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Cyclooxygenase-2 inhibitor and nano-drug delivery system drug composition and application thereof

A technology of nano-medicine and cyclooxygenase, which is applied in the direction of drug combination, capsule delivery, anti-tumor drugs, etc., to improve the therapeutic effect, promote normalization, and reduce the effect of tumor stromal cells

Inactive Publication Date: 2017-12-08
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is currently no research on the application of COX-2 inhibitors to comprehensively regulate the tumor microenvironment and achieve more effective tumor cell drug delivery.

Method used

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  • Cyclooxygenase-2 inhibitor and nano-drug delivery system drug composition and application thereof
  • Cyclooxygenase-2 inhibitor and nano-drug delivery system drug composition and application thereof
  • Cyclooxygenase-2 inhibitor and nano-drug delivery system drug composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1, the overall regulatory effect of celecoxib on the tumor microenvironment

[0032] A549 lung cancer-bearing model mice were treated with celecoxib (dose 200 mg / kg / d) for two consecutive weeks, then sacrificed, the heart was perfused, and tumors were taken to prepare frozen sections; immunofluorescent staining was performed by FAPα antibody-labeled TAF (green ), fibronectin was used as a representative extracellular matrix, which was labeled with fibronectin (green), pericytes were labeled with SMA-α antibody (green), and vascular endothelial cells were labeled with CD-31 antibody (red). The experimental results showed that, Compared with the control group, intratumoral fibroblasts were significantly reduced in the celecoxib group (eg figure 2 As shown in A, P figure 2 B), the coverage of pericytes on endothelial cells was significantly increased (as shown in figure 2 As shown in C, P 488 labeled lectins ( 488-lectin) at a dose of 5 mg / kg. After 1 h, the a...

Embodiment 2

[0033] Example 2, the effect of celecoxib on intratumoral delivery of micelles after regulating the tumor microenvironment

[0034] Weigh mPEG 2000 -PLA 2000 20mg, dissolved in 1ml acetonitrile, ultrasonically dispersed, 40°C rotary evaporation for 2h to remove acetonitrile, adding PBS preheated at 40°C for several minutes to redissolve to obtain a blank micellar preparation; measure the blank micelles with a particle size / Zeta potential analyzer The average particle size and Zeta potential value of the measured micellar particle size is about 22.1 ± 1.5nm (such as image 3 As shown in A), the potential is -3.1±0.7mv. After the micelles were negatively stained with 2% (w / v, pH=7.0) phosphotungstic acid, the morphology of the micelles was observed with a transmission electron microscope. The results showed that the particles under the electron microscope were spherical, regular in shape, smooth in surface and well dispersed (such as image 3 as shown in B);

[0035] After ...

Embodiment 3

[0037] Example 3, the therapeutic effect of celecoxib combined with paclitaxel-loaded micelles on A549 tumors

[0038] When the tumor diameter reached 4-5 mm, 24 tumor-bearing nude mice were randomly divided into four groups, 6 in each group. a, Control group (administrated with blank celecoxib preparation for two weeks, and administered blank micelles via tail vein after treatment); b, Celecoxib group (treated with intragastric administration of celecoxib preparation for two weeks, administered with tail vein after treatment) Blank micelles); c, Control+Micelles-PTX group (two-week blank celecoxib preparation intragastric administration, after the end of the treatment, tail vein administration of paclitaxel-loaded micelles); d, Celecoxib++Micelles-PTX group (two weeks Celecoxib preparations were treated by intragastric administration, and paclitaxel-loaded micelles were administered by tail vein after the treatment); the administration method of paclitaxel micelles or blank m...

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Abstract

The invention belongs to the technical field of biology and relates to a tumor targeting therapy drug composition, in particular to a cyclooxygenase-2 inhibitor and nano-drug delivery system drug composition and application thereof. According to the drug composition, COX-2 serves as a target spot to comprehensively adjust and control the tumor microenvironment so as to increase nano-drug tumor-interior delivery to be used for tumor therapy. By inhibiting COX-2 of the tumor position, reducing tumor matrix cells, destroying tumor matrix components, facilitating normalization of tumor blood vessels and increasing tumor-interior blood flow pouring and nano-particle tumor-interior penetration, tumor-interior delivery of nano drugs is increased, and the therapy effect of the nano drugs for tumor is improved. The invention provides a novel intervention strategy aiming at the tumor for clinical practice.

Description

technical field [0001] The invention belongs to the field of biological technology, and relates to a pharmaceutical composition for targeted tumor therapy, in particular to a pharmaceutical composition of a cyclooxygenase-2 inhibitor and a nanometer drug delivery system and its application. Enzyme-2 as a target to regulate the tumor microenvironment to increase the intratumoral delivery of nanomedicine for the treatment of solid tumors. Background technique [0002] The prior art discloses that the tumor microenvironment includes extracellular matrix and stromal cells, such as tumor-associated fibroblasts, vascular endothelial cells, macrophages, pericytes, and some immune cells and adipocytes. The tumor microenvironment makes the internal environment of the tumor very complicated, which seriously affects the drug delivery of the tumor. The impact mainly includes: ① Leakage of blood vessels inside the tumor, poor function, coupled with the extrusion of the matrix, the blood ...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/635A61K31/337A61K9/107A61K9/51A61P35/00
Inventor 庞志清张波蒋新国沈顺
Owner FUDAN UNIV
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