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A kind of Xanthiting nano-micelle targeting dendritic cells and its preparation method and application

A technology of nano-micelle and dendritic cells, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, and pharmaceutical formulations to reduce non-specific phagocytosis, enhance the concentration of action, and facilitate the collection and concentration poly effect

Active Publication Date: 2021-06-01
SHANDONG PROVINCIAL HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

After patent and literature search, there is no report on the research related to Xanthin nano-micelle preparations

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  • A kind of Xanthiting nano-micelle targeting dendritic cells and its preparation method and application
  • A kind of Xanthiting nano-micelle targeting dendritic cells and its preparation method and application
  • A kind of Xanthiting nano-micelle targeting dendritic cells and its preparation method and application

Examples

Experimental program
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Embodiment 1

[0045] (1) NGR-modified targeted polymer synthesis

[0046] Its preparation method includes: dissolving NHS-PEG-PDLLA and NGR in borate buffer (Borate-buffered saline, PH = 9.0) at a molar ratio of 2:1, reacting at room temperature and stirring for 12 h, then dialyzing with distilled water ( MWCO3500da) was purified and freeze-dried to obtain NGR-PEG-PDLLA. The resulting product is used 1 H NMR for structural identification, the results are as follows figure 1 .

[0047]Results and analysis: Figure A is the synthesis route of the NGR-modified nanomaterial NGR-PEG-PDLLA. Figure B, Figure C and Figure D are the NMR spectra of the starting material NHS-PEG-PDLLA, NGR and the product NGR-PEG-PDLLA in the synthesis scheme, in which the ellipse represents the characteristic peak of NGR, and the reaction product spectrum shows the characteristic peak on NHS (δ 2.65 ppm) disappeared, while the characteristic peak of NGR appeared, indicating that NGR was successfully connected to t...

preparation example 1

[0050] Preparation Example 1: Weigh 36 mg carrier material (35.1 mg mPEG 2000 -PDLLA 2000 and 0.9 mg NGR-PEG 2000 -PDLLA 2000 ) and 2 mg Xanthiting were placed in a round bottom flask, 4 mL of absolute ethanol was added, and the carrier material and drug were fully dissolved by ultrasonication. The solution was placed in a rotary evaporator at 60 °C for 30 min to evaporate the organic solvent completely to obtain a dry and transparent mixed film matrix. Then 10 mL of water for injection preheated at 60°C was added, hydrated to form micelles under stirring conditions, and then passed through a 0.22 μm sterile filter membrane for fine filtration to sterilize, and the filtrate was freeze-dried to obtain a sample. The result is as figure 2 shown.

[0051] Preparation method of fluorescence-loaded targeting polymer micelles (NGR-DiI-PM):

preparation example 2

[0052] Preparation example 2: Weigh 36 mg carrier material (35.1 mg mPEG 2000 -PDLLA 2000 and 0.9 mg NGR-PEG 2000 -PDLLA 2000 ) and 2 mg of fluorescent dye DiI were placed in a round bottom flask, 4 mL of absolute ethanol was added, and the carrier material and drug were fully dissolved by ultrasonication. The solution was placed in a rotary evaporator at 60 °C for 30 min to evaporate the organic solvent completely to obtain a dry and transparent mixed film matrix. Then 10 mL of water for injection preheated at 60°C was added, hydrated to form micelles under stirring conditions, and then passed through a 0.22 μm sterile filter membrane for fine filtration to sterilize, and the filtrate was freeze-dried to obtain a sample.

[0053] Preparation method of blank targeting polymer micelles:

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to a xanthin nano-micelle targeting dendritic cells, a preparation method and application thereof. Xanthiting nano-micelle is obtained by blending non-targeting polymer material and targeting polymer material with Xanthiting, and the average particle size of the Xanthiting nano-micelle is 17.83±0.28nm. The mass ratio of oriented polymer material, non-targeted polymer material and xanthin is 0.9:35.1:2. The preparation method is as follows: dissolving targeting polymer material, non-targeting polymer material and xanthin in absolute ethanol, mixing evenly, removing absolute alcohol, adding water, filtering and freeze-drying. The polymer micelle can realize active targeting, which is beneficial to the collection and concentration of drugs to the inflammatory area, reduces the non-specific phagocytosis of xanthin by other cells, and enhances the effective activity of xanthin in dendritic cells. The effective concentration can inhibit the recurrence of allergic rhinitis, and the effect is better than that of budesonide.

Description

[0001] field of invention [0002] The invention belongs to the technical field of medicines, and in particular relates to a xanthin nano-micelle targeting dendritic cells, a preparation method and application thereof. Background technique [0003] Allergic rhinitis (AR) is an inflammatory disease characterized by excessive differentiation of TH2 cells. It is one of the most common chronic diseases, affecting 40% of the world's population. Due to its high incidence and refractory Human health and quality of life, increasing social and economic burden, has become a global health problem. The prevalence of AR continues to increase worldwide. Drug therapy and immunotherapy are currently the main methods of AR treatment. However, high relapses due to insufficient immune tolerance or severe side effects caused by long-term treatment, as well as rapid loss of drugs are still important. The main problem of clinical application. In recent years, dendritic cells (DC) have become a ho...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/34A61K47/18A61K31/365A61P11/02A61P37/08
CPCA61K9/1075A61K31/365A61K47/18A61K47/34A61P11/02A61P37/08
Inventor 夏明王成赵苗青刘成程孙超郑雪
Owner SHANDONG PROVINCIAL HOSPITAL
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