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A self-assembled nanoparticle loaded with anticancer drugs based on low-generation pamam dendrimers and its application in antitumor

A technology for self-assembling nanoparticles and dendrimers, applied in the field of biomedicine, can solve the problems of high production cost, complex reaction process, low yield, etc., and achieve significant therapeutic advantages and the effect of simple and easy operation.

Active Publication Date: 2020-05-08
FUZHOU UNIV
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Problems solved by technology

At present, the application of PAMAM is still mainly based on drug carriers. For example, patent CN201410271351 discloses a folic acid-PAMAM-ursolic acid nano drug with tumor targeting. The initial materials used in this nano drug are highly toxic G3 and G5 To replace polyamide-amine dendrimers (PAMAM), the amino groups on the surface of PAMAM need to be replaced with hydroxyl groups to reduce the toxicity of the material itself, and then folic acid and ursolic acid are reacted with the hydroxyl groups on the surface of PAMAM to finally synthesize the target product. The reaction process is complicated, the production cost is high, and the yield is not high, which limits its application to a certain extent

Method used

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  • A self-assembled nanoparticle loaded with anticancer drugs based on low-generation pamam dendrimers and its application in antitumor
  • A self-assembled nanoparticle loaded with anticancer drugs based on low-generation pamam dendrimers and its application in antitumor
  • A self-assembled nanoparticle loaded with anticancer drugs based on low-generation pamam dendrimers and its application in antitumor

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Embodiment Construction

[0058] In order to make the content of the present invention easier to understand, the technical solutions of the present invention will be further described below in conjunction with specific embodiments, but the present invention is not limited thereto.

[0059] 1. Preparation of EL@PAMAM(G0) / HA

[0060] At 50 °C, 100 µL of 25 µM erlotinib in absolute ethanol was quickly added to 700 µL of water with shaking (7 replicates were prepared), followed by 100 µL of 25, 50, 75, 100, 125 , 150, 175, and 200 µM PAMAM (G0) aqueous solutions were quickly added to the above solutions, and after shaking for one minute, 100 µL of 500 µM HA aqueous solutions were added to the above 7 solutions, and then shaken for 5 minutes. After the end, the sample was ultrasonically treated for 15 minutes, and then left at room temperature to prepare EL@PAMAM(G0) / HA self-assembled nanocomposites with different charge ratios.

[0061] 2. Preparation of EL@PAMAM(G1) / HA

[0062] At 50 °C, 100 µL of 250 µ...

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Abstract

The invention belongs to the technical field of biological medicines, and particularly relates to preparation of nanometer medicine delivery system EL@PAMAM / HA self-assembled nanoparticles and an application in anti-tumor field. On the basis of low-generation dendrimer PAMAM (G0 / G1) and tumor cell CD44 receptor targeted HA (hyaluronic acid), a targeted self-assembled nanometer medicine delivery system EL@PAMAM / HA NPs is prepared with a solvent exchange method. The small-molecule self-assembled nanometer carrier system can encapsulate erlotinib as an antitumor medicine, has a pH response property, releases more medicines under the acidic condition, can target tumor cells with high expression of CD44, and can specifically deliver more therapeutic medicines to a tumor site to play pharmacodynamic effect, thereby having a significant therapeutic advantage.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to the preparation and anti-tumor application of a nano drug delivery system EL@PAMAM / HA self-assembled nanoparticle. Background technique [0002] Erlotinib, whose general trade name is Tarceva, is an anti-tumor targeted therapy drug officially approved by the US FDA in 2004, and has also been certified by my country's State Food and Drug Administration (CFDA). And it was approved to enter the Chinese market in 2007. The chemical structural formula of erlotinib (abbreviated as EL in the present invention) is [0003] [0004] , the chemical name is N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinolineamine hydrochloride, which is a kind of epidermal growth factor receptor (Epithelial Growth Factor Receptor, EGFR) are highly selective small molecule quinazoline derivatives. EL is used for the third-line treatment of locally advanced or metastatic non-small ce...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/36A61K31/517A61P35/00
CPCA61K9/5146A61K9/5161A61K31/517
Inventor 邵敬伟沈志春吴月煌
Owner FUZHOU UNIV
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