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A dual-targeting polymer drug nanocarrier and its preparation method and application

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

Active Publication Date: 2022-08-02
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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  • A dual-targeting polymer drug nanocarrier and its preparation method and application
  • A dual-targeting polymer drug nanocarrier and its preparation method and application
  • A dual-targeting polymer drug nanocarrier and its preparation method and application

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preparation example Construction

[0042] The preparation method of the double-targeted polymer drug nanocarrier is:

[0043]S1. Weigh PLGA-PEG-MAL, PLGA-PEG-FA and PLGA-PEG-OMe respectively, mix to obtain a mixture, add dichloromethane to dissolve, add the first sodium cholate solution, and obtain initial Emulsion, the initial emulsion is added dropwise to the second sodium cholate solution, after the dropwise addition is completed, the dichloromethane is distilled off under reduced pressure to obtain a nanoparticle colloid solution, and the nanoparticle colloid solution is ultrafiltered or centrifuged for precipitation , the folic acid-targeted nanomicelles were prepared;

[0044] S2. The folic acid-targeting nanomicelles prepared in S1 are re-dispersed in deionized water, and the brain-targeting peptide Angiopep-2 is added according to the molar ratio of sulfhydryl to maleimide group of 2:1, and then the reaction is blocked. system, stirring the reaction at room temperature, ultrafiltration or centrifugatio...

Embodiment 1-3

[0048] Prepared by the emulsification solvent evaporation method, and 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 3mg, 6mg and 11mg respectively, add 0.5ml of dichloromethane to dissolve, add 2ml of the first sodium cholate solution with a mass concentration of 1%, and use an ultrasonic cell disintegrator to perform pulse ultrasonic treatment (ultrasonic 5s, intermittent 5s), ultrasonic power 100W, pulse ultrasonic treatment time 60s, to obtain a primary emulsion, the primary emulsion was added dropwise to 1 ml of a second sodium cholate solution with a mass concentration of 0.1%, and the dichloride was removed by rotary steaming at a temperature of 37 ° C for 15 min. Methane to obtain a nanoparticle colloidal solution, which was placed in an ultrafiltration centrifuge tube with a molecular weight cut-off of 3 kDa, and after centrifugation at 5000 rpm for 45 min, the pr...

Embodiment 4-6

[0051] It was prepared by emulsification solvent evaporation method, and PLGA-PEG-OMe, PLGA-PEG-MAL and PLGA-PEG-FA were precisely weighed respectively, the total amount was 6 mg, and the weighing ratio was 4:1:1. Methyl chloride was dissolved, 2ml of the first sodium cholate solution with a mass concentration of 1% was added, and pulsed ultrasonic treatment was performed with an ultrasonic cell disintegrator (ultrasonic 5s, intermittent 5s), ultrasonic power 100W, and pulse ultrasonic treatment time were 30s, 60s, 90s , obtain the primary emulsion, add the primary emulsion dropwise to 1 ml of the second sodium cholate solution with a mass concentration of 0.1%, and rotate at 37 ° C for 15 min to remove dichloromethane 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 was collected to obtain the folic acid-targeting nanomicelles...

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Abstract

The invention provides a dual-targeting polymer drug nanocarrier, which belongs to the field of nano-biomedical materials. Modified with a tumor-targeting functional molecule and a brain-targeting peptide, the tumor-targeting functional molecule is folic acid, and the brain-targeting peptide and the nanomaterial are connected through a sulfhydryl-maleimide group; the present invention is biodegradable The polylactic-glycolic acid is the core, and the Angiopep-2 / folic acid dual-targeting polymer drug nanocarrier is obtained by surface modification of tumor-targeting functional molecules and brain-targeting peptides, which can effectively overcome the BBB barrier and target tumor cells at the same time. , which can be used as a nano-formulation encapsulating drug for targeted treatment of glioma.

Description

technical field [0001] The invention relates to the field of nanometer biomedical materials, in particular to a dual-targeting polymer drug nanocarrier and a preparation method and application thereof. Background technique [0002] Glioma is the tumor with the highest incidence in the central nervous system, accounting for about 46% of intracranial tumors. It is considered to be one of the most destructive and lethal tumors, with strong malignant proliferation ability, high infiltration ability and rapid Recurrence ability. Due to the unclear boundary between brain tumor tissue and normal tissue, it 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 the Some chemotherapeutic drugs are difficult to reach the brain tissue, and the concentration of drugs at the tumor site is low, which is not enough to kill tumor cells. Therefore,...

Claims

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Application Information

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Patent Type & Authority Patents(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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