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

Polyphosphoester prodrug simultaneously bonding camptothecin and adriamycin amycin and preparing method and application thereof

A technology of polyphosphate and camptothecin, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., achieves the advantages of simple product purification technology, high yield, and improved blood circulation time. Effect

Active Publication Date: 2018-07-17
SUZHOU UNIV
View PDF8 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the prior art, although there have been some reports on the prodrugs of camptothecin and doxorubicin and their use in the synergistic treatment of tumors, the two drugs are simultaneously bonded to the polymer as a synergistic therapeutic polymer prodrug There are not many reports, so it is necessary to develop a new system for two drugs to be bonded to the polymer at the same time; the polymer used should have good biocompatibility and biodegradability, good stimulation of the tumor microenvironment Responsiveness, and considering that multi-agent therapy can modulate different signaling pathways in diseased cells, maximize therapeutic effect (i.e. achieve synergy) and potentially overcome resistance mechanisms

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
  • Polyphosphoester prodrug simultaneously bonding camptothecin and adriamycin amycin and preparing method and application thereof
  • Polyphosphoester prodrug simultaneously bonding camptothecin and adriamycin amycin and preparing method and application thereof
  • Polyphosphoester prodrug simultaneously bonding camptothecin and adriamycin amycin and preparing method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1: Random copolymer CPT- ss -PBYP 30 - b -PEEP 80 Synthesis of (1:20:50)

[0076] Camptothecin dithiol compounds (CPT- ss -OH) as the initiator and stannous octoate as the catalyst, through the "one-pot method" continuous ring-opening polymerization of BYP and EOP to obtain CPT- ss -PBYP- b -PEEP random copolymer, the preparation process is carried out under anhydrous and oxygen-free conditions. The syringes and needles used in the experiment were dried in an oven at 120 °C for 5 h, and were taken out and cooled in a desiccator before the reaction. Dry the clean ampoule bottle (pre-installed with a magnetic stirring rotor) in a 120 °C oven for about 5 hours, take it out and connect it to a vacuum pump with a latex tube, fill it with high-purity argon while vacuuming, and repeat the operation three times to remove the bottle. moisture and oxygen. Add the camptothecin dithiol compound (CPT- ss-OH) (0.185 g, 0.35 mmol), BYP (1.251 g, 7.1 mmol), EOP (2.645...

Embodiment 2

[0077] Example 2: Random copolymer CPT- ss -PBYP 28 - b -PEEP 33 Synthesis

[0078] Camptothecin dithiol compounds (CPT- ss -OH) as the initiator and stannous octoate as the catalyst, through the "one-pot method" continuous ring-opening polymerization of BYP and EOP to obtain CPT- ss -PBYP- b -PEEP random copolymer. The preparation process is carried out under anhydrous and oxygen-free conditions. The syringes and needles used in the experiment were dried in an oven at 120 °C for 5 h, and were taken out and cooled in a desiccator before the reaction. Dry the clean ampoule bottle (pre-installed with a magnetic stirring rotor) in a 120 °C oven for about 5 hours, take it out and connect it to a vacuum pump with a latex tube, fill it with high-purity argon while vacuuming, and repeat the operation three times to remove the bottle. Moisture and oxygen; in the ampoule, add the camptothecin dithiol compound (CPT- ss -OH) (0.189 g, 0.35 mmol), BYP (1.249 g, 7.1 mmol), EOP (1...

Embodiment 3

[0079] Example 3: Random copolymer CPT- ss -PBYP 68 - b -PEEP 53 Synthesis

[0080] Camptothecin dithiol compounds (CPT- ss -OH) as the initiator and stannous octoate as the catalyst, through the "one-pot method" continuous ring-opening polymerization of BYP and EOP to obtain CPT- ss -PBYP- b -PEEP random copolymer. The preparation process was carried out under anhydrous and oxygen-free conditions. The syringes and needles used in the experiment were dried in an oven at 120 °C for 5 h, and were taken out and cooled in a desiccator before the reaction. Dry the clean ampoule bottle (pre-installed with a magnetic stirring rotor) in a 120 °C oven for about 5 hours, take it out and connect it to a vacuum pump with a latex tube, fill it with high-purity argon while vacuuming, and repeat the operation three times to remove the bottle. moisture and oxygen. Add the camptothecin dithiol compound (CPT- ss -OH) (0.189 g, 0.35 mmol), BYP (1.873 g, 10.5 mmol), EOP (2.623 g, 17.5 m...

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
Login to View More

Abstract

The invention discloses a polyphosphoester prodrug simultaneously bonding camptothecin and adriamycin amycin and a preparing method and application thereof. The prodrug (CPT-ss-PBYP-hyd-DOX)-b-PEEP can be self-assembled in a water solution to form a prodrug nanometer particle; the hydrophobic drug camptothecin and adriamycin amycin and a propargyl-group-containing polyphosphoester (PBYP) chain segment form a kernel of the nanometer particle; a hydrophilic ethyl polyphosphoester (PEEP) chain segment forms a shell of the nanometer particle, and the shell of the nanometer particle has the effectof stabilizing the nanometer particle; disulfide-bond oxidation-reduction rupture can occur under the glutathione condition, hydrazone bond rupture occurs in the acid environment, micelle is damaged,and therefore a hydrophobic anti-cancer drug gathered inside the nanometer particle is rapidly released. The polyphosphoester prodrug simultaneously bonding the camptothecin and the adriamycin amycinhas the 'acid / reduction' sensibility, the biocompatibility and the biodegradability, the hydrophilia of the anti-cancer drug is improved, and therefore the polyphosphoester prodrug can be used for thesensibility-exciting anti-cancer prodrug.

Description

technical field [0001] The invention belongs to the field of biomedical polymer materials, and in particular relates to a polyphosphate prodrug bonded with camptothecin and doxorubicin at the same time, and a preparation method and application thereof. Background technique [0002] Combination therapy of multiple drugs can improve the treatment effect of cancer, because this treatment method can effectively overcome the multidrug resistance of tumor cells. Camptothecin (CPT) and doxorubicin (DOX) are a common group of combination drugs, both of which are topoisomerase inhibitors. Camptothecin and doxorubicin act on topoisomerase Ⅰ and Ⅱ respectively. The combination of the two drugs can effectively promote cell apoptosis and hinder cell proliferation. In an appropriate ratio, it can also achieve synergistic treatment effect. However, the disadvantages of these two drugs are poor water solubility, unstable blood, and large toxic and side effects on normal tissues, so they ar...

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 Applications(China)
IPC IPC(8): A61K47/69A61K47/59A61K31/704A61P35/00C08G79/04A61K31/4745
CPCA61K31/4745A61K31/704C08G79/04A61K47/6907A61K47/59A61P35/00A61K2300/00
Inventor 倪沛红董淑祥何金林张明祖孙月刘洁
Owner SUZHOU 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