Nano drug delivery system containing polymer and phospholipid and preparation method thereof

A nano-drug-loading and polymer technology, applied in the field of nano-medicine, can solve the problems of low targeting and limited drug loading rate, and achieve controllable biodegradation, simple and easy preparation method, and low toxicity of degradation products. Effect

Active Publication Date: 2013-04-17
珠海中科先进技术研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, traditional polymer nanocarriers or nanoliposome carriers generally have the problems of low targeting and limited drug loading rate (ratio of drug mass to carrier mass)

Method used

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  • Nano drug delivery system containing polymer and phospholipid and preparation method thereof
  • Nano drug delivery system containing polymer and phospholipid and preparation method thereof

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preparation example Construction

[0020] In addition, this embodiment also provides a method for preparing a nano drug-loading system containing polymers and phospholipids, including the following steps:

[0021] Step S110, preparing a polylactic acid-glycolic acid copolymer acetonitrile solution with a concentration range of 1-5 mg / mL and a drug methanol solution with a concentration range of 1-5 mg / mL, and mixing the drug methanol solution with the polylactic acid-glycolic acid copolymer acetonitrile solution According to the volume ratio of 5:100 to 20:100, the mixed solution containing the drug and the polylactic acid-glycolic acid copolymer is obtained.

[0022] Step S120, dissolving phospholipids and distearoylphosphatidylethanolamine-polyethylene glycol-folic acid linear polymers in a mixed solution of chloroform and methanol, then adding them to ethanol aqueous solution, and heating to 65°C to obtain phospholipids and linear polymers A mixture of polymers, wherein the concentration of phospholipids is ...

Embodiment 1

[0031] Dissolve an appropriate amount of docetaxel in methanol to obtain a docetaxel solution with a concentration of 2 mg / mL; dissolve an appropriate amount of PLGA in acetonitrile to obtain a PLGA solution with a concentration of 2 mg / mL; take an appropriate amount of soybean lecithin and DSPE-PEG- FoLate was dissolved in a mixture of chloroform and methanol to obtain soybean lecithin at a concentration of 1 mg / mL and DSPE-PEG-FoLate at a concentration of 25 mg / mL, wherein the volume ratio of chloroform to methanol was 9:1. Then 100 μL of docetaxel solution and 1 mL of PLGA acetonitrile solution were mixed ultrasonically to obtain a mixed solution containing docetaxel and PLGA.

[0032]Add 4.8 μL DSPE-PEG-FoLate solution and 180 μL soybean lecithin solution into 3 mL ethanol aqueous solution, heat to 65 °C and stir for 3 minutes to obtain a phospholipid mixture, wherein the mass fraction of ethanol in the ethanol aqueous solution is 4%.

[0033] Add 1.1 mL of the above-menti...

Embodiment 2

[0036] Dissolve an appropriate amount of docetaxel in methanol to obtain a docetaxel solution with a concentration of 2 mg / mL; dissolve an appropriate amount of PLGA in acetonitrile to obtain a PLGA solution with a concentration of 2 mg / mL; take an appropriate amount of soybean lecithin and DSPE-PEG- FoLate was dissolved in a mixture of chloroform and methanol to obtain soybean lecithin at a concentration of 1 mg / mL and DSPE-PEG-FoLate at a concentration of 25 mg / mL, wherein the volume ratio of chloroform to methanol was 9:1. Then take 50 μL of docetaxel solution and 1 mL of PLGA acetonitrile solution and ultrasonically mix to obtain a mixed solution containing docetaxel and PLGA.

[0037] Add 4.8 μL of DSPE-PEG-FoLate solution and 180 μL of soybean lecithin solution into 6 mL of ethanol aqueous solution, heat to 65 °C and stir for 3 minutes to obtain a phospholipid mixture, wherein the mass fraction of ethanol in the ethanol aqueous solution is 4%.

[0038] Add 1.05 mL of the...

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Abstract

The invention relates to a nano drug delivery system containing polymer and phospholipid. The system comprises polylactic-co-glycolic acid, phospholipid, drug and linear polymer of distearoyl phosphatidyl ethanolamine, polyethylene glycol and folic acid, wherein the drug is coated by the polylactic-co-glycolic acid to form a core; the phospholipid surrounds the surface of the polylactic-co-glycolic acid to form an intermediate layer; and the linear polymer of the distearoyl phosphatidyl ethanolamine, the polyethylene glycol and the folic acid uses the distearoyl phosphatidyl ethanolamine to interleave in the phospholipid intermediate layer to form an outer layer to provide a shell of the polyethylene glycol and a targeting ligand of the folic acid. The Nano drug delivery system containing polymer and phospholipid has comprehensive advantages of the polymer and a nano-liposome, has the advantages of good biocompatibility, controllable biodegradability and low toxicity of degradation products, capacities of easily realizing targeted controlled release and achieving surface functionalization, and the like. In addition, the invention further provides a preparation method of the nano drug delivery system containing the polymer and the phospholipids, which is simple and convenient to operate.

Description

technical field [0001] The invention relates to the field of nanomedicine, in particular to a nano drug-carrying system containing polymers and phospholipids and a preparation method thereof. Background technique [0002] Traditionally, a variety of delivery systems that can carry drugs have been developed. Among them, the two mainstream nanocarriers represented by polymer nanoparticles and nanoliposomes can efficiently encapsulate and transport drugs, and have become a research hotspot for scientists from all over the world. [0003] The two mainstream nanocarriers represented by polymer nanoparticles and nanoliposomes have many advantages and have solved many problems, such as the solubility of insoluble drugs and the sustained release of drugs. However, traditional polymer nanocarriers or nanoliposome carriers generally have the problems of low targeting and limited drug loading rate (ratio of drug mass to carrier mass). Contents of the invention [0004] Based on this...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/34A61K47/24A61K31/337A61P35/00
Inventor 蔡林涛郑翠芳郑明彬龚萍赵鹏飞
Owner 珠海中科先进技术研究院有限公司
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