and preparation method and application thereof

A nanoparticle and polymer technology, applied in the direction of drug combination, pharmaceutical formula, genetic material components, etc., to avoid adhesion, inhibit angiogenesis, and achieve targeted effects

Inactive Publication Date: 2015-02-18
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] The purpose of the present invention is to provide a nanoparticle containing polyspermine polymer for the treatment of vascular proliferation, so as to solve the above-mentioned technical problems existing in the existing anti-VEGF drugs for inhibiting vascular proliferation
[0020] Another object of the present invention is to provide the above-mentioned preparation method of nanoparticles containing polyspermine polymers for the treatment of vascular proliferation, so as to solve the above-mentioned technical problems existing in the existing anti-VEGF drugs that inhibit vascular proliferation

Method used

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  • Poly spermine polymer-contained nano-particle, and preparation method and application thereof
  • Poly spermine polymer-contained nano-particle, and preparation method and application thereof
  • Poly spermine polymer-contained nano-particle, and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Example 1 Preparation of Polyspermine Polymer (PSA)

[0045] The whole reaction is carried out in an anhydrous and oxygen-free environment (protected by high-purity nitrogen). Spermine and 2,5-imidazole dicarbaldehyde are reacted at a molar ratio of 1:2.5. The reaction solvent is anhydrous ethanol (in anhydrous Add anhydrous magnesium sulfate to ethanol and let it stand for 48 hours, and then distill to obtain fresh anhydrous ethanol for later use). Dissolve spermine (1 mol) and 2,5-imidazole dicarbaldehyde (2.5 mol) with absolute ethanol, respectively, and make 20mL and 50mL solutions. The reaction was carried out with stirring at room temperature, and the o-phthalaldehyde solution was added dropwise to the spermine solution with a constant pressure dropping funnel. The reaction was stopped after 24 hours, and most of the solvent was removed by a vacuum rotary evaporator under reduced pressure and low temperature. Then the product was dissolved in a small amount of ultra...

Embodiment 2

[0047] Example 2 Preparation of Polyspermine Polymer (PSA) Coated Plasmid DNA Nanoparticles

[0048] The polyspermine polymer prepared in Example 1 was formulated into an aqueous solution with a concentration of 2μg / μl and diluted with sterile water to 20ng / μl, 40ng / μl, 100ng / μl, 200ng / μl, 1000ng / μl and 2000ng / μl solution. In addition, the plasmid DNA containing 5'-GGAGUACCCUGAUGAGAUC-3' was made into an aqueous solution with a concentration of 20ng / μl. Add an equal volume of the polyspermine polymer aqueous solution to the plasmid DNA aqueous solution, vortex for 5 minutes, and let stand for 20 minutes to obtain a series of nanoparticle solutions.

Embodiment 3

[0049] Example 3 Characterization of the particle size and potential of nanoparticles

[0050] Put the series of particle solutions prepared in Example 2 into the test tank of the BIC90plus particle size potential analyzer. The mass ratios of PSA to plasmid DNA in the particles of the series of particle solutions are 1, 2, 5, 10, 50, 100, and set The test temperature is 25°C, the medium is water, the viscosity is 0.89 cp, the refractive index is 1.330, and the light scattering angle is 90. , The detection wavelength is 659nm, each sample is tested 3 times, each run time is 2min, and the average particle size is recorded. The result is figure 1 As shown, the results show that the particle size of the nanoparticles is below 200 nm.

[0051] Put the series of particle solutions prepared in Example 2 into the test tank of the BIC90plus particle size potential analyzer. The mass ratios of PSA to plasmid DNA in the particles of the series of particle solutions are 1, 2, 5, 10, 50, 100, ...

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Abstract

The invention relates to the technical field of drugs for treating angiogenesis, in particular to a poly spermine polymer-contained nano-particle for treating angiogenesis, and a preparation method and application of the nano-particle. The poly spermine polymer-contained nano-particle comprises a poly spermine polymer and a genetic material, wherein the mass ratio of the poly spermine polymer to the genetic material is (1-100): 1. Compared with the prior art, the nano-particle provided by the invention can effectively inhibit angiogenesis, can realize the delivery of genetic material, can avoid problems of in vivo toxicity and in vivo immunogenicity, can avoid adhesion of in vivo non-target tissues as the nano-particle is uncharged, can realize targeting of in vivo diseased cells so as to effectively improve the targeting effect, and does not affect the endocytosis of the in vivo diseased cells.

Description

Technical field [0001] The present invention relates to the technical field of drugs for treating vascular hyperplasia, in particular to a nanoparticle containing polyspermine polymer for treating vascular hyperplasia, and a preparation method and application. Background technique [0002] New blood vessels can be accompanied by wound repair, tumor growth, intraocular ischemic lesions and many other conditions. The formation of new blood vessels is a very complex biological process. A large number of current studies have shown that vascular endothelial growth factor (VEGF) and its family members can specifically promote the division, proliferation and migration of endothelial cells. Play an important role in the formation process. [0003] VEGF is a type of glycoprotein widely distributed in brain, kidney, liver, spleen, lung, bone and other tissues in humans and animals. Human mature VEGF exists in five subtypes-VEGFl21, VEGFl45, VEGFl65, VEGFl89, and VEGF206, all of which are d...

Claims

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Application Information

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IPC IPC(8): A61K48/00A61K47/34A61K9/14A61P9/10A61P35/00A61P17/02
Inventor 袁伟恩车俊怡原明璐
Owner SHANGHAI JIAO TONG UNIV
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