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Preparation method of RGD-modified dendrimer-encapsulated CuS nanoparticles

A technology of dendritic macromolecules and nanoparticles, which can be applied to the preparation method of peptides, medical preparations containing non-active ingredients, and medical preparations containing active ingredients. Water-soluble, promotes phagocytosis, and inhibits tumor growth

Active Publication Date: 2020-02-11
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Searching domestic and foreign literature, there is no relevant report on nanomaterials with pH-responsive charge reversal and glutathione-responsive drug release

Method used

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  • Preparation method of RGD-modified dendrimer-encapsulated CuS nanoparticles
  • Preparation method of RGD-modified dendrimer-encapsulated CuS nanoparticles
  • Preparation method of RGD-modified dendrimer-encapsulated CuS nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] (1) Dissolve 20mg of COOH-PEG-6-M in 5mL of DMSO, then add 6.91mg of RGD fully dissolved in 2mL of DMSO dropwise into the DMSO solution of COOH-PEG-6-M, and stir for 1 day , dialyzed for three days with a dialysis bag with a molecular weight cut-off of 1000, and then freeze-dried to obtain COOH-PEG-RGD. The COOH-PEG-RGD that gets 5mg synthesis is dissolved in deuterated water and carries out nuclear magnetic resonance analysis (1H NMR) (see figure 2 a). It can be seen from the figure that the spectral peaks at 7.3 and 7.4ppm prove that RGD is successfully connected to PEG, and it can be seen from the peak area integration that 0.7 RGD is connected to each PEG.

[0054] (2) Dissolve bis(2-dimethylaminoethyl) disulfide dihydrochloride (compound 1) (10.1g, 35.9mmol) and triethylamine (10.0mL, 71.7mmol) in anhydrous methanol (100mL ), the mixture was stirred at room temperature for 30 min. Then acrylic acid (48.3mL, 710mmol) and hydroquinone (500mg, 4.54mmol) were added...

Embodiment 2

[0060] (1) Mix and dissolve 13.75mg COOH-PEG-RGD, 8.16mg EDC and 4.80mg NHS prepared in Example 1 in 5mLDMSO, stir and activate for 3.5h, then add the mixed solution dropwise to G5.NH 2 DMSO solution (20 mg, 5 mL), stirred for 2 to 4 days, dialyzed and freeze-dried to obtain G5.NH 2 -PEG-RGD. Take 5 mg of prepared G5.NH 2 -PEG-RGD was dissolved in deuterated water for nuclear magnetic resonance analysis (1H NMR) (see image 3 a) and by integrating the peak area, it can be known that the average of each G5.NH 2 5.3 PEG-RGD were connected on.

[0061] (2) Take the CBT containing benzaldehyde terminal prepared in Example 1 and fully dissolve it in methanol solvent (22 mg, 5 mL), and then add it dropwise to G5.NH 2 - PEG-RGD methanol solution (52mg, 10mL) stirred at room temperature for 2-4h, dialyzed and freeze-dried to obtain G5.NH 2 -PEG-RGD-CBT. Take 5 mg of prepared G5.NH 2 -PEG-RGD-CBT dissolved in deuterated water for nuclear magnetic resonance analysis (1H NMR) (see...

Embodiment 3

[0065] Get the G5.NH prepared in Example 2 2 -PEG-RGD, G5.NH 2 -PEG-RGD-CBT, G5.NH 2 - PEG-RGD-CBT-DOX, {(CuS)-G5.NHAc-PEG-RGD-CBT-DOX} and G5.NH 2 Dissolve 1mg in 2mL aqueous solution, ultrasonically homogenize, measure UV absorption (see Figure 4 ). The UV results showed that DOX was successfully connected to the dendrimer, and the absorption peak was around 500nm, which was somewhat shifted compared with the absorption peak at 480nm of pure DOX. The formed CuS has a strong near-infrared absorption, and the absorption value becomes stronger and stronger with the extension of the wavelength, until the highest measurement limit of 1100nm, which also fully demonstrates the successful synthesis of CuS nanoparticles.

[0066] Dissolve the {(CuS)-G5.NHAc-PEG-RGD-CBT-DOX} prepared in Example 2 in 1 mL of ultrapure water (1 mg), then drop 5 μL of the nanoparticle suspension on the surface of the copper grid, Air-dried for TEM testing (see Figure 5 a). The high-resolution TE...

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Abstract

The invention relates to a preparation method of RGD-modified dendrimer-encapsulated CuS nanoparticles. The preparation method comprises the steps that a targeting reagent PEG-RGD and CBT with a pH response are used for modifying a fifth-generation dendrimer, then the surface of the dendrimer is covalently modified with doxorubicin containing disulfide bonds, then copper sulfide nanoparticles areencapsulated in the dendrimer by using the reaction of copper chloride and sodium sulfide, and finally, all remaining amino groups on the surface of the dendrimer are acetylated. The functionalized copper sulfide nanoparticles prepared by the preparation method have good monodispersity, colloidal stability, biocompatibility and extremely high resistance to non-specific protein adsorption, have pH-responsive charge reversal performance to promote phagocytosis of nano-platforms by cancer cells and have the drug release performance with glutathione reduction response. The combined treatment of tumor chemotherapy and photothermal therapy can be realized and is supplemented by photothermal and photoacoustic imaging, and potential application value in the field of integration of diagnosis and treatment is achieved.

Description

technical field [0001] The invention belongs to the field of integrated nanomaterials for diagnosis and treatment, in particular to a preparation method of CuS nanoparticles wrapped by RGD modified dendrimers. Background technique [0002] Cancer has become the leading cause of death and a major public health problem in China. Early diagnosis and efficient treatment are the key issues to be solved first to reduce mortality and improve survival rate. In recent years, nanomaterials have received increasing attention due to their potential applications in drug delivery, molecular imaging, and therapy. Especially its application in photothermal therapy, such as nano-venus, molybdenum sulfide nanoparticles and copper sulfide nanoparticles, because of their good chemical stability, biocompatibility and unique optical properties, are widely used in biosensors, light Thermal therapy and molecular imaging are often regarded as star nano-platforms for the integration of multimodal t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/22A61K49/00A61K41/00A61K47/69A61K47/60A61K47/64A61K31/704A61P35/00C07K5/037C07K1/107
CPCA61K31/704A61K41/0052A61K49/00A61K49/0002A61K49/225A61K47/60A61K47/64A61K47/6925A61P35/00C07K5/0215A61K2300/00
Inventor 史向阳熊智娟沈明武
Owner DONGHUA UNIV
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