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A kind of amphiphilic graft copolymer and its application

A technology of graft copolymers and hydrophilic polymers, which is applied in the field of pharmaceutical preparations, can solve the problems of lack of reversibility of intelligent responsive micelles, achieve improved stability and targeting efficiency, strengthen deep penetration, and improve safety Effect

Active Publication Date: 2022-07-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the problem of the lack of reversibility of the existing smart responsive micelles, the purpose of the present invention is to provide an amphiphilic graft copolymer which can self-assemble in a neutral or alkaline environment Form a micelle structure. As the pH of the environment changes, the micelle disintegrates in an acidic environment and exists as a stretched chain structure. When the disintegrated micelle monomer re-enters a neutral or alkaline environment, it can self-assemble again form micellar structure

Method used

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  • A kind of amphiphilic graft copolymer and its application
  • A kind of amphiphilic graft copolymer and its application
  • A kind of amphiphilic graft copolymer and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] 1. Synthesis of γ-PGA-NH-PHis

[0050] (1) γ-PGA-NH 2 Synthesis: Weigh 100 mg of γ-PGA and add 2 mL of ultrapure water, stir to dissolve, add 345.06 mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC.HCl) , 207.18 mg N-hydroxysuccinimide (NHS), activated at room temperature for 30 min. 270.45 mg of ethylenediamine (EDA) was weighed into the activated γ-PGA solution, and the reaction was stirred at room temperature for 12 h. After the reaction, the reaction solution was taken for dialysis with a dialysis bag with a molecular weight cut-off of 3.5KDa, and freeze-dried for 48 hours to obtain a white loose solid, namely γ-PGA-EDA.

[0051] (2) Synthesis of γ-PGA-NH-PHis: Weigh 67.62 mg of PHis(16), 11.50 mg of EDC.HCl, and 6.9 mg of NHS, dissolved in 2 mL of dimethyl sulfoxide (DMSO), and activated at room temperature for 30 min. 41.43 mg of γ-PGA-EDA was weighed, dissolved in 300 μL of ultrapure water, diluted to 2 mL with DMSO, added to the activated...

Embodiment 2

[0088] Synthesis of PVA-PHis: Weigh 20 mg of PHis(16), 6.82 mg of EDC.HCl, and 4.34 mg of DMAP, dissolved in 5 mL of 0.1 M MES buffer (pH=5.8), and activated at room temperature for 30 min. 10 mg of PVA was weighed and dissolved in 2 mL of MES buffer, added to the activated PHis solution, and stirred at room temperature for 24 h. The reaction solution was dialyzed and freeze-dried to obtain a white solid, namely PVA-PHis.

[0089] Preparation of micelles: Dissolve an appropriate amount of PVA-PHis in a pH 7.4 PBS solution to form micelles by self-assembly.

[0090] The hydrated particle size of the micelle solution obtained in Example 5 was measured by dynamic light scattering technique, the pH of the solution was adjusted to 6.5, and after standing for half an hour, the hydrated particle size was measured again, and the pH of the solution was re-adjusted to 7.4, and the solution was allowed to stand. Half an hour later, the hydrated particle size was measured again. The res...

Embodiment 3

[0095] Synthesis of PEI-PHis: Weigh 20 mg of PHis(16), 6.82 mg of EDC.HCl, and 4.08 mg of NHS, dissolved in 5 mL of 0.1 M MES buffer (pH=5.8), and activated at room temperature for 30 min. 15 mg of PEI was weighed and dissolved in 2 mL of MES buffer, added to the activated PHis solution, and stirred for 24 h at room temperature. The reaction solution was dialyzed and freeze-dried to obtain a white solid, namely PEI-PHis.

[0096] Preparation of micelles: Dissolve an appropriate amount of PEI-PHis in a pH 7.4 PBS solution to form micelles by self-assembly.

[0097] The hydrated particle size of the obtained micelle solution was measured by dynamic light scattering technique, the pH of the solution was adjusted to 6.5, and after standing for half an hour, the hydrated particle size was measured again, and the pH of the solution was re-adjusted to 7.4, and after standing for half an hour , and measure its hydrated particle size again. The results of hydrated particle size under...

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Abstract

The invention discloses an amphiphilic graft copolymer and an application thereof, belonging to the technical field of pharmaceutical preparations. The amphiphilic graft copolymer includes a hydrophilic polymer whose backbone is modified with an amphiphilic short chain containing an imidazole group. Since the amphiphilic graft copolymer of the present invention has an amphiphilic short chain containing an imidazole group, it can undergo reversible morphological changes in response to pH changes, and self-assemble to form a micellar structure in a neutral or alkaline environment; In an acidic environment, the disintegration of micelles exists in the form of a stretched chain structure. When re-entering a neutral or alkaline environment after disintegration, the micelles will self-assemble again to form a micellar structure.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an amphiphilic graft copolymer and an application thereof. Background technique [0002] In recent years, polymer micelles, as a new nano-drug delivery system, have attracted more and more attention due to their unique properties, such as good passive targeting, excellent drug-carrying capacity, and stable structure, and have become an important part of pharmacy. It is a research hotspot in the field. At present, many nanomicelle preparations have been listed at home and abroad, which have great clinical application value. [0003] At present, polymer micelles mainly use amphiphilic block or graft copolymers as carriers, and the hydrophilic components mainly include polyethylene glycol, polyvinyl alcohol, poly(N-vinyl-2-pyrrolidone), polysaccharide, Hyaluronic acid, hydrophilic polyamino acids, etc., whose hydrophilic properties can increase the s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G81/00C08G81/02A61K47/34A61K9/107A61K47/64A61K47/69A61K33/243A61K31/337A61P35/00A61P29/00A61P7/02A61K49/00
CPCC08G81/00C08G81/024A61K47/34A61K9/1075A61K47/64A61K47/6907A61K33/243A61K31/337A61P35/00A61P29/00A61P7/02A61K49/00A61K2300/00
Inventor 孙春萌涂家生陈大力伊宸辰嵇梦
Owner CHINA PHARM UNIV
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