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

Paclitaxel bonded amphipathic aliphatic polyester-b-polyphosphate high polymer and preparation thereof

An aliphatic polyester and polyphosphate technology, which is applied in the direction of artificially synthesized active ingredients of polymeric materials, drug combinations, anti-tumor drugs, etc., can solve the problem of no anti-cancer drugs, etc.

Inactive Publication Date: 2012-06-20
SUZHOU UNIV
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] According to investigations, there has been no literature report on the preparation of anticancer drugs by directly bonding paclitaxel to polyε-caprolactone and polyphosphate amphiphilic block copolymers by ring-opening polymerization.

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
  • Paclitaxel bonded amphipathic aliphatic polyester-b-polyphosphate high polymer and preparation thereof
  • Paclitaxel bonded amphipathic aliphatic polyester-b-polyphosphate high polymer and preparation thereof
  • Paclitaxel bonded amphipathic aliphatic polyester-b-polyphosphate high polymer and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Example 1: Preparation of a polymer drug bonded by paclitaxel-polyε-caprolactone

[0066] Put the vial, glass syringe, needle and glass stopper with the stir bar in an oven at 120°C for 12 hours to dry, then take out the syringe and needle and put it in a desiccator to cool, plug the vial with a ground glass stopper and connect it Use an oil pump to cool to room temperature on the double-row tube, then fill with high-purity argon, and vent three times, and finally fill with argon, add white paclitaxel powder (0.20g, 0.23mmol) and Stannous octoate (0.047g, 0.12mmol) viscous liquid. Exhaust air twice, use a dry syringe to extract the solvent o-dichlorobenzene after argon exchange, add it to the branch bottle, stir to dissolve until the system is clear and transparent. Then use a dry syringe to add ε-caprolactone monomer (1.33 g, 0.012 mol), and the molar ratio of the amount to the initiator paclitaxel is 40-60:1. Put the reaction flask into the set 90-110°C oil bath, and r...

Embodiment 2

[0067] Example 2: Preparation of paclitaxel-polyε-caprolactone-polyphosphate bonded polymer drug (PTX-PCL-b-PEEP)

[0068] Place the vial, glass syringe, needle and ground glass stopper with the stir bar in an oven at 120°C for 12 hours to dry, remove the syringe and needle into a desiccator to cool, and stopper the vial bottle with the ground glass stopper Then connect it to the double-row pipe and use an oil pump to cool to room temperature, then fill with high-purity argon, and pump for three times, and finally fill with argon, add the number average molecular weight of about 4800g / mmol paclitaxel under the condition of argon Bonded polyε-caprolactone (PTX-PCL 35 ) Macromolecular initiator (0.58g, 0.12mmol) and stannous octoate (0.024g, 0.06mmol) viscous liquid. Exhaust air twice, use a dry syringe to extract tetrahydrofuran and add the solvent tetrahydrofuran to the branch vial, stir to dissolve until the system is clear and transparent. Then use a syringe to add phosphate m...

Embodiment 3

[0069] Example 3: Preparation of polymer micelles containing anticancer drugs by film forming method

[0070] Take 5mg sample PTX-PCL in a round bottom flask 35 -b-PEEP 16 Stir in 5 mL of tetrahydrofuran to fully dissolve, and then completely remove the tetrahydrofuran by rotary evaporation, then add 5 mL of phosphate buffer solution with a pH of 7.4, and stir overnight. Its morphology and micelle size were observed by transmission electron microscope, see Figure 5 .

[0071] The above PTX-PCL 35 -b-PEEP 16 It self-assembles in phosphate buffer solution to form micelles with hydrophobic drugs and lipophilic aliphatic polyester as the core and water-soluble polyphosphate as the shell. On the one hand, it can improve the strong hydrophobicity of the paclitaxel drug, thereby avoiding the rejection reaction in the process of drug delivery in the body; on the other hand, through the degradation of polyester, slow release of the drug, avoiding the sharp increase in drug concentration to...

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 field of medicament control release, and in particular relates to a paclitaxel bonded amphipathic aliphatic polyester-b-polyphosphate high polymer. The high polymer comprises a polyphosphate chain segment, an aliphatic polyester chain segment and a paclitaxel group, wherein the two ends of the aliphatic polyester chain segment are respectively connected with the paclitaxel group and the polyphosphate chain segment by virtue of ester bonds; the aliphatic polyester chain segment is selected from a poly(epsilon-caprolactone) chain segment or a polyactic acid segment. The high polymer can perform self-assembly in a phosphoric acid buffer solution PBS to form a hydrophobic medicament and a micelle in which lipophilic aliphatic polyester is used as a core and water-soluble polyphosphate is used as a shell. Through the preparation, on one hand, the strong hydrophobicity of a paclitaxel medicament is improved so as to avoid the rejection reaction of the medicament in the in vivo transportation process, and on the other hand, the medicament is slowly released through degradation of polyester so as to avoid the harmfulness of sharp increase of medicament concentration on other normal cells of tissue organs, thereby reaching the effect that an anti-tumor medicament is released controllably.

Description

Technical field [0001] The invention belongs to the field of controlled drug release, and relates to a polymer drug in which taxol, a hydrophobic drug for treating tumors, is bonded to a biocompatible and biodegradable amphiphilic aliphatic polyester-b-polyphosphate block copolymer And its synthesis method. Background technique [0002] Paclitaxel (Taxol, trade name) is a tricyclic diterpene substance extracted from Taxus plants, which has anti-tumor effects. Since it was approved by the U.S. Food and Drug Administration (FDA) for the treatment of advanced ovarian cancer in 1992, studies have gradually found that it has a high curative effect on breast, ovarian and lung cancer. Because paclitaxel is composed of a large ring structure and numerous hydrophobic groups, its solubility in water is very poor, making it difficult to prepare an injection. In order to improve its water solubility, reduce the excretion of P-glycoprotein, and enhance the anti-cancer ability of colon cance...

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): C08G79/04C08G63/08A61K31/80A61P35/00
Inventor 倪沛红张国艺张明祖
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