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

Polymersome with hydrophilic lumen carrying anthracene ring medicines as well as preparation method and application

An anthracycline and polymer technology is applied in the field of drug carriers to achieve the effects of good in-vitro stability and high drug encapsulation efficiency

Inactive Publication Date: 2015-07-15
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
View PDF4 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no literature report on the loading of hydrophilic anthra

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
  • Polymersome with hydrophilic lumen carrying anthracene ring medicines as well as preparation method and application
  • Polymersome with hydrophilic lumen carrying anthracene ring medicines as well as preparation method and application
  • Polymersome with hydrophilic lumen carrying anthracene ring medicines as well as preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] A kind of polycaprolactone-b-polyethylene glycol-b-polycaprolactone (PCL-b-PEG-b-PCL) amphiphilic triblock copolymer is made by following method: (PCL 2000 -b-PEG 2000 -b-PCL 2000 )

[0036] (1) ε-caprolactone (ε-CL) by calcium hydride (CaH 2 ) is dried and distilled under reduced pressure for subsequent use; polyethylene glycol 2000 (PEG, molecular weight 2000) is azeotropically dehydrated with toluene;

[0037] (2) Weigh 5g PEG 2000 and 10g ε-CL and add them to the dry polymerization tube treated by silanization, add stannous octoate as catalyst, and the added mass of the catalyst is the reactant (PEG 2000 and ε-CL) 0.1% of the mass, and then the system was vacuum-filled with nitrogen for 3 times, vacuum-sealed, and placed in a 120°C constant temperature oil bath to react for 12 hours to obtain a polymer;

[0038] (3) Dissolve the polymer in a small amount of dichloromethane, pour a large amount of petroleum ether for re-precipitation, and vacuum-dry the precipita...

Embodiment 2

[0040] a PCL 4000 -b-PEG 4000 -b-PCL 4000 Amphiphilic triblock copolymers prepared by the following method:

[0041] (1) ε-CL via CaH 2 Dry and distill under reduced pressure for later use; PEG 4000 is azeotropically dehydrated with toluene;

[0042] (2) Weigh 5g of PEG 4000 and 10g of ε-CL and add them to the dry polymerization tube treated with silanization, add stannous octoate as catalyst, and the added mass of the catalyst is the reactant (PEG 4000 and ε-CL) 0.1% of the mass, and then the system was vacuum-filled with nitrogen for 3 times, vacuum-sealed, and placed in a 160°C constant temperature oil bath to react for 16 hours to obtain a polymer;

[0043] (3) Dissolve the polymer in a small amount of dichloromethane, pour a large amount of anhydrous ether for reprecipitation, and vacuum dry the precipitate at 40°C to constant weight to obtain PCL 4000 -b-PEG 4000 -b-PCL 4000 Amphiphilic triblock copolymers.

Embodiment 3

[0045] a PCL 6000 -b-PEG 6000 -b-PCL 6000 Amphiphilic triblock copolymers prepared by the following method:

[0046] (1) ε-CL via CaH 2 Dry and distill under reduced pressure for later use; PEG 6000 is azeotropically dehydrated with toluene;

[0047] (2) Weigh 5g PEG 6000 and 10g ε-CL and add them to the dry polymerization tube treated by silanization, add stannous octoate as catalyst, and the addition quality of the catalyst is the reactant (PEG 6000 and ε-CL) 0.1% of the mass, and then the system was vacuum-filled with nitrogen for 3 times, vacuum-sealed, and placed in a 160°C constant temperature oil bath to react for 16 hours to obtain a polymer;

[0048] (3) Dissolve the polymer in a small amount of dichloromethane, pour a large amount of anhydrous methanol for reprecipitation, and vacuum dry the precipitate at 40°C to constant weight to obtain PCL 6000 -b-PEG 6000 -b-PCL 6000 Amphiphilic triblock copolymers.

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 discloses a polymersome with a hydrophilic lumen carrying anthracene ring medicines as well as a preparation method and an application. The preparation method comprises the following steps: (1) dissolving a PCL-b-PEG-b-PCL amphiphilic triblock copolymer in an organic solvent, carrying out rotary evaporation in a rotary evaporator to remove the organic solvent, forming a layer of uniform film on the inner wall of an eggplant-shaped bottle, and drying the film; (2) adding an ammonium sulfate water solution, carrying out hydration, oscillating the materials to mix the materials uniformly, and carrying out ultrasonic treatment in an ice bath to obtain a stable blank polymersome dispersion liquid; (3) dialyzing the blank polymersome dispersion liquid; (4) dissolving water-soluble anthracene ring medicines in deionized water, adding the solution to the blank polymersome dispersion liquid, and stirring the solution; cooling the product to the room temperature and dialyzing the product, thus obtaining the polymersome with the hydrophilic lumen carrying the anthracene ring medicines. The polymersome has good in vivo and in vitro stability and higher entrapment efficiency and effectively gathers on tumor sites, thus achieving the aim of targeted therapy.

Description

technical field [0001] The invention belongs to the field of drug carriers, and relates to polymer vesicles loaded with anthracycline drugs in a hydrophilic inner cavity, a preparation method and an application thereof Background technique [0002] Malignant tumors are one of the three major diseases that seriously threaten human health today, and chemotherapy is one of the important means of non-surgical treatment of malignant tumors. In recent years, with the in-depth study of the mechanism of action of chemotherapeutic drugs and the continuous discovery of new chemotherapeutic drugs, the level of clinical tumor treatment has been greatly improved. However, there are still many unsatisfactory effects of tumor chemotherapy, mainly due to the lack of selectivity of chemotherapy drugs on tumor cells and normal cells, so they show strong toxic and side effects on normal cells. In order to improve the targeting and bioavailability of anti-tumor drugs, reduce toxic and side eff...

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): A61K9/50A61K31/136A61K31/704A61P35/00
Inventor 张琳华朱敦皖董霞孙洪范孔德领
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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