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Pegized heparin nanomicelle loaded with carboxylic acid antineoplastic drug and preparation method thereof

一种抗肿瘤药物、纳米胶束的技术，应用在医药领域，能够解决很难作用于靶向位点、无法通过、载体生物相容性差等问题

Active Publication Date: 2021-09-14
KINDOS PHARM 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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  • Pegized heparin nanomicelle loaded with carboxylic acid antineoplastic drug and preparation method thereof
  • Pegized heparin nanomicelle loaded with carboxylic acid antineoplastic drug and preparation method thereof
  • Pegized heparin nanomicelle loaded with carboxylic acid antineoplastic drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0044]

[0045] in,

[0046]

[0047] PEG-HP stands for PEGylated heparin polymer with the structure:

[0048]

[0049]can also be

[0050]

[0051] Wherein, the acyl group is connected to the hydroxyl group at the end of polyethylene glycol through an ester bond.

Embodiment 2

[0053] Loading bendamustine on PEGylated heparin molecules, the structure is as follows:

[0054]

[0055] PEG-HP stands for PEGylated heparin polymer with the structure:

[0056]

[0057] can also be

[0058]

[0059] Wherein, the acyl group is connected to the hydroxyl group at the end of polyethylene glycol through an ester bond.

Embodiment 3

[0061] Load raltitrexed on the PEGylated heparin molecule, the structure is as follows:

[0062]

[0063] PEG-HP stands for PEGylated heparin polymer with the structure:

[0064]

[0065] can also be

[0066]

[0067] 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 PEGylated heparin nano-micelle loaded with carboxylic acid antineoplastic drugs. The drug loading system is a conjugate of carboxylic acid antineoplastic drugs loaded on PEGylated heparin molecules. Using the natural polysaccharide heparin, which is biodegradable, good compatibility and high availability, as a drug carrier, by combining PEG-modified and carboxylic acid anti-tumor drugs, the nanoparticles exhibit significantly enhanced anti-tumor therapy than free drugs in in vivo treatment Index and biosecurity.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a PEGylated heparin nano-micelle loaded with carboxylic acid 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 in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/60A61K47/61A61K31/519A61K31/4184A61P35/00
CPCA61K47/6907A61K47/60A61K47/61A61K31/519A61K31/4184A61P35/00A61K47/545A61K31/517
Inventor 李方年石坚田欣欣
Owner KINDOS PHARM CO LTD