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Polypeptide targeting placenta-like chondroitin sulfate A, targeted nano-particles and preparation method and application thereof

A chondroitin sulfate and nanoparticle technology, applied in the direction of inactive components of polymer compounds, can solve the problem of no receptors and delivery vehicles reported in the literature, and achieve good targeting, strong affinity, and improve the effect of treatment effect.

Active Publication Date: 2019-04-09
SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the specific receptor of pl-CSA is unknown, and there are no literature reports on receptors, delivery vehicles, etc. that can specifically bind to pl-CSA.

Method used

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  • Polypeptide targeting placenta-like chondroitin sulfate A, targeted nano-particles and preparation method and application thereof
  • Polypeptide targeting placenta-like chondroitin sulfate A, targeted nano-particles and preparation method and application thereof
  • Polypeptide targeting placenta-like chondroitin sulfate A, targeted nano-particles and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] A method for preparing placenta-like chondroitin sulfate A targeting nanoparticles coated with doxorubicin, comprising the following steps:

[0088] (1) Dissolve polylactic acid-glycolic acid copolymer (PLGA, the molecular weight is 15000, the copolymerization ratio of monomeric lactic acid and glycolic acid is 50:50) in acetonitrile to obtain an acetonitrile solution of PLGA with a concentration of 2 mg / mL;

[0089] (2) 90 μg of soybean lecithin, 210 μg of DSPE-PEG-COOH (the molecular weight of PEG is 2000), and 750 μg of doxorubicin were dissolved in 3 mL of 4% ethanol to obtain the first mixed solution;

[0090] (3) Add 1 mL of PLGA acetonitrile solution dropwise to 3 mL of the first mixed solution at a rate of 0.3 mL / min, and use an ultrasonic cell disruptor to perform ultrasonic treatment at a frequency of 20 KHz and a power of 130 W, and the ultrasonic time is 5 min ;

[0091] The ultrasonicated solution was subjected to ultrafiltration centrifugation in an ultra...

Embodiment 2

[0098] A preparation method of placenta-like chondroitin sulfate A targeted nanoparticles co-encapsulated doxorubicin and indocyanine green, the difference from Example 1 is that the first mixed solution contained in step (2) It is 750 μg of indocyanine green (ICG) and 750 μg of doxorubicin.

Embodiment 3

[0100] A preparation method of placenta-like chondroitin sulfate A targeting nanoparticles, comprising the following steps:

[0101] (1) Polycaprolactone (molecular weight is 10000) is dissolved in acetone, obtains polycaprolactone solution, and concentration is 1mg / mL;

[0102] (2) 40 μg of egg yolk lecithin, 100 μg of DSPE-PEG-NH 2 (The molecular weight of PEG is 3000), 250 μg of prodigiosin was dissolved in 3 mL of 4% methanol to obtain the first mixed solution;

[0103] (3) Add 1mL of polycaprolactone solution dropwise to 3mL of the first mixed solution at a rate of 0.2mL / min, and use an ultrasonic cell breaker to perform ultrasonic treatment at a frequency of 20KHz and a power of 80W. 6 minutes;

[0104] The ultrasonicated solution was subjected to ultrafiltration centrifugation in an ultrafiltration centrifuge tube with a molecular weight cut-off of 5kDa, and washed with water, and repeated 4 times, wherein the centrifugation speed was 3000rpm, and each centrifugation ...

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Abstract

The invention provides a nanoparticle targeting placenta-like chondroitin sulfate A. The nanoparticle comprise a hydrophobic core, a single lipid molecular layer coating the hydrophobic cores and a hydrophilic shell targeting the placenta-like chondroitin sulfate A. The hydrophobic core comprises a hydrophobic polymer, the compound of the hydrophilic shell is a polypeptide grafted amphipathic large molecular compound, the hydrophobic end of the amphipathic large molecular compound penetrates the single lipid molecular layer, the hydrophilic end of the amphipathic large molecular compound is connected to the polypeptide through an amido bond, and the polypeptide is exposed out of the single lipid molecular layer. The amino acid sequence of the polypeptide is selected from one or more of amino acid sequences: SEQ ID NO: 1 to SEQ ID NO: 3. The invention also provides a preparation method and application of the nanoparticle as well as the polypeptide for targeting placenta-like chondroitinsulfate A.

Description

technical field [0001] The invention belongs to the technical field of drug carriers, and in particular relates to a placenta-like chondroitin sulfate A targeting nanoparticle and a preparation method and application thereof. Background technique [0002] Cancer is a serious threat to human health. At present, cancer treatment is mainly based on surgery, chemotherapy and radiotherapy, but most of the chemotherapy drugs are non-selective, widely distributed in the body, and have large toxic side effects on normal tissues and organs at therapeutic doses. Designing and constructing a drug-loading system that can specifically recognize cancer cells while reducing the side effects of chemotherapy drugs plays a vital role in the treatment of cancer. [0003] Recent research on nanotechnology-based targeted delivery systems has brought new opportunities for cancer therapy. It can maximize the delivery of therapeutic drugs to target organs, while having little impact on non-target ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42
CPCA61K47/42
Inventor 范秀军张保珍郑明彬程国钢李丹赵鹏飞蔡林涛张键
Owner SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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