Preparation method and use of degradable polymer nano-microcapsules

A technology for degrading polymers and nano-microcapsules. It is applied in the direction of microcapsules, nanocapsules, and medical preparations of non-active ingredients. It can solve the problems of adverse therapeutic effects and low drug loading, and achieve fast release speed and preparation The effect of simple process and uniform molecular weight distribution

Inactive Publication Date: 2014-06-04
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the reported ultrasound contrast agents are usually too low in drug loading, which is not conducive to their therapeutic effect, so the preparation of high drug loading ultrasound contrast agents is also a key issue

Method used

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  • Preparation method and use of degradable polymer nano-microcapsules
  • Preparation method and use of degradable polymer nano-microcapsules
  • Preparation method and use of degradable polymer nano-microcapsules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Preparation of PMAA microcapsules with a shell thickness of 25 nm and a crosslinking degree of 40%

[0028] (1) Synthesis of uncrosslinked PMAA nanospheres: 2 g of MAA, 0.04 g of AIBN, and 80 mL of acetonitrile were added to a 100 mL single-necked bottle and heated to 100 o C, reflux reaction for 2 h. The solvent and unreacted monomers were removed by centrifugation, washed three times with acetonitrile, and dried in a vacuum oven for 24 h.

[0029] (2) Synthesis of PMAA nanospheres with core-shell structure: Take 100 mg PMAA nanospheres, 200 mg MAA monomer, 80 mg BACy cross-linking agent, 10 mg AIBN initiator, 40 mL acetonitrile, heat to 100 o C, reflux reaction for 2 h. Unreacted monomers were removed by centrifugation, washed three times with acetonitrile, and dried in a vacuum oven for 24 h.

[0030] (3) Dissolve the prepared PMAA nanospheres with core-shell structure in 50 mL ethanol solution and heat to 50 oC , etch for 3 h. Centrifuged, washed...

Embodiment 2

[0031] Example 2: Preparation of PAA microcapsules with a shell thickness of 15 nm and a crosslinking degree of 30%

[0032] (1) Synthesis of uncrosslinked PAA nanospheres: AA 1 g, AMBN 0.02 g, and 80 mL of acetonitrile were added to a 100 mL single-necked bottle and heated to 100 o C, reflux reaction for 2 h. The solvent and unreacted monomers were removed by centrifugation, washed three times with acetonitrile, and dried in a vacuum oven for 24 h.

[0033] (2) Synthesis of PAA nanospheres with core-shell structure: take 50 mg of PAA nanospheres, 200 mg of AA monomer, 60 mg of BACy cross-linking agent, 10 mg of AMBN initiator, 40 mL of acetonitrile, and heat to 120 o C, reflux reaction for 1 h. Unreacted monomers were removed by centrifugation, washed three times with acetonitrile, and dried in a vacuum oven for 24 h.

[0034] (3) Dissolve the prepared PAA nanospheres with core-shell structure in 50 mL water and heat to 50 oC , etch for 3 h. Centrifuged, washed 3 time...

Embodiment 3

[0035] Example 3: Preparation of PHEMA microcapsules with a shell thickness of 10 nm and a crosslinking degree of 20%

[0036] (1) Synthesis of uncrosslinked PHEMA nanospheres: HEMA 0.5 g, AMBN 0.02 g, and 50 mL of acetonitrile were added to a 100 mL single-necked bottle and heated to 90 o C, reflux reaction for 2 h. The solvent and unreacted monomers were removed by centrifugation, washed three times with acetonitrile, and dried in a vacuum oven for 24 h.

[0037] (2) Synthesis of PHEMA nanospheres with core-shell structure: Take 50 mg PHEMA nanospheres, 200 mg HEMA monomer, 40 mg BACy crosslinker, 10 mg AIBN initiator, 40 mL acetonitrile, heat to 90 o C, reflux reaction for 1 h. Unreacted monomers were removed by centrifugation, washed three times with acetonitrile, and dried in a vacuum oven for 24 h.

[0038] (3) Dissolve the prepared PHEMA nanospheres with core-shell structure in 50 mL of water and ethanol, and heat to 50 oC , etch for 3 h. Centrifuged, washed 3 t...

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Abstract

The invention relates to a preparation method and a use of degradable polymer nano-microcapsules. The preparation method comprises the following steps of carrying out backflow deposition on an acrylic acid monomer to produce uncross-linked polymer nano-microspheres, carrying out backflow deposition to coat a disulfide bond cross-linked polymer shell layer on the surface of the uncross-linked polymer nano-microsphere by disulfide bond-containing N,N'-bis(acryloyl)cystamine as a cross-linking agent, transferring the prepared core-shell composite microspheres into ethanol or water, and carrying out uncross-linked polymer core etching to obtain the degradable polymer nano-microcapsules having monodispersity. The preparation method can be carried out fast, has simple aftertreatment processes, is free of an etching process adopting strong acid or strong alkali and is safe and efficient. After freeze-drying treatment, the degradable polymer nano-microcapsule can carry doxorubicin as a cancer-resistant drug and the cavity of the degradable polymer nano-microcapsule is further filled with perfluorohexane having ultrasonic response so that the degradable polymer nano-microcapsule is effectively used as an ultrasonic contrast agent and a drug carrier. The ultrasonic contrast agent can be fast decomposed to form very low molecular-weight linear molecules (Mn<5000) in the presence of glutathione or dithiothreitol as a reducing agent.

Description

technical field [0001] The invention relates to a method for preparing novel degradable polymer nano-microcapsules and its application in ultrasonic contrast agents and drug carriers, belonging to the technical fields of new materials and biomedicine. Background technique [0002] Ultrasound imaging (US) technology is one of the most widely used imaging technologies in the world. Because low-intensity ultrasound causes little damage to human tissue, it has the advantages of safety, wide application, real-time, repeatable inspection, strong ability to identify soft tissues, high flexibility and low price, making ultrasound image diagnosis the first choice for medical image diagnosis. . However, compared with CT imaging and magnetic resonance imaging, the sensitivity and resolution of ultrasound imaging are very low. When the two soft tissue interfaces have similar acoustic impedance, the reflected echoes between the two are very similar, so only ultrasound diagnosis is used....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/22A61K47/32A61K9/51A61K31/704A61P35/00C08F120/06C08F120/28C08F120/54C08J3/24
Inventor 杨朋汪长春
Owner FUDAN UNIV
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