Myristic acid-mediated brain-targeting polymer micelle drug-delivery system and its preparation method and use

A technology of polymer glue and myristic acid, which is used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. The application has no relevant literature reports and other problems, and achieves the effect of facilitating subsequent development and industrialization, no immunogenicity, and improving the degree of concentration

Active Publication Date: 2014-12-03
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] So far, there is no relevant literature report on the preparation and application of myristic acid-mediated brain-targeted polymer micellar drug delivery system

Method used

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  • Myristic acid-mediated brain-targeting polymer micelle drug-delivery system and its preparation method and use
  • Myristic acid-mediated brain-targeting polymer micelle drug-delivery system and its preparation method and use
  • Myristic acid-mediated brain-targeting polymer micelle drug-delivery system and its preparation method and use

Examples

Experimental program
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Embodiment 1

[0051] Construct the targeted functional material (I), and combine the targeted functional material with the amphiphilic polymer material (II) and anti-tumor drugs in a certain proportion to make a polymer micelle drug delivery system; it includes:

[0052] (1) Fluorescence tracking of myristic acid-polymer micelles

[0053] Myristic acid and amino polyethylene glycol distearoylphosphatidylethanolamine are reacted at room temperature, and the product is purified by dialysis.

[0054] With the molar ratio of brain-targeted functional materials and amphiphilic polymer materials at 5:95, polymer micelles loaded with coumarin-6 (C6) and DiR were prepared by film-forming hydration method, and removed by gel chromatography. free fluorescein;

[0055] (2) Preparation of myristic acid-polymer micelles / DTX

[0056] The polymer micelles loaded with the chemical drug docetaxel (DTX) were prepared by using the film-forming hydration method with a molar ratio of brain-targeting funct...

Embodiment 2

[0063] Example 2 Preparation of myristic acid-polymer micelles / DTX (MC-micelles / DTX)

[0064] Myristic acid-aminopolyethylene glycol-distearoylphosphatidylethanolamine (MC-PEG-DSPE):

[0065] Weigh an appropriate amount of MC, dissolve it in DMF, add a certain amount of NHS and EDC·HCl to activate for 3 h, centrifuge to get the supernatant; weigh an appropriate amount of NH 2 - PEG-DSPE in DMF, add the supernatant drop by drop, then add 50 μL of DIEA, stir overnight at room temperature; precipitate the above reaction solution with glacial ether, centrifuge, and disperse the dried product with double distilled water after vacuum drying , purified by dialysis, and freeze-dried to obtain a white solid MC-PEG-DSPE; 1 H-NMR to verify its structure (500 MHz, CD 3 Cl) (eg figure 1 shown), the results show that: the compound has between 0.8-1.5ppm two The characteristic peak of stearyl phosphatidylethanolamine, the characteristic peak of polyethylene glycol appears between 3...

Embodiment 3

[0069] Example 3 BCECs cell uptake test of myristic acid-polymer micelles (MC-micelles)

[0070] Preparation of myristic acid-polymer micelles / C6 (MC-micelles / C6):

[0071] Coumarin-6 (C6)-labeled mPEG-micelles were prepared by film-forming hydration method. The specific preparation method was as follows: mPEG-DSPE was mixed with 50 μg fluorescent dye C6, vortexed for 1 min, and evaporated to dryness at 37°C. Form a film, dry in vacuum to remove residual organic solvent, add 200 μL of HEPES (pH 7.4, 10 mmol / L), vortex for 10 min, shake in a water bath at 37 °C for 2 h, use gel filtration chromatography, use G50 as filler, HEPES To remove unencapsulated C6 from the elution medium, mPEG-micelles / C6 was obtained after passing through a 0.22 μm microporous membrane; using the same preparation process, the molar ratio of MC-PEG-DSPE to mPEG-DSPE was 5:95, Prepare MC-micelles / C6, measure the C6 content with a fluorescence spectrophotometer, and calculate the content from the st...

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Abstract

The invention belongs to the technical field of polymers and medicinal preparations and relates to a myristic acid-mediated brain-targeting polymer micelle drug-delivery system and its preparation method and use. The myristic acid-mediated brain-targeting polymer micelle drug-delivery system is an antitumor drug-loading polymer micelle drug-delivery system comprising a brain-targeting functional material (I), an amphiphilic polymer material (II) and an antitumor drug. An in-vitro and in-vivo activity evaluation experiment proves that the myristic acid-mediated brain-targeting polymer micelle drug-delivery system is obviously superior to a common polymer micelle drug-delivery system, can go through a blood-brain barrier and delivery the drug into the brain, can substantially improve drug accumulation in the brain, has obviously antineoplastic effects and can be used for improving antineoplastic drug effects of treating brain tumors. The myristic acid-mediated brain-targeting polymer micelle drug-delivery system has a good application prospect.

Description

technical field [0001] The invention belongs to the technical field of polymer materials and pharmaceutical preparations, and relates to a novel brain-targeted polymer micelle drug delivery system, in particular to a myristic acid-mediated polymer micelle brain-targeted drug delivery system and its preparation methods and applications. Background technique [0002] Studies have reported that brain tumors are a common malignant disease of the central nervous system, including primary brain tumors and brain metastases. Because the brain tumor is close to the central nervous system of the patient, it is difficult to completely remove it with general clinical surgery, which often leads to tumor recurrence. Therefore, surgical resection of brain tumors combined with chemotherapy is usually used clinically for the prevention and treatment of tumor recurrence. [0003] So far, the targeted drug delivery system for the treatment of brain tumors has mostly used brain-targeted or tu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K9/107A61K45/00A61P35/00
Inventor 陆伟跃张智新谢操魏晓丽李瑾孟庆刚
Owner FUDAN UNIV
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