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Active targeting brain-tumor-resisting drug and preparation method thereof

An anti-tumor drug and drug technology, applied in the field of drugs, can solve the problems of less drugs, inability to achieve tumor cell growth, and effective inhibition

Active Publication Date: 2016-04-13
NINGBO INST OF MATERIALS TECH & ENG CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, most of the research on brain-targeted drug delivery systems is aimed at crossing the blood-brain barrier. Due to the existence of a large part of the drug, a considerable part of the drug is basically released outside the brain tumor, which makes the drug actually reach the brain tumor cells very little, and it is impossible to achieve a real and effective inhibition of tumor cell growth.

Method used

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  • Active targeting brain-tumor-resisting drug and preparation method thereof
  • Active targeting brain-tumor-resisting drug and preparation method thereof
  • Active targeting brain-tumor-resisting drug and preparation method thereof

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preparation example Construction

[0150] The present invention also provides a kind of preparation method of described composition, and described method comprises the steps:

[0151] (1) providing a nanocarrier loaded with antitumor drugs;

[0152] (2) performing a coupling reaction between the nanocarrier and the target molecule in step (1) to obtain the composition.

[0153] In another preferred example, the nanocarrier and the target molecule are as described above.

[0154] In another preferred example, the antitumor drug is as described above.

[0155] In another preferred example, in the composition obtained in step (2), the weight ratio of the nanocarrier: the antineoplastic drug: the target molecule is 50-95:1-20:0.01-1, preferably For 60-90:3-15:0.02-0.5.

[0156] Typically, the coupling reaction is selected from the group consisting of:

[0157] (1) Condensation reaction of carboxyl group and amino group;

[0158] (2) addition reaction of thiol and maleimide; and / or

[0159] (3) Non-covalent bi...

Embodiment 1

[0214] Embodiment 1 prepares composition NPY-LPHNP-TXT

[0215] (1) Preparation of TXT-embedded lipopolymer hybrid (LPHNP) nanocarriers

[0216] Preparation mass concentration is the acetone solution 10ml of the PLGA polymer of 5mg / ml and the ethanol solution 50ml of the DSPE-PEG (molar ratio: 8.5 / 1.5) that mass concentration is the lecithin / 0.24mg / ml of 0.15mg / ml respectively, will The lecithin / DSPE-PEG ethanol solution was heated to 65° C. to dissolve the lecithin / DSPE-PEG. Add the acetone solution of PLGA dropwise into the ethanol solution of preheated lecithin / DSPE-PEG, stir at room temperature for 2 hours, and wash with ultrafiltration centrifuge tube (10KDa) for 3 times to remove residual organic solvent and unreacted substances, to obtain Polylactic acid-glycolic acid (PLGA), lecithin and distearoylphosphatidylethanolamine-polyethylene glycol (DSPE-PEG) composite LPHNP nanocarriers. The antitumor drug TXT is dissolved in PLGA acetone solution, and the same method as a...

Embodiment 2

[0227] Example 2 Composition NPY-LPHNP-TXT activity test on tumor cells SK-N-BE2 and HEC-1B-Y5

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Abstract

The invention relates to an active targeting brain-tumor-resisting drug and a preparation method thereof and specifically discloses a compound. The compound comprises a nano-carrier with the particle size less than 200nm and a target molecule, and the target molecule is coupled to the surface of the nano-carrier and has high affinity on a neuropeptide receptor Y1 on a blood brain barrier and a neuropeptide receptor Y2 on brain tumor cells. The invention further discloses a composition comprising the compound and a preparation method and application of the composition. The compound or the composition can effectively cross the blood brain barrier to get into the brain and can be combined with the brain tumor cells in a high specificity manner so as to deliver the antitumor drug into the tumor cells, drug concentration in the cells is heightened effectively, and the brain tumor cells are killed powerfully.

Description

technical field [0001] The invention relates to the field of drugs, in particular to an active targeting anti-brain tumor drug and a preparation method thereof. Background technique [0002] With the aging of human society and the deterioration of the global ecological environment, the incidence of brain diseases is gradually increasing. Among them, for cancers that occur in the brain, most of the existing treatment methods have certain limitations. For example, conventional surgical treatment has disadvantages such as strong invasiveness and difficulty in healing after operation; and chemotherapy, due to the existence of the blood-brain barrier (BBB), it is difficult for more than 98% of drugs to cross the blood-brain barrier and reach specific tumor sites in the brain. , which leads to poor therapeutic effect and large toxic side effects of chemotherapy. The above limitations make the cure rate and survival rate of brain cancer far lower than other cancers. Based on this...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/127A61K9/107A61K47/42A61K45/00A61K31/337A61P35/00
Inventor 李娟吴爱国田宇辰
Owner NINGBO INST OF MATERIALS TECH & ENG CHINESE ACADEMY OF SCI
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