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A preparation method of nanoparticles with pH sensitivity and anticancer activity

A technology of anti-cancer activity and nanoparticles, applied in the direction of organic active ingredients, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as large market demand, complex human blood, and single source , to achieve the effect of good anti-malignant tumor activity, strong operability, and strong anti-malignant tumor effect

Active Publication Date: 2021-05-28
QILU UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] The existing proteins used as drug carriers include albumin, collagen, whey protein, etc. From the perspective of biocompatibility, degradability and cytotoxicity, commonly used albumin includes human serum albumin (HSA) And bovine serum albumin (BSA), but HSA can only be obtained from healthy human blood, the market demand is large, the supply is in short supply, the cost of a single source is high, and human blood is more complicated, there are potential threats of various pathogenic microorganisms, So we choose BSA with similar structure, cheap price and high purification degree to replace HSA

Method used

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  • A preparation method of nanoparticles with pH sensitivity and anticancer activity
  • A preparation method of nanoparticles with pH sensitivity and anticancer activity
  • A preparation method of nanoparticles with pH sensitivity and anticancer activity

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] A nanoparticle consisting of the following components in parts by mass:

[0042]

[0043]

[0044] The preparation method of nanoparticles with pH sensitivity and anticancer activity of the present invention comprises the following steps:

[0045] (1) Preparation of cinnamaldehyde derivatives

[0046] Take 0.5 parts of anthranilic hydrazide in the three-necked flask 1, add 47 parts of absolute ethanol to fully dissolve the anthranilic hydrazide, raise the temperature to 70°C, add 0.6 parts of cinnamaldehyde, 2 drops of glacial acetic acid, and continue the reaction for 8 hours. After the reaction, the anhydrous ethanol was removed by rotary evaporation at 45°C, and the solid precipitate was washed with an appropriate amount of dichloromethane, then separated by suction filtration, and repeated three times, and a yellow powder was obtained after drying. The obtained powder is carried out correlative test, obtains infrared spectrogram (attachment figure 1 ), H NMR...

Embodiment 2

[0052] A nanoparticle consisting of the following components in parts by mass:

[0053]

[0054] The preparation method of nanoparticles with pH sensitivity and anticancer activity of the present invention comprises the following steps:

[0055] (1) Preparation of cinnamaldehyde derivatives

[0056] Take 2 parts of anthranilic hydrazide in the three-necked flask 1, add 50 parts of absolute ethanol to fully dissolve the anthranilic hydrazide, raise the temperature to 70°C, add 1 part of cinnamaldehyde, 2 drops of glacial acetic acid, and continue the reaction for 8 hours. After the reaction, remove absolute ethanol by rotary evaporation at 45°C, wash the solid precipitate with an appropriate amount of dichloromethane, then separate by suction filtration, repeat three times, and obtain a yellow powder after drying;

[0057] (2) Preparation of BSA-CAE NPs

[0058] Take 0.3 parts of BSA in the three-necked flask 2, then add 25 parts of PBS buffer solution, place the three-nec...

Embodiment 3

[0062] A nanoparticle consisting of the following components in parts by mass:

[0063]

[0064] The preparation method of nanoparticles with pH sensitivity and anticancer activity of the present invention comprises the following steps:

[0065] (1) Preparation of cinnamaldehyde derivatives

[0066] Take 3 parts of anthranilic hydrazide in the three-necked flask 1, add 72 parts of absolute ethanol to fully dissolve the anthranilic hydrazide, raise the temperature to 70°C, add 4 parts of cinnamaldehyde, 2 drops of glacial acetic acid, and continue the reaction for 8 hours. After the reaction, remove absolute ethanol by rotary evaporation at 45°C, wash the solid precipitate with an appropriate amount of dichloromethane, then separate by suction filtration, repeat three times, and obtain a yellow powder after drying;

[0067] (2) Preparation of BSA-CAE NPs

[0068] Take 0.3 parts of BSA in the three-necked flask 2, then add 23 parts of PBS buffer solution, place the three-ne...

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Abstract

The present invention relates to a preparation method of nanoparticles with pH sensitivity and anticancer activity. The purpose of the present invention is to provide a kind of high biocompatibility, biodegradable, stable system, and improved drug efficacy in view of the deficiencies of the prior art. The preparation method of the medicine, namely the preparation method of bovine serum albumin-cinnamaldehyde derivative nanoparticles. We chose to use bovine serum albumin (BSA) to covalently graft cinnamaldehyde derivatives to prepare nanoparticles. The prepared nanoparticles are drug carriers with both pH responsiveness and antitumor activity. It can further combine the antitumor drug doxorubicin through physical combination, and through the compounding effect of synergistic administration, the dose of doxorubicin can be reduced while the corresponding lethality rate of cancer cells can be achieved, so as to achieve the purpose of anticancer. And the whole preparation process is green, pollution-free, and has strong operability.

Description

technical field [0001] The invention relates to the technical fields of polymer chemistry, biochemistry, pharmaceutical preparations, etc., and particularly provides a preparation method of nanoparticles with pH sensitivity and anticancer activity. Background technique [0002] The existing proteins used as drug carriers include albumin, collagen, whey protein, etc. From the perspective of biocompatibility, degradability and cytotoxicity, commonly used albumin includes human serum albumin (HSA) And bovine serum albumin (BSA), but HSA can only be obtained from healthy human blood, the market demand is large, the supply is in short supply, the cost of a single source is high, and human blood is more complicated, there are potential threats of various pathogenic microorganisms, So we choose BSA with similar structure, cheap price and high purification degree to replace HSA. In addition to these advantages, the homology between BSA and HSA is as high as 76%, which effectively r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/64A61K47/69A61K31/11A61K31/704A61P35/00
CPCA61K31/11A61K31/704A61K47/643A61K47/6931A61P35/00A61K2300/00
Inventor 秦大伟常书华
Owner QILU UNIV OF TECH
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