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Lipidosome-polymer drug-loaded nanoparticle and preparation method and application thereof

A drug-loaded nanometer and polymer technology, applied in liposome delivery, pharmaceutical formulations, active ingredients of heavy metal compounds, etc., can solve the problem of low tumor tissue specific recognition, improve antitumor effect, and enhance tumor targeting. sexual effect

Active Publication Date: 2016-12-07
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although the liposome-polymer hybrid nanoparticle of the invention has a long circulation time in the blood, can improve the curative effect of the drug, reduce toxic and side effects, etc., but the phospholipid bilayer coated by the outermost layer is specific for tumor tissue. The sex recognition effect is low, and its targeting only depends on the nano-effect of nano-materials

Method used

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  • Lipidosome-polymer drug-loaded nanoparticle and preparation method and application thereof
  • Lipidosome-polymer drug-loaded nanoparticle and preparation method and application thereof
  • Lipidosome-polymer drug-loaded nanoparticle and preparation method and application thereof

Examples

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Embodiment 1

[0072] In this example, liposome-polymer drug-loaded nanoparticles were prepared by the following method, which specifically included the following steps:

[0073] (1) Dissolve 20 mg of amphiphilic cationic polymer PEI-PLGA in 1 mL of dichloromethane, add 200 μL of water to the organic phase, and use an ultrasonic cell disruptor to sonicate at 35% power for 5 minutes to form colostrum;

[0074] (2) Adding 2 mL of 2% polyvinyl alcohol (PVA) aqueous solution to the colostrum obtained in step (1), and adding 200 μL of doxorubicin in dichloromethane (containing 2 mg of doxorubicin) dropwise, Use an ultrasonic cell breaker to ultrasonicate for 5 minutes at 40% power to form double emulsions;

[0075] (3) under stirring, add the double emulsion obtained in step (2) into 10 mL of PVA aqueous solution with a concentration of 0.6%, continue stirring for 3 min, and remove the organic solvent with a rotary evaporator to obtain a nanoparticle suspension;

[0076] (4) Mix and stir the nanop...

Embodiment 2

[0081] In this example, liposome-polymer drug-loaded nanoparticles were prepared by the following method, which specifically included the following steps:

[0082] (1) Dissolve 10 mg of amphiphilic cationic polymer PEI-PLGA in 1 mL of dichloromethane, add 100 μL of water to the organic phase, and use an ultrasonic cell disruptor to sonicate for 3 minutes at 35% power to form colostrum;

[0083] (2) Adding 5 mL of concentration to the colostrum obtained in step (1) is 3% polyvinyl alcohol (PVA) aqueous solution, and add dropwise the dichloromethane solution of 400 μ L of doxorubicin (containing 2 mg of doxorubicin), Using an ultrasonic cell disruptor to sonicate for 8 minutes at 40% power to form double emulsions;

[0084] (3) under stirring, add the double emulsion obtained in step (2) into 8 mL of 1% PVA aqueous solution, continue stirring for 5 min, and remove the organic solvent with a rotary evaporator to obtain a nanoparticle suspension;

[0085] (4) Mix and stir the nan...

Embodiment 3

[0090] In this example, liposome-polymer drug-loaded nanoparticles were prepared by the following method, which specifically included the following steps:

[0091] (1) Dissolve 40 mg of amphiphilic cationic polymer PEI-PLGA in 1 mL of dichloromethane, add 250 μL of water to the organic phase, add 100 μL of an aqueous solution of doxorubicin hydrochloride (containing 2 mg of doxorubicin hydrochloride ), using an ultrasonic cell disruptor to sonicate for 8 minutes at 35% power to form colostrum;

[0092] (2) Add 2 mL of 1% polyvinyl alcohol (PVA) aqueous solution to the colostrum obtained in step (1), and add 200 μL of paclitaxel in dichloromethane (containing 2 mg of paclitaxel) dropwise. Use ultrasound at 40% power for 3 minutes to form double emulsion;

[0093] (3) under stirring, add the double emulsion obtained in step (2) into 15 mL of 0.8% PVA aqueous solution, continue stirring for 10 min, and remove the organic solvent with a rotary evaporator to obtain a nanoparticle ...

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Abstract

The invention provides a lipidosome-polymer drug-loaded nanoparticle and a preparation method and application thereof. The lipidosome-polymer drug-loaded nanoparticle comprises a three-layer structure, wherein the innermost layer is the drug-loaded nanoparticles formed by taking an amphiphilic cationic polymer as a carrier-coated chemotherapeutic drug; the intermediate layer is a platelet inhibitor layer adsorbed onto the surface of the drug-loaded nanoparticles; and the outermost layer is a lipid bilayer connected with tumor microenvironment responsiveness polypeptides. The lipidosome-polymer drug-loaded nanoparticle disclosed by the invention is capable of specifically targeting tumor tissues, has tumor microenvironment responsiveness, and can achieve the effects of improving tumor vascular permeability without influencing functions of blood vessels at normal tissue or cell parts, enhancing permeability and retention of the drug-loaded nanoparticles to tumor cells, enhancing the EPR effect, improving enrichment of the drug-loaded nanoparticles at tumor location and realizing high tumor killing efficiency.

Description

technical field [0001] The invention belongs to the technical field of nanomedicine, and relates to a liposome-polymer drug-loaded nanoparticle, a preparation method and application thereof. Background technique [0002] The main methods of clinical cancer treatment are surgical treatment, radiotherapy, chemotherapy and some other adjuvant treatments. According to recent data, no more than 30% of cancer patients have the opportunity to undergo surgical treatment. Therefore, for most cancer patients Chemotherapy is said to be the main treatment. Due to the severe side effects brought to patients during radiotherapy and chemotherapy, the search for new tumor treatment methods has become the primary task of scientific researchers. With the rapid development of nanomedicine, nanomedicine has shown unique advantages in tumor treatment due to its unique small size effect. It can be enriched in a large number of tumor sites, kill tumor cells efficiently, and greatly reduce the dos...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K9/127A61K47/42A61K45/06A61K9/50A61P35/00A61P7/02A61K31/4365A61K31/282A61K31/337A61K31/704A61K39/395
CPCA61K9/5073A61K31/282A61K31/337A61K31/4365A61K31/704A61K39/395A61K45/06A61K2300/00
Inventor 聂广军张银龙李素萍赵颖季天骄赵潇
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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