Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Drug carrier, micelle, drug as well as preparation methods and application thereof

A carrier and drug technology, applied in the fields of drug carriers, micelles, medicaments and their preparation, can solve problems such as difficult to effectively control postoperative metastasis and recurrence process

Pending Publication Date: 2020-11-20
SICHUAN UNIV
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the strategy of regulating the above factors at a single site is difficult to effectively control the progression of postoperative metastasis and recurrence.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Drug carrier, micelle, drug as well as preparation methods and application thereof
  • Drug carrier, micelle, drug as well as preparation methods and application thereof
  • Drug carrier, micelle, drug as well as preparation methods and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Synthesis of embodiment 1 low molecular weight heparin and hydrophobic carotenoid copolymer

[0092] The purpose of this example is to exemplarily illustrate the synthesis method of low molecular weight heparin and hydrophobic carotenoid copolymer, and the characterization of low molecular weight heparin and hydrophobic carotenoid copolymer.

[0093] 1. Preparation of enoxaparin sodium and astaxanthin copolymer:

[0094] Accurately weigh 25.0 mg of astaxanthin, and dissolve it in 24.0 mL of N,N-dimethylformamide (DMF) at room temperature. In addition, 50.0 mg of low molecular weight heparin (enoxaparin sodium) was accurately weighed, dissolved in 3.0 mL of formamide under the condition of heating in a water bath at 60°C, and then 1-(3-dimethylaminopropyl)-3-ethyl carbon Diimine hydrochloride (EDC) 60.0 mg, N-hydroxysuccinimide (NHS) 36.0 mg and 4-dimethylaminopyridine (DMAP) 10.0 mg were stirred and activated at 25°C for 3 hours in the dark. After the activation was c...

Embodiment 2

[0099] Example 2 Structural Characterization of Low Molecular Weight Heparin and Hydrophobic Carotenoid Copolymer (Taking Example 1 Copolymer as an Example)

[0100] 1. The hydrogen spectrum confirmation of LMWH-AST copolymer:

[0101] Take 6.0 mg of the freeze-dried LMWH-AST sample powder, accurately weigh it, and dissolve it in 0.5 mL of D2O and DMSO-d6 respectively. And weigh 3.0mg of LMWH and 3.0mg of AST, respectively dissolved in 0.5mL of D2O and 0.5mL of DMSO-d6 as a reference sample. Proton nuclear magnetic resonance (1H-NMR) analysis was performed at 400 MHz.

[0102] The result is as figure 2 As shown, compared with the LMWH and AST spectra, the LMWH-AST sample forms forward micelles in D2O. In the spectra, a series of peaks between δ=3.5-5.5ppm are hydrogen peaks on the carbon chain skeleton in LMWH, and δ= 6.5ppm is the hydrogen peak on the carbon chain skeleton in AST. Taken together, the 1H-NMR results confirmed the successful synthesis of LANPs.

[0103] 2...

Embodiment 3

[0112] Synthesis of embodiment 3 fondaparinux sodium and astaxanthin copolymer

[0113] Accurately weigh 25.0 mg of astaxanthin, and dissolve it in 24.0 mL of N,N-dimethylformamide (DMF) at room temperature. In addition, accurately weigh 50.0 mg of fondaparinux sodium, dissolve it in 3.0 mL of formamide under the condition of heating in a water bath at 60°C, and then add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide salt Hydroxysuccinimide (EDC) 60.0mg, N-hydroxysuccinimide (NHS) 36.0mg and 4-dimethylaminopyridine (DMAP) 10.0mg, stirred and activated at 25°C for 3h in the dark. After the activation was completed, add 2 drops / s (about 40 μL / s) into the above-mentioned astaxanthin solution at a stirring speed of 600 rpm, and react in the dark at 30°C for 48 hours under the protection of argon (Ar). After the reaction was completed, the reaction solution was added into 3 times the volume of acetone at 0° C., shaken thoroughly, and then centrifuged at 4000 rpm at room temperature...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention relates to the field of drug preparations, and discloses a drug carrier, a micelle, a drug as well as preparation methods and application thereof. The drug carrier and the micelle comprise: A) a hydrophilic part comprising a hydrophilic heparin compound; and B) a hydrophobic part comprising one of hydrophobic carotenoid and vitamin A compounds, wherein the hydrophilic part and the hydrophobic part are linked in a specific manner. The drug carrier and the micelle not only have functions of blocking activation of an NF-[kappa]B signal pathway and an STAT3 signal pathway in an initial step in an inflammation feedforward loop, inhibiting recruitment of myeloid-derived suppressor cells in tumor parts and remote organs, inhibiting implantation of tumor cells in the remote organs and improving local immunosuppression microenvironments so as to inhibit tumor related inflammations, premetastatic niche reconstruction, tumor cell immune escape and strangle circulating tumor cells, but also can realize the best tumor and tumor metastasis inhabitation effects by further entrapping an anti-tumor drug.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical carrier, micelles, medicaments and their preparation methods and applications. Background technique [0002] Cancer is a serious threat to the health of modern humans. According to statistics from the National Cancer Center, about 3.929 million people were diagnosed with cancer in 2015 in my country, with an average of 7.5 people diagnosed every minute, and the trend is increasing year by year. At present, the treatment methods for cancer mainly include chemical drug therapy (chemotherapy), tumor radiation therapy (radiotherapy) and surgical resection. Among them, although chemotherapy can directly kill tumor cells and has a certain degree of tumor inhibition, it has a large toxic side effect and a single mechanism of action, so the therapeutic effect needs to be further improved. Therefore, if tumors can be inhibited from different mechanisms during c...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/36A61K9/107A61K31/704A61P35/00A61P35/04
CPCA61K47/36A61K9/1075A61K31/704A61P35/00A61P35/04Y02A50/30
Inventor 何勤卢正则龙洋李曼
Owner SICHUAN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com