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Nanocarrier medicine, as well as preparation method and application of nanocarrier medicine

A technology of nano-carriers and drugs, applied in the field of nano-carrier drugs and their preparation, to achieve guaranteed effects, significant therapeutic effects, and improved killing effects

Active Publication Date: 2018-05-01
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

So far, there are no effective drugs approved by the US Food and Drug Administration (FDA) for the treatment of TNBC

Method used

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  • Nanocarrier medicine, as well as preparation method and application of nanocarrier medicine
  • Nanocarrier medicine, as well as preparation method and application of nanocarrier medicine
  • Nanocarrier medicine, as well as preparation method and application of nanocarrier medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] In this example, the nano-carrier drug uses polylactic acid-glycolic acid (PLGA) as a carrier, loaded with NVP-BEZ235 and chlorin E6 (Ce6), and uses lecithin and distearoylphosphatidylethanolamine - Polyethylene glycol (DSPE-PEG) for PEGylation of the carrier surface.

[0057] The preparation method is as follows:

[0058] (1) Dissolve 0.5mg NVP-BEZ235 and 0.2mg Ce6 in 300μL DMSO to obtain a drug solution;

[0059] (2) 15 mg of polylactic acid-glycolic acid was dissolved in 700 μL of acetonitrile to obtain a carrier solution;

[0060] (3) Mix the drug solution obtained in step (1) with the carrier solution obtained in step (2), and ultrasonicate for 2 minutes to form an oil phase solution;

[0061] (4) 3 mg of lecithin and 3 mg of distearoylphosphatidylethanolamine-polyethylene glycol were dissolved in 5 mL of deionized water to obtain an aqueous phase solution;

[0062] (5) Add the oil phase solution obtained in step (3) to the water phase solution obtained in step ...

Embodiment 2

[0067] In this example, the nano-carrier drug uses polylactic acid-glycolic acid (PLGA) as a carrier, loaded with NVP-BEZ235 and chlorin E6 (Ce6), and uses lecithin and distearoylphosphatidylethanolamine - Polyethylene glycol (DSPE-PEG) for PEGylation of the carrier surface.

[0068] The preparation method is as follows:

[0069] (1) Dissolve 0.75mg NVP-BEZ235 and 0.5mg Ce6 in 300μL DMSO to obtain a drug solution;

[0070] (2) 20 mg of polylactic acid-glycolic acid was dissolved in 700 μL of acetonitrile to obtain a carrier solution;

[0071] (3) Mix the drug solution obtained in step (1) with the carrier solution obtained in step (2), and ultrasonicate for 4 minutes to form an oil phase solution;

[0072] (4) 5 mg of lecithin and 5 mg of distearoylphosphatidylethanolamine-polyethylene glycol were dissolved in 5 mL of deionized water to obtain an aqueous phase solution;

[0073] (5) Add the oil phase solution obtained in step (3) to the water phase solution obtained in step...

Embodiment 3

[0076] In this example, the nano-carrier drug uses polylactic acid-glycolic acid (PLGA) as a carrier, loaded with NVP-BEZ235 and chlorin E6 (Ce6), and uses lecithin and distearoylphosphatidylethanolamine - Polyethylene glycol (DSPE-PEG) for PEGylation of the carrier surface.

[0077] The preparation method is as follows:

[0078] (1) Dissolve 1.2mg NVP-BEZ235 and 0.6mg Ce6 in 300μL DMSO to obtain a drug solution;

[0079] (2) 25 mg of polylactic acid-glycolic acid was dissolved in 700 μL of acetonitrile to obtain a carrier solution;

[0080] (3) Mix the drug solution obtained in step (1) with the carrier solution obtained in step (2), and ultrasonicate for 6 minutes to form an oil phase solution;

[0081] (4) 7.5 mg of lecithin and 7.5 mg of distearoylphosphatidylethanolamine-polyethylene glycol were dissolved in 5 mL of deionized water to obtain an aqueous phase solution;

[0082] (5) Add the oil phase solution obtained in step (3) to the water phase solution obtained in s...

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Abstract

The invention provides a nanocarrier medicine, as well as a preparation method and an application of the nanocarrier medicine. The nanocarrier medicine takes polylactic acid-glycolic acid as a carrier, and is loaded with NVP-BEZ235 and chlorin E6, and the surface of a carrier is subjected to PEGylation by using lecithin and distearoyl phosphoethanolamine-polyethylene glycol. The polylactic acid-glycolic acid is taken as the carrier, the chlorin E6 and the NVP-BEZ235 are combined to serve as a therapeutic agent, and the photodynamics therapy and the biotherapy are combined and produce a synergistic effect to improve the killing effect on a tumor cell. The lecithin and the DSPE-PEG are used to conduct PEGylation on the surface of a nanoparticle, the time for blood circulation is prolonged, the clearing of reticuloendothelium is reduced, the therapeutic effect is further guaranteed, so that the therapeutic effect of tumors, particularly the triple negative breast cancer, is obvious, and the nanocarrier medicine has a broad application prospect.

Description

technical field [0001] The invention belongs to the field of nano-medicine, and relates to a nano-carrier drug and a preparation method and application thereof. Background technique [0002] Triple-negative breast cancer (TNBC) has seriously threatened the physical and mental health of women all over the world due to its extremely low survival rate. Compared with other types of breast cancer, TNBC is difficult to achieve molecular targeted therapy due to the lack of unique surface receptors (ER- / PR- / HER2-), coupled with high metastasis rate and poor prognosis of advanced patients, making its treatment more challenging. How to effectively treat TNBC has been the most active research field in tumor therapy, but there are still many obstacles to be overcome. So far, there is still no effective drug approved by the US Food and Drug Administration (FDA) for the treatment of TNBC. Innovative and effective comprehensive treatment for TNBC is imminent. Targeting and inhibiting t...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K41/00A61K31/4745A61K47/34A61K47/24A61P35/00
CPCA61K9/5123A61K9/5146A61K31/4745A61K41/0071A61K2300/00
Inventor 梁兴杰艾哈迈德·沙科尔·爱尔塔汉郭伟圣卿光超
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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