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

Polymer with tumor organization pH responsiveness and micelle thereof

A tumor tissue and polymer glue technology, applied in the field of biological materials, polymer materials, and pharmaceutical preparations, can solve problems such as side effects and hinder the clinical application of drugs, and achieve good biocompatibility.

Inactive Publication Date: 2010-07-28
FUDAN UNIV
View PDF2 Cites 49 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the vast majority of anticancer drugs have serious side effects, hindering the clinical application of drugs

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
  • Polymer with tumor organization pH responsiveness and micelle thereof
  • Polymer with tumor organization pH responsiveness and micelle thereof
  • Polymer with tumor organization pH responsiveness and micelle thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Add 30g of dihydroxypolyethylene glycol (1500) into a 500ml three-necked flask, remove water under vacuum at 130°C for 4 hours, cool to 70°C with argon, add 60g of lactide, 26mg of stannous octoate (containing a small amount of toluene), 100 ℃ for 30 minutes in vacuum, argon gas flowed, and the temperature was raised to 130 ℃ for 12 hours. After the reaction is complete, the product is poured out while it is hot, and after cooling, the product is dissolved in dichloromethane and precipitated with ether to obtain a BAB type block polymer. Take 15 g of BAB block polymer, add 3.0 g of N-Boc-histidine, 3.5 g of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC·HCl), 4 - Dimethylaminopyrimidine (DMAP) 2.6g, dichloromethane 150ml, react at room temperature for 48 hours. Part of the solvent was removed by suspension evaporation, precipitated with ether, further washed at 80°C to remove residual unreacted substances and catalyst, and freeze-dried. Synthesis sche...

Embodiment 2

[0035] The product obtained in Example 1 was formulated into a 1 wt% solution with a phosphate buffer solution, the pH was adjusted, and filtered through a 0.8 micron filter head to obtain the required blank micellar solution. The prepared micelles can be degraded, see figure 2. 1 mg of doxorubicin hydrochloride and triethylamine were co-dissolved in methanol / chloroform (volume ratio 1:1, the same below), and the methanol / chloroform solution (2ml, 5mg / ml) containing the polymer was added dropwise, and spin Dry to form a film, add phosphate buffer for hydration, filter with a 0.8 micron filter head, and dialyze to remove free doxorubicin to obtain micelles loaded with doxorubicin. The release rate of drug-encapsulated micelles is different between the normal pH (7.4) of the human body and the pH (6.2) of the extracellular fluid in tumor tissue, see image 3 . The human breast cancer cell line MDA-MB-435 and cell culture medium were cultured in a six-well cell culture plate ...

Embodiment 3

[0037] Add 30g of dihydroxypolyethylene glycol (1500) into a 500ml three-necked flask, remove water under vacuum at 130°C for 4 hours, cool to 70°C with argon, add 50g of lactide, 10g of glycolide, 26mg of stannous octoate (solution in toluene), evacuate at 100°C for 30 minutes, pass argon, and raise the temperature to 130°C for 12 hours. After the reaction is complete, the product is poured out while it is hot, and after cooling, the product is dissolved in dichloromethane and precipitated with ether to obtain a BAB type block polymer. Take 10 g of BAB block polymer, add 1.8 g of N-Boc-histidine, 1.7 g of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC·HCl), 4 - Dimethylaminopyrimidine (DMAP) 1.3g, dichloromethane 150ml, react at room temperature for 48 hours. Part of the solvent was removed by suspension evaporation, precipitated with ether, further washed at 80°C to remove residual unreacted substances and catalyst, and freeze-dried. The obtained product w...

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 belongs to the technical field of pharmaceutical preparations and high molecular materials, in particular to a polymer with tumor organization pH responsiveness, a micelle and a preparation method thereof. In the invention, an amphipathic block polymer is firstly synthesized, and histidine with pH-sensitive groups or a derivate thereof is introduced to the both ends of the amphipathic block polymer. The materials are dissolved in an aqueous solvent in definite proportion to form the micelle by self-assembly; or the materials and medicines are dissolved in an organic solvent together to form a membrane by rotation, and then the membrane is dispersed in water to form a medicine-carrying micelle. The size of the micelle can be controlled by the pH adjustment. The medicine-carrying micelle has different medicine releasing rates for the tumor organization pH and the normal physiologic pH of a human body. The polymer and the micelle thereof are well-behaved carrier materials for the slow release of the medicines.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, biomaterials and polymer materials, and in particular relates to a degradable polymer and micelles thereof for accelerated drug release in tumor sites, and a preparation method of the polymers and micelles. Background technique [0002] With the development of science and technology, a series of anticancer drugs have been synthesized or isolated from nature. However, most anticancer drugs have serious side effects, which hinder the clinical application of drugs. In order to solve this problem, scientists use nanoparticles as drug carriers, such as nanomicelles to encapsulate drugs, improve the therapeutic effect of drugs, and reduce toxic and side effects. Among them, nanomicelles with a diameter of 20-200 nanometers can effectively enhance the penetration and retention (EPR effect) of particles in tumor tissues, thereby enhancing the drug efficacy. Nanoparticles with intell...

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): C08G65/48C08G63/91C08G63/664C08G69/44C08G69/40C08G69/10C08L71/08C08L67/04C08L77/04A61K47/34A61K9/00A61P35/00
Inventor 丁建东常广涛陆伟跃李翀
Owner FUDAN UNIV
Features
  • Generate Ideas
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com