Preparation method and applications of double-stage brain-targeting polymer micelle drug delivery system

A technology of polymer glue and drug delivery system, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. It is convenient for subsequent development and industrialization, the preparation method is simple, and the operation is easy.

Inactive Publication Date: 2018-07-31
HUBEI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

So far, there have been no reports on the preparation of bilevel brain-targeted micelles by host-guest molecular recognition and its application in the treatment of glioma

Method used

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  • Preparation method and applications of double-stage brain-targeting polymer micelle drug delivery system
  • Preparation method and applications of double-stage brain-targeting polymer micelle drug delivery system
  • Preparation method and applications of double-stage brain-targeting polymer micelle drug delivery system

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Effect test

Embodiment 1

[0054] A preparation method of a two-stage brain-targeted polymer micelle drug delivery system, the steps of which are:

[0055] A. Preparation of hydrophilic host molecules:

[0056] (1) Weigh 3 g of mono-(6-p-toluenesulfonyl)-cyclodextrin (6-OTs-β-CD), dissolve it in 20 mL of anhydrous ethylenediamine, and pour the mixed solution into a round bottom flask Placed in an oil bath to react. The reaction temperature is at 40 or 50 or 60 or 70 or 80 or 90 o C, the reaction time is 1 or 5 or 8 or 15 or 22 or 30 or 36 or 42 or 48 h. After the reaction, the reaction solution was dropped into 500 mL of acetone to obtain a precipitate, which was collected by suction filtration and dried in vacuo. The precipitate was purified by dissolution / reprecipitation twice, and dried in vacuo to obtain mono-6-ethylenediamine-β-cyclodextrin (M6-β-CD).

[0057] (2) Weigh 68.8 mg of mono-6-ethylenediamine-β-cyclodextrin (M6-β-CD) and maleimide-polyethylene glycol-succinimide ester (MAL-PEG-NHS )...

Embodiment 2

[0076] Application of a two-stage brain-targeting polymer micelle drug delivery system in the preparation of targeted drug carriers for the treatment or prevention of glioma (studies on anti-tumor activity in vivo and in vitro), the steps are:

[0077] A. Antitumor activity research in vitro:

[0078] (1) Cell uptake experiment

[0079] C6 cells were treated at 5.0×10 4 Cells / well were seeded into 24-well plates, and the cells were incubated in 1 mL DMEM containing 10% FBS for 24 hours. Then add free DOX solution, N-T micellar solution, D-T micellar solution (DOX content of 5 μg / mL) in fresh medium and incubate for 4 hours. After the cells were washed 3 times with PBS, fluorescent pictures of C6 cells were taken under a fluorescence microscope. At the same time, the cells were digested with trypsin and resuspended in PBS, and the uptake efficiency of the three materials by C6 cells was determined by flow cytometry.

[0080] The uptake efficiency of the three materials by b...

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Abstract

The invention relates to a preparation method and applications of a double-stage brain-targeting polymer micelle drug delivery system. According to the preparation method, the double-stage targeting micelle is formed via the subject-object interaction effect between hydrophilic molecules (Ang-2-polyethylene glycol-beta-cyclodextrin and cRGD-polyethylene glycol-beta-cyclodextrin) and hydrophobic molecule (adamantine-polycaprolactone-fluorescein isothiocyanate). The core of the double-stage targeting micelle can be used for coating hydrophobic anti-tumor drugs; entering into glioma cells throughblood cerebral barrier is realized by surface targeting peptide (Ang-2 and cRGD) induced endocytic pathway; chemotherapeutic curative effect is improved; toxic or side effect is reduced; the micelleis high in stability; the hydrophilic and hydrophobic chain length and the ratio are controllable; targeting efficiency is high; the preparation method is simple; operation is convenient; and subsequent development and industrialization are convenient.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparation technology and polymer materials, and more specifically relates to a preparation method of a two-stage brain-targeted polymer micelle drug delivery system, and also relates to a two-stage brain-targeted polymer micelle drug delivery system in Application in glioma targeting drug carrier. Background technique [0002] Glioma is the most common primary tumor of the central nervous system, accounting for about half of primary intracranial tumors. Traditional treatments include surgical resection, radiation therapy, and chemotherapy. However, due to the genetic heterogeneity and invasive growth of the tumor, it is difficult to completely remove the malignant tumor by surgery. It is reported that the 5-year survival rate of postoperative chemotherapy combined with radiotherapy is nearly 4 times higher than that of radiotherapy alone, indicating that chemotherapy is effective. Doxorubicin (D...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/61A61K47/59A61K47/64A61K31/704A61P35/00A61K31/025
CPCA61K31/025A61K31/704
Inventor 常聪郑国华
Owner HUBEI UNIV OF CHINESE MEDICINE
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