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Multifunctional anti-cancer nano material based on polypeptide-rare earth nanocrystals and preparation method of multifunctional anti-cancer nano material

A technology of nanomaterials and nanocrystals, applied in the field of nanomaterials, to achieve good pH responsiveness, significant enhancement, and the effect of overcoming multidrug resistance

Pending Publication Date: 2022-03-15
HUBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although NaYF 4 :Yb 3+ ,Er 3+ There have been many reports on the functional studies of nanocrystal-modified drug-carrying systems for treating tumors, but NaYF 4 :Yb 3+ ,Er 3+ No one has done a systematic study on the influence of the photothermal effect of nanocrystals and the combination of peptide drug loading on the morphology, structure and biological effects of the drug loading system.

Method used

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  • Multifunctional anti-cancer nano material based on polypeptide-rare earth nanocrystals and preparation method of multifunctional anti-cancer nano material
  • Multifunctional anti-cancer nano material based on polypeptide-rare earth nanocrystals and preparation method of multifunctional anti-cancer nano material
  • Multifunctional anti-cancer nano material based on polypeptide-rare earth nanocrystals and preparation method of multifunctional anti-cancer nano material

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preparation example Construction

[0037] Its preparation method comprises the following steps:

[0038] a. First, swell 2-cl resin (1.03 mmol / g, 1.0 g) in DCM (15 mL, 3 minutes each). A coupling solution was prepared by adding DIEA (1.5 mL) to a DMF (15 mL) solution containing Fmoc-Asp(OtBu)-OH (0.55 g), HOBT (0.45 g) and DIC (1.5 mL). The coupling solution was added to the resin and reacted for 1.5 hours, Kaiser test showed complete coupling. Then use methanol and DCM to block the unreacted active chlorine group, and the reaction time is 30min. After washing several times with DMF, use 20% piperidine to remove the Fmoc on the amino terminal of the peptide chain, and the reaction time is 20 min. Kaiser test showed that NH 2 Exposure exists. The resin was washed with DMF (15 mL, 3 min each).

[0039] b. After fully washing with DMF, the next amino acid can be added until the last amino acid Fmoc-Ala-OH of the P13 peptide. Finally, the protecting group in the coupled compound was removed by mixing with 20%...

Embodiment 1

[0047] A multifunctional anti-cancer nano material, the specific preparation method comprises the following steps:

[0048] a. Under the condition of avoiding light, add 1mL triethylamine and 10mg DOX·HCl into 5mL DMF, then put it in a magnetic stirrer at 20°C, contact with it for 1h at 1000r / min, and finally lyophilize (temperature -80°C, pressure 999Pa, drying time 12h) to produce DOX;

[0049] b. At the same rotational speed, add 1mg / mL NaYF to 4mg / mL DOX organic solution (the organic solvent is DMF, the volume is 1mL) 4 :Yb 3+ ,Er 3+ Organic solution (the organic solvent is DMF, the volume is 1mL), the reaction time is 15min, and about 2mL of DOX and NaYF are obtained 4 :Yb 3+ ,Er 3+ Mixed DMF organic solution;

[0050] c. Under ultrasonic conditions, use a syringe with a 0.34mm needle to add 5mL of P13 aqueous solution (6mg / mL, the drop time is 15s) into 2mL of DOX and NaYF 4 :Yb 3+ ,Er 3+ In the mixed DMF organic solution, react at room temperature for 20 minute...

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Abstract

The invention discloses a multifunctional anticancer nano material based on polypeptide-rare earth nanocrystals, which is characterized in that the nano material is a hydrophilic nano microsphere of polypeptide entrapped drug adriamycin and NaYF4: Yb < 3 + >, Er < 3 + > nanocrystals; wherein the hydrophobic end of the P13 peptide is combined with the medicine doxorubicin and the NaYF4: Yb < 3 + > and Er < 3 + > nanocrystalline in a non-covalent bond form to form a hydrophobic core; and the hydrophilic end of the P13 peptide is used as a targeting end to form a hydrophilic shell. According to the invention, polypeptide is used as a carrier for entrapment of drug adriamycin, and drug inhibition and a PDT method are combined to kill tumor cells in a manner of entrapment of NaYF4: Yb < 3 + >, Er < 3 + > nanocrystals. According to the invention, a remarkable super-addition (1 + 1 > 2) effect is generated in a synergistic treatment mode, and the effect is remarkably enhanced compared with that of any single therapy; meanwhile, the multi-mode combined treatment mode can effectively overcome the multi-drug resistance of the tumor; in addition, the defect that the drug loading system cannot be subjected to fluorescence tracking due to the fact that the polypeptide has no fluorescence characteristic is overcome.

Description

technical field [0001] The invention relates to nanomaterials, in particular to a multifunctional anti-cancer nanomaterial based on polypeptide-rare earth nanocrystals and a preparation method thereof. Background technique [0002] Nanocarrier-based unimodal therapy for tumors can achieve certain therapeutic effects, but the complexity, diversity, and heterogeneity of tumors often make it impossible for a single form of treatment to completely eradicate tumors. Therefore, the current trend of clinical research has gradually shifted from monotherapy to combination therapy in order to improve the therapeutic effect. [0003] In the study of multifunctional materials to treat diseases, up-conversion nano-luminescent materials are favored by researchers because of their ability to absorb NIR light and convert it into light and heat. Among the many up-conversion materials, the one with the highest photon conversion ability is hexagonal NaYF 4 :Yb 3+ ,Er 3+ Nanocrystalline. A...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/64A61K31/704A61K41/00A61P35/00B82Y40/00C01F17/10C01F17/36C09K11/02C09K11/77
CPCA61K47/6925A61K47/64A61K41/0052A61K31/704A61P35/00C09K11/7773C09K11/025C01F17/36C01F17/10B82Y40/00A61K2300/00
Inventor 乔茜茜李草
Owner HUBEI UNIV
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