Unlock instant, AI-driven research and patent intelligence for your innovation.

Drug delivery carrier and anti-tumor application thereof

A technology for delivering carriers and drugs, applied in anti-tumor drugs, drug combinations, capsule delivery, etc., can solve the problems of prone to hemolysis, inability to tumor sites, inability to effectively exert anti-tumor effects, and limiting the therapeutic effects of anti-tumor drugs.

Active Publication Date: 2022-04-22
ZHEJIANG UNIV HANGZHOU GLOBAL SCI & TECH INNOVATION CENT
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] An important reason for the poor anti-tumor effect of existing anti-cancer drugs is that the anti-cancer drugs have poor tumor blood vessel permeability and are difficult to be absorbed and taken up by tumor cells, etc., which greatly limits the therapeutic effect of anti-cancer drugs
Especially for tumors with low vascular permeability, because the tumor vascular endothelial cells are well-organized and tightly packed, and the gap between vascular endothelial cells is small, even when the drug is delivered to the blood vessels of these tumors, because the drug is well-organized and tightly packed tumor vascular endothelium It is difficult to effectively penetrate the gap between vascular endothelial cells and reach the microenvironment of the tumor site. Therefore, when the existing antitumor drugs are used to treat tumors with low vascular permeability, they pass through the traditional tumor permeability and retention effects ( Enhanced Permeability and Retention, EPR effect) cannot effectively penetrate from the gap of tumor blood vessels to the tumor site, and thus cannot effectively exert the anti-tumor effect
In addition, for tumors, even if anti-tumor drugs penetrate into the tumor site from tumor blood vessels, the absorption and uptake of anti-tumor drugs by tumor cells will reduce the anti-tumor effect, so that the anti-tumor effect of the drug cannot be effectively exerted
In addition, anti-tumor drugs are easy to accumulate in lysosomes, and various enzymes in lysosomes degrade the drugs, reducing the stability of the drugs in tumor cells, thereby reducing the anti-tumor effect of the drugs
[0004] Although nanocarriers provide many alternative strategies for chemotherapeutic drugs, however, existing drug-loaded nanoparticles have many disadvantages, for example, after intravenous administration, they are prone to sudden release and short blood circulation time, resulting in greater systemic toxicity. Side effects, low biological safety, such as prone to hemolysis and inability to effectively accumulate in the tumor site, in addition, the existing drug-loaded nanoparticles can not effectively penetrate into the tumor site from the tumor vascular space through the EPR effect (especially for tumors with low vascular permeability ) and the tumor has a poor ability to uptake the drug-loaded nanoparticles, so it cannot effectively achieve the anti-tumor effect
In addition, the existing drug-loaded nanoparticles are also easy to aggregate in lysosomes, and various enzymes in lysosomes degrade the nanoparticles and their loaded drugs, reducing the stability of drugs in tumor cells, thereby reducing the Anti-tumor effect

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 delivery carrier and anti-tumor application thereof
  • Drug delivery carrier and anti-tumor application thereof
  • Drug delivery carrier and anti-tumor application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0324] The present invention also provides a method for preparing the delivery carrier of the present invention, the method comprising the steps of:

[0325] (1) PEG-PCL-PEI is dissolved in an organic solvent to obtain an organic phase;

[0326] (2) mixing the organic phase with the water phase, removing the organic solvent to obtain a dispersion;

[0327] (3) After mixing the dispersion liquid and the aqueous albumin solution, they were stirred and mixed to obtain a delivery vehicle.

[0328] Specifically, the preparation method of the delivery carrier of the present invention is as described above in the first aspect of the present invention.

[0329] Typically, the delivery vector of the present invention is prepared by the method described in the examples of the present invention.

[0330] The present invention also provides a use of the delivery carrier of the present invention for preparing a drug-loaded drug complex, and the delivery carrier is used for: (i) promoting...

Embodiment 1

[0379] 1. Materials

[0380] 1.1 Preparation of PEG-PCL-PEI carrier material

[0381] The preparation and demonstration of PEG-PCL-PEI (molecular weight: 9500, PDI: 1.08, CMC: 0.723nM) and Cy5-labeled PEG-PCL-PEI (fluorescence grafting rate 3.9%) are as follows:

[0382] 1.1.1 Synthesis of PEG-PCL and PEG-PCL-PEI

[0383] Polyethylene glycol monomethyl ether (PEG, molecular weight: 2000) and caprolactone were used after strictly removing water. After heating and vacuum-drying a 50mL round-bottomed flask, PEG (2g, 1mmol) and caprolactone were sequentially added under nitrogen protection. Esters (10mL, 90mmol), stannous octoate (0.82g, 2mmol), stirred and reacted at 110°C for 24h, dissolved the mixture in a small amount of dichloromethane after cooling, precipitated with glacial ether three times, and finally filtered through a sand core funnel, and pumped the solid Vacuum drying gave 6 g of PEG-PCL with a yield of 75%.

[0384] Dissolve PEG-PCL (2g, 0.25mmol) in 20mL of anhy...

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

No PUM Login to View More

Abstract

The invention relates to a drug delivery carrier and an anti-tumor application thereof. Specifically, the invention provides a delivery carrier, which is characterized in that the delivery carrier comprises nanoparticles and albumin, and the nano material of the nanoparticles comprises PEG-PCL-PEI; and the albumin is used for modifying the nanoparticles. The delivery carrier disclosed by the invention can be used for loading a drug to form a drug compound of drug-loaded nanoparticles, and the drug-loaded nanoparticles can effectively permeate into a tumor part from a tumor vessel through endocytosis and exocytosis transport effects, and can be effectively absorbed and taken by tumor cells; the lysosome escape capability and the lysosome degradation avoiding capability are realized, the advantages of excellent long-time blood clearance half-life period, high system biological safety and the like are realized, and the anti-tumor effect of the medicine can be obviously improved.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a medicine delivery carrier and its anti-tumor application. Background technique [0002] Tumors are a serious threat to life and health, and the research on anti-tumor drugs and their delivery vehicles has become a research hotspot today. [0003] An important reason for the poor anti-tumor effect of existing anti-cancer drugs is that the anti-cancer drugs have poor tumor blood vessel permeability and are difficult to be absorbed and taken up by tumor cells, which greatly limits the therapeutic effect of anti-cancer drugs. Especially for tumors with low vascular permeability, because the tumor vascular endothelial cells are well-organized and tightly packed, and the gap between vascular endothelial cells is small, even when the drug is delivered to the blood vessels of these tumors, because the drug is well-organized and tightly packed tumor vascular endothelium It is difficult to effe...

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): A61K47/42A61K47/34A61K9/51A61K45/00A61K33/36A61P35/00
CPCA61K9/5169A61K9/5146A61K45/00A61K33/36A61P35/00
Inventor 王国伟陈丹飞方霞蔡鑫君刘衍朋
Owner ZHEJIANG UNIV HANGZHOU GLOBAL SCI & TECH INNOVATION CENT