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Targeting nanoparticle with anti-ovarian cancer activity and preparation method and application thereof

A technology targeting nanoparticles and ovarian cancer. It is applied in the direction of organic active ingredients, medical preparations containing non-active ingredients, and medical preparations containing active ingredients. It can solve chemical instability, poor oral bioavailability, and low water solubility. sexual issues

Active Publication Date: 2019-03-08
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application of curcumin is limited by its chemical instability, low water solubility and poor oral bioavailability

Method used

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  • Targeting nanoparticle with anti-ovarian cancer activity and preparation method and application thereof
  • Targeting nanoparticle with anti-ovarian cancer activity and preparation method and application thereof
  • Targeting nanoparticle with anti-ovarian cancer activity and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1: Preparation of anti-ovarian cancer active nanoparticles

[0017] (1) Preparation of anti-ovarian cancer active nanoparticles

[0018] Carbodiimide (EDC) is used as an activator of carboxyl group, and the carboxyl group (SA) of stearic acid and the primary amino group of polyethyleneimine (PEI) are dehydrated and condensed to obtain PEI-SA. 199 mg of SA were pre-dissolved in 50 ml of hot ethanol, and 100 mg of PEI were respectively dissolved in 40 ml of distilled water. Then, they were mixed at 80°C with stirring. 750 mg of EDC was added to the mixture with stirring at 300 rpm for 24 hours. The reaction solution was dialyzed against 10% ethanol solution for 48 hours using a dialysis membrane (MWCO: 3.5 KDa, Spectrum Laboratories, Laguna Hills, CA) to remove by-products. Finally, it was dialyzed against distilled water for 2 hours, and the dialyzed product was lyophilized to collect PEI-SA. The PEI-SA solution was then coated with 5 mg / ml HA to obtain a (PE...

Embodiment 2

[0023] Example 2: Preparation of anti-ovarian cancer active nanoparticles

[0024] (1) Preparation of anti-ovarian cancer active nanoparticles

[0025] Carbodiimide (EDC) is used as an activator of carboxyl group, and the carboxyl group (SA) of stearic acid and the primary amino group of polyethyleneimine (PEI) are dehydrated and condensed to obtain PEI-SA. 199 mg of SA were pre-dissolved in 50 ml of hot ethanol, and 300 mg of PEI were dissolved in 40 ml of distilled water, respectively. Then, they were mixed at 80°C with stirring. 750 mg of EDC was added to the mixture with stirring at 300 rpm for 24 hours. The reaction solution was dialyzed against 10% ethanol solution for 48 hours using a dialysis membrane (MWCO: 3.5 KDa, Spectrum Laboratories, Laguna Hills, CA) to remove by-products. Finally, it was dialyzed against distilled water for 2 hours, and the dialyzed product was lyophilized to collect PEI-SA. The PEI-SA solution was then coated with 5 mg / ml HA to obtain a (P...

Embodiment 3

[0030] Example 3: Preparation of anti-ovarian cancer active nanoparticles

[0031] 1) Preparation of anti-ovarian cancer active nanoparticles

[0032] Carbodiimide (EDC) is used as a carboxyl activator to dehydrate and condense the carboxyl group (SA) of stearic acid and the primary amino group of polyethyleneimine (PEI) to obtain PEI-SA. 199 mg SA was pre-dissolved in 50 ml hot ethanol, and 500 mg PEI was dissolved in 40 ml distilled water, respectively. Then, they were mixed at 80° C. with stirring. 750 mg EDC was added to the mixture under stirring at 300 rpm for 24 hours. The reaction solution was dialyzed against 10% ethanol solution for 48 hours to remove by-products using a dialysis membrane (MWCO: 3.5 KDa, Spectrum Laboratories, Laguna Hills, CA). Finally, it was dialyzed against distilled water for 2 hours, and the dialyzed product was freeze-dried to collect PEI-SA. The PEI-SA solution was then coated with 5 mg / ml HA to obtain a lyophilized product of (PEI-SA)HA. ...

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Abstract

The invention provides a targeting nanoparticle with anti-ovarian cancer activity, which consists of stearic acid, polyethyleneimine and hyaluronic acid, and carried drugs are paclitaxel and curcumin,which respectively account for 0.4 percent of the nanoparticle and 0.4 percent of the nanoparticle. With carbodiimide as activator for the carboxyl group, the carboxyl group of the stearic acid and the primary amino group of the polyethyleneimine undergo dehydration condensation, and then mixed with the drugs, and after filtration and freeze drying, the drug-carrying targeting nanoparticle is prepared. According to the invention, by means of the polymer nanomaterial with cell uptake and cytoplasmic retention functions, the receptor-ligand characteristic is utilized to encapsulate the drugs with the target located in cells, consequently, the intake of the drugs by ovarian cancer cells is increased, the distribution of the drugs in normal tissues is reduced, reducing the toxic and side effects of the drugs, and moreover, the combination of the curcumin synergizes the toxicity of the paclitaxel to ovarian cancer cells, reversing drug resistance while enhancing the anti-ovarian cancer activity of the paclitaxel. The targeting nanoparticle disclosed by the invention can be applied in the preparation of targeting drugs with anti-ovarian cancer activity.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a targeted nanoparticle with anti-ovarian cancer activity, and preparation and application in the preparation of a drug for treating ovarian cancer. Background technique [0002] Compared with other gynecological malignancies, the incidence of ovarian cancer is relatively insidious. It has been reported that more than 75% of ovarian cancer patients are diagnosed at an advanced stage. In recent years, despite the continuous improvement in the treatment of ovarian cancer, its fatality rate is still the highest among female gynecological tumors. The five-year survival rate of ovarian cancer patients only increased from 33.7% in 1975 to 45.6% in 2011. The conventional treatment of ovarian cancer is to remove the visible tumor and residual disease through surgery and chemotherapy. Although ovarian cancer is sensitive to first-line chemotherapy drugs (such as paclitaxel), the effect is short-liv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/36A61K31/337A61K31/12A61P35/00
CPCA61K9/5146A61K9/5161A61K31/12A61K31/337A61P35/00A61K2300/00
Inventor 赵梦丹郑彩虹李君琴陈凤英罗琼费伟东杨佩磊陈玥
Owner ZHEJIANG UNIV
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