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Preparation method and applications of irinotecan hydrochloride based anti-cancer nanoparticles

A technology for irinotecan hydrochloride and nanoparticles, which is applied in the field of preparation of anticancer nanoparticles, can solve the problems of low encapsulation rate, high synthesis cost, low active ingredients, etc. small amount of effect

Inactive Publication Date: 2014-12-03
NANKAI UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although people have developed a wide variety of nanocarriers, including liposomes, polymer nanoparticles, dendrimers, and inorganic nanoparticles, there are still only two main ways for them to combine with drugs: 1) Nanocarriers combine drug molecules physically Encapsulated inside it, the encapsulation rate of this method is usually lower than 10%, that is, the carrier is the main part, which results in lower active ingredients in the drug; 2) Link the drug molecule to the polymer or peptide chain through a covalent bond, through Self-assembled into nanoparticles in solution, this method is extremely expensive

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  • Preparation method and applications of irinotecan hydrochloride based anti-cancer nanoparticles
  • Preparation method and applications of irinotecan hydrochloride based anti-cancer nanoparticles
  • Preparation method and applications of irinotecan hydrochloride based anti-cancer nanoparticles

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[0019] A preparation method of anti-cancer nanoparticles based on irinotecan hydrochloride, as shown in the figure 1 As shown, the anticancer nanoparticles based on irinotecan hydrochloride are formed by supramolecular interaction of amphiphilic sulfonated calix[4]arene (SC4AH) and irinotecan hydrochloride (IRC), and the amphiphilic sulfonated calix [4] Aromatic hydrocarbon (SC4AH) and irinotecan hydrochloride (IRC) were dissolved in water and uniformly mixed to obtain a supramolecular nanoparticle solution, and the concentration of amphiphilic sulfonated calix[4]arene (SC4AH) in the supramolecular nanoparticle solution for 10 mu M, the concentration of irinotecan hydrochloride (IRC) is 40 mu M; The molar ratio of amphiphilic sulfonated calix[4]arene to irinotecan hydrochloride was 1:4. The loading rate of the nanoparticles was determined to be 65.17% by NMR.

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Abstract

The invention discloses an irinotecan hydrochloride based anti-cancer nanoparticle, which is formed by that amphipathic 4-sulfocalixnarene (SC4AH) and irinotecan hydrochloride (IRC) are subjected to supramolecular interaction, wherein the amphipathic 4-sulfocalixnarene provides a host-guest bonding site on the surface of the nanoparticle, carries out non-covalent modification on the surface of the nanoparticle, and is used for being combined with cationic targeting agent molecules so as to realize the delivery of targeted drugs. The irinotecan hydrochloride based anti-cancer nanoparticle disclosed by the invention has the advantages that 1) the nanoparticle is simple in preparation and less in application amount of raw materials; 2) because a drug molecule is one of construction units of the nanoparticle, the nanoparticle has a high load rate while protecting the drug molecule; and 3) the nanoparticle can non-covalently modify targeting agent molecules through the inclusion interaction of calixarene on the surface of the nanoparticle, so that the nanoparticle has a broad application prospect in the field of targeted delivery of anti-cancer drugs.

Description

technical field [0001] The invention belongs to the technical field of nano supramolecular materials, in particular to a preparation method and application of irinotecan hydrochloride-based anticancer nanoparticles. Background technique [0002] In recent years, nanotechnology has been widely used in the fields of materials science, optics, electricity and drug delivery. Among them, the application of nanotechnology in the field of drug delivery mainly focuses on the selective delivery of small molecules with drug activity to the lesion site and maximizes the therapeutic effect of drug molecules while reducing the side effects of drugs, see 1) I. Brigger, C . Dubernet, P. Couvreur. Adv. Drug Delivery Rev. 2002, 54 , 631?651; 2) O. C. Farokhzad, R. Langer. ACS Nano 2009, 3 , 16?20; 3) S. E. Erb. Drug Delivery Syst. 2009, 24 , 63?70. Although people have developed a wide variety of nanocarriers, including liposomes, polymer nanoparticles, dendrimers, and inorganic na...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/4745A61K9/51A61K47/26A61P35/00
Inventor 刘育王以轩郭东升王鲲鹏
Owner NANKAI UNIV