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Placenta-targeted nanoparticle for medical abortion and its preparation method and application

A nanoparticle, targeting technology, applied in the field of medicine

Active Publication Date: 2021-07-27
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, there is still no nanoparticle highly targeted to the placenta

Method used

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  • Placenta-targeted nanoparticle for medical abortion and its preparation method and application
  • Placenta-targeted nanoparticle for medical abortion and its preparation method and application
  • Placenta-targeted nanoparticle for medical abortion and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] A method for preparing placenta-targeted nanoparticles, comprising the following steps:

[0074] (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;

[0075] (2) 90 μg of soybean lecithin, 210 μg of DSPE-PEG-COOH (the molecular weight of PEG is 2000), and 315 μg of methotrexate are dissolved in 3 mL of 4% ethanol aqueous solution to obtain the first mixed solution ;

[0076] (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 ;

[0077] The ultrasonicated solution was subjected to ultrafiltration centrifugation in an ultrafiltration centrifuge tube with a...

Embodiment 2

[0083] A method for preparing placenta-targeted nanoparticles, comprising the following steps:

[0084] (1) Polycaprolactone (molecular weight is 10000) is dissolved in acetone, obtains polycaprolactone solution, and concentration is 1mg / mL;

[0085] (2) 40 μg of egg yolk lecithin, 100 μg of DSPE-PEG-NH 2 (The molecular weight of PEG is 3000), the mifepristone of 50 μ g and the misoprostol of 50 μ g are dissolved in the methanol aqueous solution that is 4% volume fraction in 3mL, obtains the first mixed solution;

[0086] (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;

[0087] 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 centrifug...

Embodiment 3

[0091] A method for preparing placenta-targeted nanoparticles, comprising the following steps:

[0092] (1) Polylactic acid (molecular weight is 21800) is dissolved in DMF, obtains the polylactic acid solution that concentration is 4mg / mL;

[0093] (2) 800 μg of cephalin, 1600 μg of DSPE-PEG-NH2 (PEG molecular weight is 2000), and 2250 μg of letrozole were dissolved in 3 mL of acetone to obtain the first mixed solution;

[0094] (3) Add 1mL of polylactic acid solution dropwise to 3mL of the first mixed solution at a rate of 0.4mL / min, and use an ultrasonic cell disruptor to perform ultrasonic treatment at a frequency of 20KHz and a power of 160W, and the ultrasonic time is 4min ;

[0095] The ultrasonicated solution was subjected to ultrafiltration and centrifugation in an ultrafiltration centrifuge tube with a molecular weight cut-off of 10kDa, and washed with water, and repeated 4 times, wherein the centrifugation speed was 5000rpm, and each centrifugation was 3min, and the...

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Abstract

The invention provides a placenta-targeted nanoparticle, which can be used for medical abortion, which comprises a hydrophobic inner core, a monolayer lipid molecular layer wrapping the hydrophobic inner core and a hydrophilic outer shell. The hydrophobic inner core includes a hydrophobic polymer and Its loaded target delivery includes abortion drugs; the composition of the hydrophilic shell is an amphiphilic macromolecular compound grafted with a polypeptide targeting placenta-like chondroitin sulfate A, and the hydrophobic end of the amphiphilic macromolecular compound Interspersed in the monolayer lipid molecular layer, the hydrophilic end of the amphiphilic macromolecular compound is connected to the polypeptide through an amide bond, and the polypeptide is exposed outside the monolayer lipid molecular layer, wherein the amino acid sequence of the polypeptide is selected from SEQ ID NO: One or more of the amino acid sequences shown in 1-SEQ ID NO:3. The invention also provides a preparation method of the placenta-targeted nanoparticle and its application in the preparation of mammalian abortion medicine.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a placenta-targeted nanoparticle for medical abortion and its preparation method and application. Background technique [0002] The World Health Organization estimates that there are 75 million unintended pregnancies worldwide each year, and about 26 million to 53 million cases end in induced abortion. Under the premise of such a high induced abortion rate, safer and more effective induced abortion technology needs to be developed urgently. The existing induced abortion techniques are mainly divided into two categories: medical abortion and negative pressure aspiration surgical abortion. However, both technologies have major disadvantages. Although the success rate of surgical abortion is high and the time is short, the operation pain is high and it is accompanied by surgical complications; although medical abortion has the advantages of simple method and less pai...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/00C07K7/08A61K47/69A61K47/64A61K45/00A61K47/24A61K49/04A61K31/567A61K31/519A61K31/5575A61K31/4196
CPCA61K31/4196A61K31/519A61K31/5575A61K31/567A61K45/00A61K47/24A61K49/0002A61K49/0056A61K49/0093A61K49/0404A61K49/0438A61K2300/00
Inventor 范秀军谭仑波张保珍程国钢汪宝蓓肖天霞张键
Owner SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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