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Biodegradable zwitterionic polycarbonate and application thereof

A zwitterion and polycarbonate technology, applied in the direction of drug combinations, organic active ingredients, non-central analgesics, etc., can solve the problems that hinder the long-term application of PEG derivatives, and achieve controllable molecular weight, simple preparation, and reduced The effect of the immune response

Active Publication Date: 2020-07-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, these deficiencies hinder the long-term application of PEG derivatives texture to varying degrees.

Method used

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  • Biodegradable zwitterionic polycarbonate and application thereof
  • Biodegradable zwitterionic polycarbonate and application thereof
  • Biodegradable zwitterionic polycarbonate and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] (1) Polymerization of acrylate cyclic carbonate monomer AC (8k), the process is as follows:

[0049]

[0050] Under nitrogen protection, compound 1 (0.5g, 2.5mmol), isopropanol (0.0038g, 0.063mmol) as initiator, anhydrous dichloromethane (6mL) as solvent, bis(bistrimethylsilyl)amine zinc As a catalyst, it was carried out at 40°C and reacted for 12h. After the reaction, the polymer 1, ie, PAC, was purified by precipitation with glacial ether, and the yield was 80%. NMR characterization diagram see figure 1 shown.

[0051] The ring-opening polymerization of polymer 1 (PAC) was carried out at 40°C with isopropanol (Mn 60) as the initiator, anhydrous dichloromethane as the solvent, and zinc bis(bistrimethylsilyl)amine as the catalyst. . The reaction was fed under nitrogen protection. After the reaction was completed, glacial acetic acid was added to terminate the reaction, and it was purified by precipitation with glacial ether. The polymer composition and GPC char...

Embodiment 2

[0065] (1) Preparation of PAC(TCB)(8k) zwitterionic polymer micelles by solvent dialysis:

[0066] First, dissolve the zwitterionic polymer PAC (TCB) in a mixed solvent of N,N-dimethylformamide and methanol, put it into a dialysis bag (MWCO3500), and dialyze in a deionized water medium for 10 hours, during which the dialysis is replaced regularly medium. The average particle diameter of the micelles recorded by the dynamic light scattering instrument is 189nm, and the particle size distribution index is 0.11, such as Figure 5 shown.

[0067] (2) Changes in particle size of PAC(TCB)(8k) zwitterionic polymer micelles containing 10%wt bovine serum albumin:

[0068] Take 1mL of prepared polymer micelles with a concentration of 1mg / mL, add 10%wt bovine serum albumin to it, place it at room temperature, and measure the change of its particle size with a dynamic light scattering instrument at a specified time point.

[0069] Such as Figure 6 , under the condition of adding 10%w...

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Abstract

The invention discloses biodegradable zwitterionic polycarbonate and an application thereof. The method includes using a compound or a polymer containing a hydroxyl functional group mainly as an initiator for ring opening polymerization of a cyclic carbonate monomer, and obtaining functional polymers; reacting the acrylamide zwitterionic compound with a disulfydryl compound to synthesize a sulfhydrylated zwitterionic compound; finally, carrying out Michael addition reaction on the functional polymer and a sulfhydrylated zwitterionic compound to obtain the biodegradable zwitterionic polycarbonate; the biodegradable zwitterionic polycarbonate is simple and easy to synthesize, the polymerization molecular weight of the biodegradable zwitterionic polycarbonate is controllable, and the biodegradable zwitterionic polycarbonate can be used for self-assembling nano-drugs, can be used for treating various diseases such as tumors and inflammations, and can also be used for antibacterial stent coatings. Compared with previous researches, the biodegradable polymer is simple to prepare and high in protein adsorption resistance, reduces immunoreaction, and is expected to have a wide applicationprospect in the field of biomedicine.

Description

technical field [0001] The invention relates to a biodegradable zwitterionic polycarbonate with anti-nonspecific protein adsorption, a preparation method and application thereof, and belongs to the technical field of polymer materials. Background technique [0002] The adsorption of protein on the surface of materials is a very common phenomenon, and it has also brought many adverse effects to people. For example, non-specific adsorption of proteins will cause biomedical materials to cause adsorption, spreading, proliferation, and even death of cells on their surfaces; reduce the sensitivity of biosensors, etc. Proteins have a strong adsorption on hydrophobic surfaces, and hydrophobic surfaces will destroy the protein structure and denature and inactivate it. Therefore, constructing hydrophilic substances on the surface of materials can resist the adsorption of non-specific proteins. In the past few decades, people have been working on the use of polyethylene glycol (PEG) ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G64/42C08G64/30C08G64/18A61K47/34A61K9/107A61K31/337A61P35/00A61P29/00
CPCA61K9/1075A61K31/337A61K47/34A61P29/00A61P35/00C08G64/183C08G64/30C08G64/42
Inventor 陈维陈莹黄德春钟伊南
Owner CHINA PHARM UNIV
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