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PEG-PLGA nanoparticle carrying recombinant human vascular endothelial inhibitor and preparation method thereof

A PEG-PLGA90.2%-99%, vascular endothelial technology, applied in the direction of drug combination, pharmaceutical formula, medical preparations of non-active ingredients, etc., can solve the problem of protein drugs with large molecular weight, difficult to wrap nanoparticle carriers, and carrier materials Large molecular weight and other problems, to achieve the effect of high drug loading, prolonged residence time, and good sustained release effect

Inactive Publication Date: 2010-11-24
SHANDONG UNIV QILU HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In spite of this, there are still many microspheres that are currently researched on loading active proteins, and there are studies on endostat (recombinant human endostatin) slow-release microspheres, such as patents CN101536984A, CN101428142A; this type of slow-release microspheres can only be subcutaneous. Or intraperitoneal injection, not for intravenous injection
The particle size of microspheres is much larger than that of nanoparticles, and intravenous injection can easily lead to embolism, with serious consequences; and the drugs released by microspheres need to diffuse through tissues and pass through the vascular endothelial barrier before they can enter the blood circulation and reach the tumor growth site. less, can not play a good role in the treatment of drugs
Since Endostar (recombinant human vascular endostatin) is a new protein drug that has just been launched on the market, and the protein drug has a large molecular weight (22KDa), it is difficult to wrap it in a nanoparticle carrier, so the research on Endostar PEG-PLGA nanoparticles is very few
Patent CN1608675A discloses a drug-loaded nanoparticle of polymer material. This kind of nanoparticle uses PELGE and PELGA triblock copolymer as the carrier. The carrier material has a large molecular weight. The content involved in the package is mainly genes, involving small molecule polypeptide drugs Thymopentin, no technical publicity on macromolecular protein chemotherapeutic drugs; and the preparation of nano-sized particles with a wide particle size distribution and low drug loading

Method used

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  • PEG-PLGA nanoparticle carrying recombinant human vascular endothelial inhibitor and preparation method thereof
  • PEG-PLGA nanoparticle carrying recombinant human vascular endothelial inhibitor and preparation method thereof
  • PEG-PLGA nanoparticle carrying recombinant human vascular endothelial inhibitor and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Accurately weigh 5 mg of PEG-PLGA, add to 1 ml of dichloromethane and dissolve to form the organic phase. Take 50ul of endostar aqueous solution with a concentration of 10mg / ml as the water phase. Add the Endostar solution to the organic phase and vortex mix at 2800rpm, and form colostrum after homogenization. Weigh polyvinyl alcohol (PVA) and add it into double-distilled water to make it fully dissolved, adjust the concentration to 0.1%, and form the external water phase. The volume ratio of the inner water phase to the outer water phase is 1:4. Immediately add the prepared colostrum into the external water phase, shear at 25000rpm for 60s at high speed, pour the obtained emulsion into 10ml of 0.1% polyvinyl alcohol solution, stir and evaporate the organic solvent for 4 to 5 hours with magnetic stirring, and completely volatilize the dichloromethane , to obtain a colloidal solution of PEG-PLGA nanoparticles. The average particle size is 109nm, and the encapsulation ...

Embodiment 2

[0032] Accurately weigh 10 mg of PEG-PLGA, add to 1 ml of dichloromethane and dissolve to form the organic phase. Take 50ul of endostar aqueous solution with a concentration of 10mg / ml as the water phase. Add the Endostar solution to the organic phase and vortex mix at 2800rpm, and form colostrum after homogenization. Weigh polyvinyl alcohol (PVA) and add it into double-distilled water to make it fully dissolved, and adjust its concentration to 0.25% to form the external water phase. The volume ratio of the inner water phase to the outer water phase is 1:4. Immediately add the prepared colostrum into the external water phase, shear at 20,000rpm for 60s at high speed, pour the obtained emulsion into 10ml of 0.25% polyvinyl alcohol solution, and evaporate the organic solvent with magnetic stirring for 4-5 hours to completely volatilize the dichloromethane , to obtain a colloidal solution of PEG-PLGA nanoparticles. The average particle size is 198nm, and the encapsulation effi...

Embodiment 3

[0034]Accurately weigh 18 mg of PEG-PLGA, add it to 1 ml of dichloromethane and dissolve it to form the organic phase. Take 200ul of endostar aqueous solution with a concentration of 10mg / ml as the water phase. Add the Endostar solution to the organic phase and vortex mix at 2000rpm, and form colostrum after homogenization. Weigh polyvinyl alcohol (PVA) and add it into double-distilled water to make it fully dissolved, and adjust its concentration to 0.25% to form the external water phase. The volume ratio of the inner water phase to the outer water phase is 1:4. Immediately add the prepared colostrum into the external water phase, shear at 20,000rpm for 60s at high speed, pour the obtained emulsion into 10ml of 0.25% polyvinyl alcohol solution, and evaporate the organic solvent with magnetic stirring for 4-5 hours to completely volatilize the dichloromethane , to obtain a colloidal solution of PEG-PLGA nanoparticles. The average particle diameter is 253nm, and the encapsul...

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Abstract

The invention discloses a PEG-PLGA nanoparticle carrying a recombinant human vascular endothelial inhibitor and a preparation method thereof. The nanoparticle comprises the following components in percentage by weight: 1 to 9.8 percent of recombinant human vascular endothelial inhibitor and 90.2 to 99 percent of PEG-PLGA; and the particle size of the nanoparticle is 50 to 500 nm and the polydispersity index is 0.28 to 1. The PEG-PLGA nanoparticle carrying the recombinant human vascular endothelial inhibitor has the advantages of relatively smooth surface of the nanoparticle, no adhesion, controllable nanoparticle size, small particle size, narrow particle size range, convenient intravenous injection and good sustained release effect; moreover, a carrier material modified by PEG has good medicament encapsulating effect, and the hydrophilicity of the carrier material can prevent the carrier material from being captured by a reticuloendothelial system and make the carrier material long-circulated.

Description

technical field [0001] The invention relates to a drug-carrying nanoparticle with a polymer material and a preparation method thereof. Background technique [0002] In the 1970s, Professor Folkman of Harvard University in the United States proposed that when solid tumors and their metastases grow to more than 1-2 mm, the purpose of inhibiting and treating tumors can be achieved by blocking tumor angiogenesis. Based on this, endostatin can specifically inhibit the proliferation and angiogenesis of endothelial cells, make the tumor dormant, and thus inhibit tumor growth. It can restore the proliferation and apoptosis of tumor vascular endothelial cells to a balanced state without cytotoxicity, has a broad anti-tumor spectrum, does not produce drug resistance, and has a clear therapeutic target, which has a good clinical application prospect. However, when Endostar (recombinant human endostatin rh-Endo) is administered in combination with the NP chemotherapy regimen, daily adm...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K38/17A61K47/34A61P35/00A61K47/10
Inventor 胡三元陈伟杰闫治波张光永刘崇忠
Owner SHANDONG UNIV QILU HOSPITAL
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