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Dual-targeting polymer drug nano-carrier as well as preparation method and application thereof

A nano-carrier and dual-targeting technology, applied in the field of nano-biomedical materials, can solve problems such as complex functions, weakened therapeutic effects, and side effects in the central nervous system

Active Publication Date: 2021-06-15
INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Overcoming the barrier function of the BBB and successfully delivering drugs, especially biotechnology drugs such as polypeptide proteins / genes, into the brain is the first condition for the implementation of brain disease treatment; The distribution of the whole brain makes it difficult to concentrate on the lesion, and the brain tissue is the center of the human body, its functions are complex, and the neurons are very sensitive to damage. Therefore, the distribution of the drug to the whole brain not only reduces the concentration of the drug reaching the lesion, but also weakens the therapeutic effect. And it may cause serious side effects on the normal central nervous system. How to make the drug concentrate in the brain lesion is of great significance for the treatment of brain diseases.

Method used

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  • Dual-targeting polymer drug nano-carrier as well as preparation method and application thereof
  • Dual-targeting polymer drug nano-carrier as well as preparation method and application thereof
  • Dual-targeting polymer drug nano-carrier as well as preparation method and application thereof

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preparation example Construction

[0042] The preparation method of the dual targeting polymer drug nanocarrier is:

[0043]S1. Weigh PLGA-PEG-MAL, PLGA-PEG-FA and PLGA-PEG-OMe respectively, and mix them to obtain a mixture. After adding dichloromethane to dissolve, add the first sodium cholate solution, and obtain the initial Emulsion, the first emulsion is added dropwise to the second sodium cholate solution, after the dropwise addition is completed, methylene chloride is distilled off under reduced pressure to obtain a nanoparticle colloidal solution, and the nanoparticle colloidal solution is ultrafiltered or centrifugally separated and precipitated , to prepare folic acid-targeted nanomicelles;

[0044] S2. Redisperse the folic acid targeting nanomicelles prepared in S1 in deionized water, add the brain targeting peptide Angiopep-2 according to the molar ratio of sulfhydryl groups to maleimide groups at 2:1, and then block the reaction system, stirring and reacting at room temperature, ultrafiltration or ...

Embodiment 1-3

[0048] Prepared by emulsified solvent volatilization method, accurately weighed PLGA-PEG-OMe, PLGA-PEG-MAL and PLGA-PEG-FA respectively, and the weighing ratios were 1:1:1, 4:1:1, 9:1: 1. Weigh the total amount of 3 mg, 6 mg and 11 mg respectively, add 0.5 ml of dichloromethane to dissolve, add 2 ml of the first sodium cholate solution with a mass concentration of 1%, and perform pulse ultrasonic treatment with an ultrasonic cell pulverizer (ultrasonic 5s, intermittent 5s), ultrasonic power 100W, pulse ultrasonic treatment time 60s, obtain the first emulsion, the first emulsion is added dropwise in the second sodium cholate solution of 1ml mass concentration 0.1%, at 37 ℃ of temperature, rotary steaming 15min removes dichloride Methane to obtain a nanoparticle colloid solution, which is placed in an ultrafiltration centrifuge tube with a molecular weight cut-off of 3kDa, centrifuged at 5000rpm for 45min, and the precipitate is collected to prepare the folic acid-targeted nanomi...

Embodiment 4-6

[0051] Prepared by emulsified solvent evaporation method, accurately weighed PLGA-PEG-OMe, PLGA-PEG-MAL and PLGA-PEG-FA respectively, the total amount was 6mg, and the weighing ratio was 4:1:1, and 0.5ml di Methyl chloride was dissolved, and 2ml of the first sodium cholate solution with a mass concentration of 1% was added, and pulse ultrasonic treatment was performed with an ultrasonic cell disruptor (5 s of ultrasound, 5 s intermittent), the ultrasonic power was 100 W, and the pulse ultrasonic treatment time was 30 s, 60 s, and 90 s, respectively. , to obtain the primary emulsion, the primary emulsion is added dropwise in the second sodium cholate solution of 1ml mass concentration of 0.1%, and the dichloromethane is removed by rotary steaming at a temperature of 37°C for 15min to obtain a nanoparticle colloidal solution, which is placed in In an ultrafiltration centrifuge tube with a molecular weight cut-off of 3kDa, after centrifugation at 5000rpm for 45min, the precipitate...

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Abstract

The invention provides a dual-targeting polymer drug nano-carrier, and belongs to the field of nano biomedical materials. The nano-carrier comprises a nano-material formed by a poly (lactic-co-glycolic acid)-polyethylene glycol block copolymer, and the surface of the nano-material is modified with tumor targeting functional molecules and brain targeting peptides; the tumor targeting functional molecule is folic acid, and the brain targeting peptide is connected with the nano material through a sulfydryl-maleimide group. According to the invention, biodegradable polylactic acid-glycolic acid is used as a core, tumor targeting functional molecules and brain targeting peptides are modified on the surface to obtain an Angiopep-2 / folic acid dual-targeting polymer drug nano-carrier, the barrier of BBB can be effectively overcome, meanwhile, tumor cells are targeted, and the Angiopep-2 / folic acid dual-targeting polymer drug nano-carrier can be used as a drug-loaded nano-preparation for treating brain glioma.

Description

technical field [0001] The invention relates to the field of nano biomedical materials, in particular to a dual-targeting polymer drug nanocarrier and its preparation method and application. Background technique [0002] Glioma is the tumor with the highest incidence rate in the central nervous system, accounting for about 46% of intracranial tumors. It is considered to be one of the most destructive and fatal tumors. ability to relapse. Due to the unclear boundary between brain tumor tissue and normal tissue, surgery is difficult to completely remove the tumor, and the success rate is low. The existence of blood-brain barrier (BBB), blood-cerebrospinal fluid barrier (BCB) and blood-tumor barrier (BTB) also makes large Some chemotherapeutic drugs are difficult to reach the brain tissue, and the drug enrichment concentration at the tumor site is low, which is not enough to kill tumor cells. Therefore, despite comprehensive treatment such as surgery, radiotherapy and chemoth...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/64A61K47/54A61K31/337A61P35/00
CPCA61K47/545A61K47/6935A61K47/64A61K31/337A61P35/00
Inventor 王锦玉游云李新健刘德文仝燕
Owner INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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