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A tumor interstitial pH-sensitive targeting dendrimer and preparation method thereof

A dendritic polymer and tumor stroma technology, applied in the field of medicine, can solve problems such as toxic side effects, blood cell destruction, application limitations, etc., and achieve the effect of reducing toxic side effects and promoting transport

Inactive Publication Date: 2018-03-09
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the positive charge enriched on the surface of unmodified PAMAM will lead to the destruction of blood cells, causing serious toxic side effects, and it is easily recognized and phagocytized by macrophages, which greatly limits its application.
Therefore, many studies have been devoted to modifying the surface of dendrimers to cover up their positive charges. Among them, grafting polyethylene glycol (PEG) is the main modification method, but this method can reduce the toxic and side effects of the carrier as well as cell entry

Method used

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  • A tumor interstitial pH-sensitive targeting dendrimer and preparation method thereof
  • A tumor interstitial pH-sensitive targeting dendrimer and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0016] Preparation of pH-sensitive targeting dendrimers

[0017] Step 1, preparation of CMCS: Dissolve 1 g of chitosan in 15 mL of 50% wt NaOH solution, alkalinize for 24 h and then filter with suction, add the obtained solid I to 2.5 times the weight of chloroacetic acid, and react at room temperature for 24 h After suction filtration, add 50 mL of water to dissolve the obtained solid II, adjust the pH of the solution to 7.0 with 2M HCl, centrifuge the solution, add 100 mL absolute ethanol to the supernatant, suction filter, wash the obtained solid III with absolute ethanol, and The solid III was dried at 30°C, dissolved in 10 mL of water, dialyzed in water to remove impurities with a dialysis bag with a molecular weight of 3500, and freeze-dried for 72 hours to obtain 0.89 g of a white product.

[0018] figure 1 For the selected chitosan of embodiment 1 and the infrared spectrogram of the carboxymethyl chitosan of preparation. Infrared spectrum analysis shows that the main...

Embodiment 2

[0024] In vitro cellular uptake assay

[0025] Using the commercially available doxorubicin solution as a control, an in vitro cell uptake test was carried out to investigate the targeting and ability of the pH-sensitive targeting dendrimer obtained in Example 1 to promote cell uptake.

[0026] Human breast cancer MCF-7 cells were cultured at a density of 1×10 5 Cells / well were seeded in 24-well plates and cultured for 24 hours. Thereafter, cells were treated with fresh medium (pH 6.5 and pH 7.4) containing samples (doxorubicin solution and targeting dendrimer obtained in Example 1, the same final doxorubicin concentration was 6.95 µg / mL) for 4 h (37°C). After the cells were incubated for 4 h, they were washed 3 times with fresh PBS, and then the cells were digested with trypsin. After discarding the trypsin, the cells were made into a cell suspension with PBS. After centrifugation at 1000 r / min for 5 min, the supernatant was discarded, and 200 Disperse the cells in µL PBS,...

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Abstract

The invention discloses a tumor interstitial pH-sensitive targeting dendrimer and a preparation method thereof. The general formula of the dendrimer is CMCS-PAMAM-X, wherein, CMCS is carboxymethyl chitosan, PAMAM It is a cationic polyamidoamine dendrimer of the 5th generation, and X is doxorubicin. The preparation method sequentially includes three steps of preparation of CMCS, preparation of drug-loaded PAMAM inner core and preparation of pH-sensitive targeting dendrimers. The dendrimers of the present invention can not only realize the targeted delivery of drugs to tumor tissues, reduce the toxic and side effects of tumor-targeted drug-loaded delivery systems on normal tissues, but also promote the transport of carriers across tumor cell membranes and increase the drug delivery in tumor cells. Accumulation improves the curative effect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tumor interstitial pH-sensitive targeting dendrimer and a preparation method thereof. Background technique [0002] Functional polymer materials have become a hotspot in the research of tumor-targeted drug delivery systems. In recent years, a large number of functional materials have been used to prepare tumor-targeted drug delivery systems, including various liposomes, micelles, and microemulsions. However, these targeted drug-loaded delivery systems still have many disadvantages, such as poor cell entry ability and limited solubilization ability for insoluble drugs. Cationic carrier polyamidoamine (PAMAM) dendrimer macromolecule is a new type of highly branched functional material, which has the advantages of high water solubility, modifiable terminal functional groups, and large internal hydrophobic cavity. Due to the small particle size of PAMAM (5-10nm), it ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/61A61K47/59A61K31/704A61P35/00C08G83/00
Inventor 吴正红钦佳怡单其磊祁小乐秦晓雪杨蓉李文艳
Owner CHINA PHARM UNIV
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