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Interface-cross-linked temperature-sensitive polymer vesicle and use thereof

A technology of interfacial cross-linking and polymers, which is applied in the direction of medical preparations and pharmaceutical formulations of non-active ingredients, can solve the problems of premature drug release, low drug bioavailability, and low efficiency, and achieve high-efficiency entrapment and overcoming The effect of low drug entrapment efficiency

Inactive Publication Date: 2009-09-02
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Diblock, triblock, graft and hyperbranched copolymers have all been found to form vesicles, but most preparations use organic solvents
These vesicles generally have the problems of low yield and low encapsulation efficiency of hydrophilic drugs, and the bioavailability of drugs is also low; there are few studies on targeted vesicles, and the release of drugs to lesion sites such as cancer cell areas Low efficiency, which limits the medical application of polymersome biogenesis
[0005] Designing a polymersome system responsive to signals (pH, temperature, etc.) , 18, 2905) can solve the above problems, but there are few reports on such systems
At the same time, the self-assembled structure is unstable, and it dissociates after being injected into the body after a large amount of dilution, resulting in premature release of the drug. In terms of cross-linked polymer vesicles, especially the research on cross-linked systems with stimuli-responsive cross-linking agents has not been reported.

Method used

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  • Interface-cross-linked temperature-sensitive polymer vesicle and use thereof
  • Interface-cross-linked temperature-sensitive polymer vesicle and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1, RAFT polymerization to obtain triblock copolymer PEG-PAA-PNIPAM

[0040] Under argon protection, the initiator AIBN (0.62mg, 3.77μmol), the macromolecular RAFT reagent PEG-DMP (0.10g, 19μmol), acrylic monomer AA (0.0328g, 0.456mmol) and 5.0mL of dioxane Add it to a 10mL Schlenk vacuum-sealed bottle, put the bottle in an oil bath at 70℃ after 30 minutes of argon gas, stir and react for 24 hours, take a sample to determine the conversion rate of AA monomer, and add the second order to the rest NiPAAM (0.4260g, 3.8mmol) and some AIBN (0.2mg dissolved in 0.2mL dioxane) were allowed to react at 70°C for another 24 hours. After the reaction, it was precipitated in cold ether and dried under vacuum for 48 hours. , The triblock copolymer is obtained, and the yield is 70 to 86%. NMR results show that its structure is PEG 113 -PAA 24 -PNIPAM 211 PNIPAM accounts for about 78% of the molecular weight of the entire molecule, and its LCST in PBS is 38.5°C.

Embodiment 2

[0041] Example 2: RAFT polymerization to obtain block copolymer DEX-PMA-NIPAM

[0042] Under argon protection, the initiator AIBN (0.62mg, 3.77μmol), the macromolecular RAFT reagent DEX-CPDPA (0.127g, 20μmol), the methacrylic acid monomer MA (9.46mg, 110μmol) and 5.0mL of dioxane The ring was added to a 10mL Schlenk vacuum-sealed bottle. After argon for 30 minutes, the bottle was placed in an oil bath at 75°C. After stirring and reacting for 24 hours, a sample was taken to determine the conversion rate of the MA monomer, and the second was added to the rest Monomer NIPAAM (0.7230g, 6.4mmol) and some AIBN (0.2mg dissolved in 0.2mL dioxane) were allowed to react at 75°C for another 24 hours. After the reaction, it was precipitated in cold ether and then dried in vacuum 48 Within hours, a triblock copolymer is obtained with a yield of 70-75%. NMR results show that its structure is DEX37-PMA 5 -PNIPAM 356 , PNIPAM accounts for about 86% of the molecular weight of the entire molecule, ...

Embodiment 3

[0043] Example 3: RAFT polymerization to obtain block copolymer PEG 113 -PHA 10 -NIPAM 90

[0044] Under argon protection, the initiator AIBN (0.62mg, 3.77μmol), the macromolecular RAFT reagent PEG-CPDPA (0.10g, 19μmol), 5-hexenoic acid monomer HA (22.8mg, 200μmol) and 4.0mL of two Add oxane into a 10mL Schlenk vacuum-sealed bottle. After 30 minutes of argon, place the bottle in an oil bath at 75°C. After stirring and reacting for 24 hours, take a sample to determine the conversion rate of HA monomer, and add to the rest The second monomer NIPAM (0.1930g, 1.70mmol) and some AIBN (0.2mg dissolved in 0.2mL dioxane) were allowed to react at 70°C for another 24 hours. After the reaction, it was precipitated in cold ether and vacuum After drying for 48 hours, a triblock copolymer is obtained with a yield of 70-75%. NMR results show that its structure is PEG 113 -PHA 10 -NIPAM 90 PNIPAM accounts for about 61% of the molecular weight of the entire molecule, and its LCST in PBS is 38°C. ...

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Abstract

The invention discloses an interface-cross-linked temperature-sensitive polymer vesicle and a method for preparing the same. The interface-cross-linked temperature-sensitive polymer vesicle is formed by a block copolymer which at least comprises a hydrophilic block, a cross-lined interstrand block and a temperature sensitive block, wherein the hydrophilic block forms the membrane shell of the polymer vesicle, the temperature sensitive block forms the membrane nuclear of the polymer vesicle, and the cross-lined interstrand block forms the interface of the polymer vesicle to cross-link the interface of the polymer vesicle to stabilize the structure of the vesicle, and thus the interface-cross-linked temperature-sensitive polymer vesicle is formed; as the vesicle is formed in an aqueous solution system and the interface of vesicle is cross-linked, the small molecule drug, macromolecular drug and probe molecule entrapment efficiency of the polymer vesicle, the circulation stability in vivo blood and the efficiency of endocytosis by tumor cells are improved; and as a result, the bioavailability of drugs is improved and the polymer vesicle can be expelled out of the body conveniently.

Description

Technical field [0001] The invention relates to a drug carrier and a preparation method thereof, in particular to a drug release system of crosslinked temperature-sensitive polymer vesicles. Background technique [0002] Polymersomes formed by self-assembly of amphiphilic polymers in water using intermolecular interactions have high membrane stability, adjustable properties (such as thickness, elasticity, toughness, and degradability), and large content. It can encapsulate hydrophilic and hydrophobic substances, and has great application potential in the controlled release of drugs. Diblock, triblock copolymers, graft copolymers and hyperbranched copolymers have all been found to form vesicles, but most preparations use organic solvents. [0003] Being able to prepare vesicles directly in water will have more advantages in the packaging and controlled release of water-soluble drugs. For example, the Discher group studied the biocompatibility of polyethylene glycol-polybutene (PEO...

Claims

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Application Information

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IPC IPC(8): C08J3/00A61K47/32
Inventor 孟凤华徐海飞钟志远
Owner SUZHOU UNIV
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