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Preparation method and application of highly nucleus-targeted anti-tumor nanomedicine

A nano-drug and anti-tumor technology, applied in the fields of nano-drugs and biomedicine, can solve the problems of low efficiency and the inability of nano-drugs to penetrate the nuclear membrane, so as to inhibit invasiveness and metastasis, inhibit division, proliferation and migration, and improve killing. effect of action

Pending Publication Date: 2019-12-17
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently developed nanocarrier materials, such as metals, metal oxides, semiconductors, and polymers, can target drug delivery to the tumor microenvironment, but their efficiency is low, and nanomedicine cannot penetrate the nuclear membrane.

Method used

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  • Preparation method and application of highly nucleus-targeted anti-tumor nanomedicine
  • Preparation method and application of highly nucleus-targeted anti-tumor nanomedicine
  • Preparation method and application of highly nucleus-targeted anti-tumor nanomedicine

Examples

Experimental program
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Effect test

Embodiment 1

[0029] A method for preparing highly nuclear-targeted anti-tumor nano-medicine includes the following steps:

[0030] 1) The TAT polypeptide and graphite powder are mixed in a mass ratio of 1:1-1:5 and placed in a ball mill tank. Ball mill at room temperature at 300-500rpm for 3-5 hours. After ball milling, add deionized water to wash out the product. Centrifugation at 1000-3000 speeds for 5-15 minutes is used, and then a high-speed centrifugal treatment at 5000-8000 rpm for 5-15 minutes is used to sequentially remove impurities in the precipitate. Then finally the precipitate is dispersed in deionized water, which is graphene (TG) functionalized with TAT polypeptide. From figure 1 It can be seen that through the edge-functionalized ball milling method, the TAT polypeptide can be easily and efficiently loaded onto the two-dimensional graphene plane. From figure 2 It can be seen that the prepared nano drug carrier TG has good water dispersibility. And our research found that ...

Embodiment 2

[0034] Physical and chemical properties of the MMC-TG nanomedicine prepared in Example 1:

[0035] From image 3 It can be seen that the height of the prepared graphene sheet is about 0.8 nm, indicating that it is a single-layer graphene. After covalent loading of MMC drugs, the thickness of the nanomaterials rose to 4.3nm.

Embodiment 3

[0037] Evaluation of the targeted anti-tumor effect of the nanomedicine MMC-TG prepared in Example 1.

[0038] We used the Transwell two-cell co-culture system to investigate the targeted anti-tumor effect of MMC-TG. Transwell plate is a special cell culture plate, divided into upper layer and lower layer. Between the two layers is a permeable membrane. The components in the culture medium on the membrane can freely pass through the permeable membrane but the cells cannot. In this experiment, ARPE-19 normal cells and OCM-1 tumor cells were cultured simultaneously in the upper and lower chambers of the Transwell plate, and then MMC-TG and MMC were added to co-culture with the cells for 72 hours to detect cell viability. From image 3 In (a) and (b), it can be seen that after MMC-TG was co-cultured with the two kinds of cells for 72 hours, when the MMC concentration reached 4 μg / mL, the survival rate of OCM-1 tumor cells dropped to below 5%, while ARPE- 19 The survival rate of nor...

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Abstract

The invention belongs to the field of nanomedicine and biomedicine, and discloses a preparation method and application of highly nucleus-targeted anti-tumor nanomedicine. According to the preparationmethod and the application of the highly nucleus-targeted anti-tumor nanomedicine, a polypeptide with nucleus targeting ability and graphite powder are subjected to blending and ball milling, and polypeptide functionalized graphene (TG) with high tumor targeting ability and nucleus targeting ability is prepared under normal temperature and pressure. Furthermore, carboxyl group is introduced into the TG by using an acetic acid plasma technology, and the anti-tumor drug mitomycin C (MMC) is loaded on the TG. The prepared anti-tumor nanomedicine MMC-TG has good tumor cell nucleus targeting ability and can highly selectively target tumor cells. The tumor killing rate is 95% or above, but at the same time, the anti-tumor nanomedicine MMC-TG has little damage to normal cells. Experimental results confirm that the developed nanomedicine first plays a role in the nucleus, and has efficient tumor cell nucleus targeting ability, tumor killing ability and tumor metastasis inhibiting ability.

Description

Technical field [0001] The invention belongs to the field of nano-medicine and biomedicine, and specifically relates to a preparation method and application of a highly nuclear-targeted anti-tumor nano-medicine. Background technique [0002] The rapid proliferation and metastasis of tumor cells have caused the incurable nature of most cancers and brought a great threat to human life and health. For example, choroidal melanoma is one of the most common ocular malignant tumors in adults, with a high mortality rate and a five-year survival rate of less than 50%, mainly due to the high systemic metastasis rate of this type of tumor. Although a variety of techniques have been developed to treat choroidal melanoma, including surgical resection, laser treatment, radiotherapy and systemic chemotherapy, these methods are only for in situ tumors, and they are helpless for metastatic tumors. In addition to causing great pain to the patient , And failed to improve the survival rate of patie...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/64A61K47/52A61K31/407A61P35/00A61P35/04
CPCA61K47/64A61K47/52A61K31/407A61P35/00A61P35/04
Inventor 单素艳刘勇林蜜蜜晏露
Owner WENZHOU MEDICAL UNIV
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