Lipidosome-polymer hybrid nano particle and preparation method and application thereof

A hybrid nanoparticle and nanoparticle technology, applied in liposome delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of poor biocompatibility, etc., and achieve the effect of simple equipment, prolonging cycle time, and convenient and applicable operation process

Active Publication Date: 2014-07-02
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The polymer has good mechanical stability and strong drug loading capacity, but poor biocompatibility

Method used

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  • Lipidosome-polymer hybrid nano particle and preparation method and application thereof
  • Lipidosome-polymer hybrid nano particle and preparation method and application thereof
  • Lipidosome-polymer hybrid nano particle and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Prepare irinotecan as the hydrophobic drug model, 5-fluorouracil and oxaliplatin as the hydrophilic drug model, mPEG / PLA as the amphiphilic polymer model, lecithin and cholesterol as the liposome model and Liposome-polymer hybrid nanoparticles with a multilamellar structure loaded with three drugs.

[0050] (1) Dissolve 20 mg of polymer PLA-PEG in 1 mL of dichloromethane as the oil phase; add 250 μL of 2 mg / mL 5-fluorouracil aqueous solution;

[0051] (2) Use an ultrasonic cell disruptor (Ningbo Xinzhi Ultrasonic Cell Disruptor: SCIENTZ-IID) to act for 4 minutes at 4% power to form a uniform emulsion;

[0052] (3) Add 2 mL of 2% polyvinyl alcohol (PVA) into a round beaker, add the emulsion prepared in (2) while stirring, and slowly add 250 μL of dichloromethane dissolved in 2 mg / mL irinotecan ;

[0053] (4) After stirring for 3 minutes, take it out and use an ultrasonic cell disruptor to act for 5 minutes at 5% power;

[0054] (5) Add 10 mL of 0.6% PVA into a round b...

Embodiment 2

[0063] Preparation of nanoparticles loaded with irinotecan, 5-fluorouracil and oxaliplatin to obtain spherical nanoparticles with a particle size of about 161.63±21.76nm, the drug loading of 5-fluorouracil is 2%, and the encapsulation efficiency is 20% , the specific implementation is as follows:

[0064] (1) Dissolve 20 mg of polymer PLA-PEG in 1 mL of dichloromethane as the oil phase; add 250 μL of 8 mg / mL 5-fluorouracil aqueous solution;

[0065] (2) Utilize the ultrasonic cell breaker to act for 4 minutes under 4% power to form a uniform emulsion;

[0066] (3) Add 2 mL of 2% polyvinyl alcohol (PVA) into a round beaker, add the emulsion prepared in (2) while stirring, and slowly add 250 μL of dichloromethane dissolved with 10 mg / mL irinotecan;

[0067] (4) After stirring for 3 minutes, take it out and use an ultrasonic cell disruptor to act for 5 minutes at 5% power;

[0068] (5) Add 10 mL of 0.6% PVA into a round beaker, slowly add the emulsion prepared in (4) while stir...

Embodiment 3

[0074] Nanoparticles loaded with 5-fluorouracil and irinotecan were prepared to obtain spherical nanoparticles with a particle size of about 165.63±14.38nm, the drug loading was 12%, and the encapsulation rate of irinotecan was 96%. The implementation is as follows:

[0075] (1) Dissolve 20 mg of polymer PLGA-PEG in 1 mL of dichloromethane, and add 250 μL of 0.4 mg / mL 5-fluorouracil aqueous solution as the oil phase;

[0076] (2) Utilize the ultrasonic cell breaker to act for 4 minutes under 4% power to form a uniform emulsion;

[0077] (3) Add 2 mL of 2% polyvinyl alcohol (PVA) into a round beaker, add the emulsion prepared in (2) while stirring, and slowly add 250 μL of dichloromethane dissolved in 10 mg / mL irinotecan ;

[0078] (4) After stirring for 3 minutes, take it out and use an ultrasonic cell disruptor to act for 5 minutes at 5% power;

[0079] (5) Add 10 mL of 0.6% PVA into a round beaker, slowly add the emulsion prepared in (4) while stirring, and stir for 10 mi...

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Abstract

The invention relates to a lipidosome-polymer hybrid nano particle and a preparation method and an application thereof. The lipidosome-polymer hybrid nano particle comprises an amphiphilic polymer nano particle and a lipid bilayer coating the surface of the amphiphilic polymer nano particle as well as medicines embedded into the amphiphilic polymer nano particle and between the amphiphilic polymer nano particle and the lipid bilayer and having different water solubilities. The nano particle provided by the invention has a multi-layered structure to embed medicines with different water solubilities, thereby realizing a synergistic effect of different medicines. The particle is high in biocompatibility, can circulate in blood for a long time, has the targeted and sustained-release effects, improves the curative effect of the medicines and reduces the toxic and side effects of the medicines, and can be used as a carrier system of an anti-tumor medicine. The preparation method provided by the invention is simple in process, convenient in operating process, and can be produced in a small scale in a laboratory and also can be industrially produced in a large scale.

Description

technical field [0001] The invention relates to the field of pharmaceutical technology, in particular to a preparation method for forming liposome-polymer hybrid nanoparticles by assembling different water-soluble drugs and amphiphilic polymers and liposomes, and the prepared nanoparticles, and their use in Application in the preparation of antitumor drugs. Background technique [0002] In the 21st century, despite the rapid development of medical technology, cancer is still one of the major diseases that seriously threaten human health. Although the survival rate of cancer patients has improved with the improvement of medical level in the past few decades, the death rate of cancer is still high compared with the decline rate of death rate of other diseases (such as cardiovascular disease). In the past 20 years, one out of every 4-5 deaths in China died of cancer, ranking first among the causes of death. The latest statistics show that there are 2.2 million new cancer case...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/34A61P35/00
Inventor 聂广军李凤赵潇王海郝继辉
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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