Preparation method for nanoparticles with small particle size and nanoparticle medicine carrier

A nanoparticle and drug technology, which is applied in the preparation of small-sized nanoparticles and nanoparticle drug carriers, can solve the problems of low biosafety, inability to use tumor growth and recurrence, and poor biocompatibility of nano-anticancer drugs. Achieve the effects of simple preparation method, wide application and strong tumor penetration

Inactive Publication Date: 2014-01-22
SHENZHEN INST OF ADVANCED TECH
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Problems solved by technology

[0003] However, conventional nano-anticancer drugs often have the problem of low biological safety, and due to the large particle size (usually greater than 100nm) and poor biocompatibility, they cannot be effectively enriched in dense tumors, so the curative effect is minimal
Cannot be used in in vivo experiments or inhibit the growth and recurrence of such tumors

Method used

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  • Preparation method for nanoparticles with small particle size and nanoparticle medicine carrier
  • Preparation method for nanoparticles with small particle size and nanoparticle medicine carrier

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preparation example Construction

[0019] Specifically, the preparation method of the present invention mainly includes four steps: preparing a solution, forming a phospholipid film, self-assembling the nano-precipitate, and collecting by ultrafiltration. It should be understood that although these steps are described in this order below, the specific order of these steps is not limited thereto, for example, it is not necessary to prepare all the solutions first, and it is also possible to prepare only the phospholipid film formation and nanoprecipitation self-assembly steps to be used in this step. solution.

[0020] Solution preparation steps: Dissolve PLGA in acetonitrile, although the concentration has little effect on the preparation of nanoparticles, usually, the concentration of 1-10mg / ml can be used; dissolve lecithin and DSPE-PEG in ethanol respectively In the aqueous solution, a lecithin solution and a DSPE-PEG solution are formed. Because the solubility of phospholipids in water is low, aqueous ethan...

Embodiment 1

[0031] Preparation solution: acetonitrile solution of PLGA, the concentration is 2.5mg / ml; solution of lecithin and DSPE-PEG in 4% ethanol aqueous solution, the concentration is 1mg / ml.

[0032] Phospholipid film formation: add 800 μl of lecithin solution and DSPE-PEG solution to 2ml of 4% ethanol solution, wherein the mass ratio of lecithin: DSPE-PEG is 1:1, and spin dry after ultrasonic mixing to form a uniform phospholipid film.

[0033] Nano-precipitation self-assembly: Mix 3.2ml of PLGA solution into 4ml of 4% ethanol aqueous solution, shake and mix, add dropwise to the film-forming container, heat to 65°C and keep stirring during the dropwise addition. The mass ratio of PLGA to total phospholipids is 5:1. After completion of the dropwise addition, keep stirring in a water bath at 65° C. for 2 hours.

[0034] Ultrafiltration collection: Collect by centrifugation with a 10kDa ultrafiltration tube to obtain nanoparticles with small particle size.

[0035] The average par...

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Abstract

The invention relates to the nano-medicine field, and concretely discloses a preparation method for nanoparticles with small particle size and an obtained nanoparticle medicine carrier. The method comprises steps: preparation of solutions, PLGA is dissolved in acetonitrile, and phosphatidylcholine bilayer and DSPE-PEG are dissolved in aqueous solutions of ethanol respectively; phosphatide film formation: the phosphatidylcholine bilayer solution and the DSPE-PEG solution are mixed, subjected to ultrasonic treatment and mixed uniformly, the solvents are removed, and phosphatide films are formed; nano-precipitation self assembly: the PLGA solution is added in the film-formed container, after mixing, the mixture is kept at the temperature of 60-65 DEG C with heat preservation, thus the PLGA and phosphatide are subjected to nano-precipitation self assembly for nanoparticles; and ultrafiltration collection: the nanoparticles are obtained after ultrafiltration centrifugation and collection. The preparation method is simple. The surfaces of the obtained nanoparticles with small particle size are charged negatively, and the nanoparticles have strong tumour penetrability and high cycling stability in organism. The nanoparticle can load various hydrophobic, hydrophilic and amphipathic medicines s as a medicine carrier and can be used widely.

Description

technical field [0001] The invention relates to the field of nano-medicine, in particular to a method for preparing nanoparticles with small diameters, and a nano-particle drug carrier prepared thereby. Background technique [0002] Dense tumors of pancreatic cancer, bladder cancer and other cancers have always been a difficult problem in cancer treatment. In the research of nano-anticancer drugs, nano-carriers are used to carry anti-tumor drugs to prepare nano-drugs, and the metabolic characteristics of the carrier itself are used to deliver the drugs to the tumor site, so as to achieve efficient treatment of tumors. Nanocarriers made of polymers, liposomes or lipopolymers are widely used in clinical research due to their advantages of good biocompatibility, efficient entrapment and delivery of drugs and genes. [0003] However, most conventional nano-anticancer drugs have the problem of low biological safety, and due to the large particle size (usually greater than 100nm)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/34A61K47/24B82Y5/00
Inventor 蔡林涛赵鹏飞郑明彬龚萍岳彩霞罗震宇郑翠芳
Owner SHENZHEN INST OF ADVANCED TECH
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