Drug nano preparation and preparation method thereof

A nano-preparation and drug technology, which is applied in the field of preparation of nano-drug-loaded preparations, can solve the problems of high expression level of transcription factor HIF1alpha in tumor cells, impermeability to tumor tissue, etc., to achieve increased penetration, increased toxicity, and simple preparation process Effect

Active Publication Date: 2017-10-24
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] However, at the tumor site, the extracellular matrix is ​​denser, the blood vessels are abnormal, and the interstitial fluid pressure is increased. Due to these factors, nanoparticles usually can only passively gather around the tumor blood vessels, but cannot penetrate the entire tumor tissue.
At the same time, the hypoxic characteristics of most solid tumors cause the expression level of the transcription factor HIF1alpha in tumor cells to be too high, which is one of the important reasons for the chemoresistance of tumors
[0005] The current traditional nano-preparation can not solve the above two problems well

Method used

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  • Drug nano preparation and preparation method thereof

Examples

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Effect test

Embodiment 1

[0052] 1. Preparation of 20% PEG2K-AZO-PAMAM (20% PEG grafting rate, PEG molecular weight 2000) nanocarrier

[0053] 1) Take 5mg of AZO, ultrasonically dissolve it in 3ml of pyridine, add 4.37mg of EDC·HCl, 2.56mg of NHS and 0.23mg of 4-DMAP, adjust the pH of the solution to 5 with 1mol / L HCl, and stir at room temperature for 2 hours to activate the carboxyl group of AZO .

[0054] 2) Dissolve 37mg of mPEG-NH2 (MW=2000) in 1ml of pyridine; slowly add the mPEG pyridine solution into the AZO solution under magnetic stirring, and add 5 μl of triethylamine dropwise; stir overnight at room temperature.

[0055] 3) Remove the pyridine solution by vacuum rotary evaporation at 50°C to obtain an orange-yellow film product. Add 10ml of pure water to redissolve, centrifuge at 3000rpm for 5min to remove free AZO precipitate, and obtain mPEG-AZO aqueous solution. Add 4.37mg EDC·HCl, 2.56mg NHS, adjust the pH of the solution to 5 with 1mol / L HCl, stir at room temperature for 2 hours, and ...

Embodiment 2

[0065] This embodiment removes mPEG-NH 2 The molecular weight of PEG5K-AZO-PAMAM is 5000, and the dosage is 92.5 mg, and other steps are the same as in Example 1 to prepare 20% PEG5K-AZO-PAMAM (20% PEG grafting ratio, PEG molecular weight 5000).

Embodiment 3

[0067] In this example, except that the dosage of 20.5% PAMAM (G5.0) was 200 μl, other steps were the same as in Example 1 to prepare 10% PEG2K-AZO-PAMAM (10% PEG grafting ratio, PEG molecular weight 2000).

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Abstract

The invention discloses a drug nano preparation and a preparation method thereof. The drug nano preparation comprises a nano carrier. The nano carrier is of a core-shell structure formed by a hydrophilic outer chain and a lyophobic core. The hydrophilic outer chain is a water soluble polymer or water soluble polysaccharide; the lyophobic core is polyamide-amine. siRNA is adsorbed to the surface of the lyophobic core and an anti-tumor drug and a lyophobic probe are buried therein; the hydrophilic outer chain is connected to the lyophobic core through azobenzene-4,4-dicarboxylic acid. The low-oxygen responsive nano carrier is prepared by connecting methoxyl polyoxamide (PEG) and polyamide-amine (PAMAM) through azobenzene-4,4-dicarboxylic acid and can be used for co-carrying chemotherapeutics and siRNA. The nano preparation not only is reduced in grain size and strong in penetrability under stimulation of low-oxygen micro-environment of tumor, but also is simple in preparation process, and the toxicity to tumor cells is increased.

Description

technical field [0001] The invention relates to the field of preparation of nano drug-loaded preparations, in particular to a drug nano preparation and a preparation method thereof. Background technique [0002] Cancer is the second leading cause of human death, and the high morbidity and mortality rates of tumors make it one of the major challenges in the medical field. Chemotherapy is still the most important means of tumor treatment, but the traditional standard chemotherapy often produces a variety of unavoidable side effects and systemic toxicity. The emergence of nano-delivery systems improves the targeting of drugs to tumor sites, allowing more drugs to accumulate in tumor sites, thereby greatly reducing the toxic and side effects on other normal tissues and organs. At present, several anti-tumor nano-preparations have been released, such as Doxil and Abraxane. [0003] In the prior art, there are many studies on anti-tumor nano-preparations. The design of nano dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/18A61K47/36A61K47/34A61K49/00A61K31/704A61K31/713A61P35/00
CPCA61K9/5146A61K9/5161A61K31/704A61K31/713A61K49/0021A61K2300/00
Inventor 韩旻谢智奇皇甫铭一郭望葳郭宁宁林梦婷王田田刘惠娜陈捷键高建青
Owner ZHEJIANG UNIV
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