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

Preparation method of a class of pH-responsive amphiphilic rod-shaped doxorubicin polymer prodrug

A doxorubicin and amphiphilic technology, which is applied in the field of amphiphilic rod-shaped polymeric prodrugs and their preparation, can solve the problems of strong toxic and side effects, non-selectivity, low medical efficiency and the like, and achieve the effect of effective treatment

Active Publication Date: 2019-10-22
SOUTHWEST UNIV
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The most common problems of anticancer drug molecules including doxorubicin are poor water solubility, small molecular size and non-selectivity. In the process of drug delivery, there are poor blood circulation stability, low drug bioavailability, strong side effects and Low medical efficiency and other issues

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
  • Preparation method of a class of pH-responsive amphiphilic rod-shaped doxorubicin polymer prodrug
  • Preparation method of a class of pH-responsive amphiphilic rod-shaped doxorubicin polymer prodrug
  • Preparation method of a class of pH-responsive amphiphilic rod-shaped doxorubicin polymer prodrug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Preparation of pH-responsive Dex-P(MGMA)-b-P(OEGMA) amphiphilic rod-like polymeric prodrug

[0041] (1) Preparation of Dex-Br: Under the condition of argon atmosphere, the dextran (Dex) dissolved in the ionic liquid (1-allyl-3-methylimidazole chloride) was cooled to 0°C, and then N - A mixed solution of methylpyrrolidone (NMP) and N,N-dimethylformamide (DMF), then slowly add 2-bromoisobutyryl bromide (BIBB), ice bath for 0.5-2h, and then rise to room temperature (25 ℃) and react in the dark for 12-72 hours, then precipitate in deionized water, dissolve the precipitate with acetone, and repeat the purification three times to obtain a light yellow intermediate product, which is dried in a vacuum oven (25-30°C), and then the resulting The light yellow intermediate product was dissolved in NMP, cooled to 0°C, then slowly added BIBB, ice-bathed for 0.5-2h, then raised to room temperature (25°C) and reacted in the dark for 12-72h, then precipitated in deionized wate...

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
diameteraaaaaaaaaa
Login to View More

Abstract

The invention relates to the fields of chemical synthesis and biological representation, and more particularly, provides a preparation method and an application of a pH-responsive amphiphilic rod-likepolymer prodrug, which is represented as the drawing in the specification. The preparation method of the amphiphilic rod-like polymer material includes the following steps: 1) synthesizing a rod-likeATRP initiator on the basis of glucan; 2) introducing a pH-responsive hydrophobic block on the basis of ATRP reaction; 3) introducing a hydrophilic block on the basis of ATRP reaction to obtain an amphiphilic polymer material; 4) substituting an ester group on the terminal of MGMA by means of hydrazine hydrate, thus producing a pH-responsive precursor; 5) forming a hydrazone bond by means of a carbonyl group on adriamycin and an amino group on the polymer material, thus producing the pH-responsive polymer prodrug. By means of weak acidity of interior of cancer cells, the amphiphilic rod-likepolymer prodrug can selectively release a drug by means of pH-stimulating response. The polymer prodrug is high in micelle stability, is high in drug carrying capacity and enables drug release to be under stimulating response control.

Description

technical field [0001] The invention relates to the fields of chemical medicine and biological application, in particular to a pH-stimulated amphiphilic rod-like polymeric prodrug and its preparation and use. Background technique [0002] Doxorubicin (DOX) is one of the common anticancer drugs, its CAS number: 23214-92-8, chemical structure: C 27 h 29 NO 11 , relative molecular weight: 543.52, it can inhibit the synthesis of RNA and DNA, and has the strongest inhibitory effect on RNA. Adriamycin is a cycle non-specific drug, which has effects on a variety of tumors. Therefore, it is effective on tumor cells of various growth cycles All have a killing effect. Doxorubicin is mainly applicable to acute leukemia, and has a certain therapeutic effect on acute lymphoblastic leukemia and myeloid leukemia. It is generally used as a second-line drug, that is, it can be considered when the first-line drug is resistant. Its mechanism of action is mainly that the drug intercalates i...

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
Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/56A61K9/107A61K31/704A61P35/00C08B37/02C08F251/00C08F285/00C08F8/30C08F8/32C08F220/28
Inventor 许志刚石潇潇马晓倩白霜薛鹏康跃军
Owner SOUTHWEST 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