Heparin nano-drug loading system for loading amino anti-tumor drug and preparation method of heparin nano-drug loading system

An anti-tumor drug and nano-drug loading technology, which is applied in the field of medicine, can solve the problems of being unable to pass through, difficult to act on the target site, and poor biocompatibility of the carrier, so as to achieve a large safe dose and prevent degradation or degradation of external factors. It is the effect of non-essential metabolic inactivation and reduction of toxic and side effects

Active Publication Date: 2020-12-25
NANJING KING FRIEND BIOCHEM PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although a large number of researches on nano-drug carriers have been reported, there is still the problem of poor biocompatibility of the carriers. Some of them will be cleared by the reticuloendothelial system (RES) after entering the body, and some cannot pass through the cell membrane, nuclear membrane, etc. barrier, it is difficult to act on the target site

Method used

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  • Heparin nano-drug loading system for loading amino anti-tumor drug and preparation method of heparin nano-drug loading system
  • Heparin nano-drug loading system for loading amino anti-tumor drug and preparation method of heparin nano-drug loading system
  • Heparin nano-drug loading system for loading amino anti-tumor drug and preparation method of heparin nano-drug loading system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Daunorubicin is loaded on the PEGylated heparin molecule, the structure is as follows:

[0044] ,

[0045] in,

[0046] PEG-HP stands for PEGylated heparin polymer with the structure:

[0047] ,

[0048] can also be

[0049]

[0050] Wherein, the acyl group is connected to the hydroxyl group at the end of polyethylene glycol through an ester bond.

Embodiment 2

[0052] Lenalidomide is loaded on the PEGylated heparin molecule with the following structure:

[0053]

[0054] PEG-HP stands for PEGylated heparin polymer with the structure:

[0055] ,

[0056] can also be

[0057]

[0058] Wherein, the acyl group is connected to the hydroxyl group at the end of polyethylene glycol through an ester bond.

Embodiment 3

[0060] Lapatinib is loaded on the PEGylated heparin molecule with the following structure:

[0061]

[0062] PEG-HP stands for PEGylated heparin polymer with the structure:

[0063] ,

[0064] can also be

[0065]

[0066] Wherein, the acyl group is connected to the hydroxyl group at the end of polyethylene glycol through an ester bond.

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Abstract

The invention discloses a heparin nano-drug loading system for loading an amido anti-tumor drug. The drug loading system is a conjugate for loading the amido anti-tumor drug on PEGylated heparin molecules. Natural polysaccharide heparin which is biodegradable, good in compatibility and high in availability is used as a drug carrier, and PEG modification and the amino anti-tumor drug are combined,so that nanoparticles show an anti-tumor treatment index and biological safety which are remarkably enhanced compared with those of a free drug in in-vivo treatment.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a heparin nano-drug loading system loaded with amine-based antitumor drugs and a preparation method thereof. Background technique [0002] At present, anti-tumor drug carriers are developing rapidly, various emerging drug delivery systems are emerging, and nano drug delivery systems based on macromolecular biomaterials have emerged as the times require. A multifunctional drug delivery system developed by combining macromolecular biomaterials and small molecule drugs through physical embedding or chemical bonding, using the EPR effect of macromolecular carrier materials on solid tumors, macromolecular carrier materials can make drugs selectively enrich in tumor sites set to achieve passive targeting. And through the specific physiological characteristics of the tumor site compared with normal tissues, such as pH value, GSH level or the concentration of specific enzymes, the inte...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K47/60A61K47/69A61K31/704A61K31/454A61K31/517A61P35/00
CPCA61K47/61A61K47/60A61K47/6907A61K31/704A61K31/454A61K31/517A61P35/00Y02P20/55A61K31/136A61K31/166A61K31/506A61K31/7068A61K31/7076
Inventor 李方年石坚田欣欣
Owner NANJING KING FRIEND BIOCHEM PHARMA CO LTD
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