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 rare reports, premature release of drugs, and low efficiency, and achieve the goal of overcoming low loading efficiency, The effect of efficient package loading

Inactive Publication Date: 2011-07-20
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
  • Interface-cross-linked temperature-sensitive polymer vesicle and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment one, RAFT polymerization obtains triblock copolymer PEG-PAA-PNIPAM

[0042] Under the protection of argon, the initiator AIBN (0.62 mg, 3.77 μmol), the macromolecular RAFT reagent PEG-DMP (0.10 g, 19 μmol), the acrylic acid monomer AA (0.0328 g, 0.456 mmol) and 5.0 mL of dioxane Add it into a 10mL Schlenk vacuum-sealed bottle, put the bottle in an oil bath at 70°C after passing argon for 30 minutes, stir and react for 24 hours, take a sample to measure the conversion rate of AA monomer, and add the second monomer to the rest NIPAAM (0.4260g, 3.8mmol) and some AIBN (0.2mg dissolved in 0.2mL dioxane) were reacted at 70°C for another 24 hours. After the reaction, it was precipitated in cold ether, and then vacuum-dried for 48 hours. , to obtain a three-block copolymer with a yield of 70-86%. NMR results show that its structure is PEG 113 -PAA 24 -PNIPAM 211 , wherein PNIPAM accounts for about 78% of the molecular weight of the entire molecule, and its LCST i...

Embodiment 2

[0043] Embodiment two, RAFT polymerization obtains block copolymer DEX-PMA-NIPAM

[0044] Under the protection of argon, the initiator AIBN (0.62 mg, 3.77 μmol), the macromolecular RAFT reagent DEX-CPDPA (0.127 g, 20 μmol), the methacrylic acid monomer MA (9.46 mg, 110 μmol) and 5.0 mL of dioxane Put the ring into a 10mL Schlenk vacuum-sealed bottle, put the bottle in an oil bath at 75°C after passing argon for 30 minutes, stir and react for 24 hours, take a sample to measure the conversion rate of MA monomer, and add the second Monomer NIPAAM (0.7230g, 6.4mmol) and some AIBN (0.2mg dissolved in 0.2mL dioxane) were reacted at 75°C for another 24 hours. After the reaction, it was precipitated in cold ether, and then vacuum-dried for 48 Hours, a tri-block copolymer was obtained with a yield of 70-75%. NMR results show that its structure is DEX37-PMA 5 -PNIPAM 356 , wherein PNIPAM accounts for about 86% of the molecular weight of the entire molecule, and its LCST in PBS is 33°...

Embodiment 3

[0045] Embodiment three, RAFT polymerization obtains block copolymer PEG 113 -PHA 10 -NIPAM 90

[0046] Under the protection of argon, the initiator AIBN (0.62 mg, 3.77 μmol), the macromolecular RAFT reagent PEG-CPDPA (0.10 g, 19 μmol), the 5-hexenoic acid monomer HA (22.8 mg, 200 μmol) and 4.0 mL of di Add oxyhexane into a 10mL Schlenk vacuum-sealed bottle, put the bottle in an oil bath at 75°C after argon gas flow for 30 minutes, stir and react for 24 hours, take a sample to measure the conversion rate of HA monomer, and add 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 was completed, it was precipitated in cold ether, and vacuum After drying for 48 hours, a tri-block copolymer was obtained with a yield of 70-75%. NMR results show that its structure is PEG 113 -PHA 10 -NIPAM 90 , wherein PNIPAM accounts for about 61% of the molecular weight of the ent...

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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 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 formedby 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 polyby 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 intermer 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 solutface 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 vivoion 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.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 a cross-linked temperature-sensitive polymer vesicle. Background technique [0002] Polymersomes are self-assembled in water by amphiphilic polymers using intermolecular interactions. The membrane has high stability, adjustable properties (such as thickness, elasticity, toughness and degradability), large internal capacity, It can wrap hydrophilic and hydrophobic substances, and has great application potential in the controlled release of drugs. Diblock, triblock, graft and hyperbranched copolymers have all been found to form vesicles, but most are prepared using organic solvents. [0003] The ability to prepare vesicles directly in water will have more advantages in the encapsulation and controlled release of water-soluble drugs. For example, the Discher group studied the biocompatibility of polyethylene glycol-polybutene (PEO-PEE) and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08J3/00A61K47/32
Inventor 孟凤华徐海飞钟志远
Owner SUZHOU UNIV
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