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A kind of preparation method of active targeting anticancer drug nanoparticles

An anti-cancer drug, active targeting technology, applied in drug combination, anti-tumor drugs, nanotechnology and other directions, can solve the problem of poor targeting of anti-tumor drugs, improve compliance, reduce the incidence and severity of adverse reactions , enhance the effect of curative effect

Active Publication Date: 2022-07-26
HEILONGJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The present invention solves the technical problem of poor targeting of existing anticancer drugs, and provides a preparation method for actively targeting anticancer drug nanoparticles

Method used

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  • A kind of preparation method of active targeting anticancer drug nanoparticles
  • A kind of preparation method of active targeting anticancer drug nanoparticles

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specific Embodiment approach 1

[0023] Embodiment 1: This embodiment is a preparation method of active targeting anticancer drug nanoparticles, which is specifically carried out according to the following steps:

[0024] 1. Dissolving 3,3'-dithiodipropionic acid (DTPA) in acetic anhydride, warming up to the reaction temperature and reacting, then recovering acetic anhydride under reduced pressure to obtain product A, washing product A with glacial ether to obtain 3 ,3'-dithiodipropionic anhydride (DTDPA);

[0025] 2. Add camptothecin (CPT) and 3,3'-dithiodipropionic anhydride (DTDPA) obtained in step 1 to anhydrous pyridine, stir and dissolve, and add 4-dimethylaminopyridine under ice-water bath conditions The anhydrous pyridine solution of (DMAP) was heated to the reaction temperature and reacted, and the solvent was evaporated under reduced pressure to obtain product B, which was washed with dilute hydrochloric acid solution, dissolved in methanol, filtered to remove insoluble impurities, then recovered me...

specific Embodiment approach 2

[0029] Embodiment 2: This embodiment is different from Embodiment 1 in that the reaction temperature of 3,3'-dithiodipropionic acid and acetic anhydride in step 1 is 80-150°C. Others are the same as the first embodiment.

specific Embodiment approach 3

[0030] Embodiment 3: This embodiment is different from Embodiment 1 or 2 in that the molar ratio of camptothecin to 3,3'-dithiodipropionic anhydride in step 2 is (0.25-3):1. Others are the same as in the first or second embodiment.

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Abstract

A preparation method of active targeting anticancer drug nanoparticles, and the invention relates to the field of anticancer drug preparation. The invention aims to solve the technical problem of poor targeting of existing antitumor drugs. Methods: 1. Preparation of 3,3'-dithiodipropionic anhydride; 2. Preparation of camptothecin-20-O-3,3'-dithiodipropionate; 3. Preparation of CUR-FA; 4. Preparation of CPT‑ss‑CUR‑FA; 5. Preparation of CPT‑ss‑CUR‑FA nanoparticles. The nanoparticle prepared by the invention can passively target the tumor site by enhancing the penetration and retention effects. After the drug enters the tumor cell, the disulfide bond is broken under the action of the reducing agent, and the P-glycoprotein inhibitor curcumin and camptothecin synergize. Anti-tumor effect, thereby enhancing the selectivity and curative effect on tumor sites and reducing side effects on normal tissues. The active targeting anticancer drug nanoparticle prepared by the invention is used in the field of cancer treatment.

Description

technical field [0001] The invention relates to the field of anticancer drug preparation. Background technique [0002] Tumors are still a major class of diseases with a very high mortality rate. The vast majority of antitumor drugs have the characteristics of poor water solubility, poor targeting and cytotoxicity, cannot directly reach tumor cells, and cause damage to normal cells, with high frequency and serious adverse reactions. Camptothecin and curcumin are both very effective drugs for the treatment of tumors, and have synergistic anti-tumor effects. Therefore, how to connect the two together to make a complex, so that the two can enter the cell at the same time to exert a better drug effect, is the focus of current research. SUMMARY OF THE INVENTION [0003] The invention aims to solve the technical problem of poor targeting of existing anti-tumor drugs, and provides a preparation method of active targeting anti-cancer drug nanoparticles. [0004] A preparation m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/12A61K31/4745A61K47/32A61K47/54A61K47/55A61P35/00B82Y5/00
Inventor 李强龚显峰赵学玲徐高成
Owner HEILONGJIANG UNIV
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