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Targeted EGFR (epidermal growth factor receptor) modified platinum drug supported albumin nanoparticle as well as preparation and application thereof

A technology of albumin nanoparticles and platinum drugs, which is applied in the directions of drug combination, drug delivery, and medical preparations of inactive ingredients, etc., to achieve the effect of inhibiting tumor growth, good stability, and promoting tumor cell apoptosis.

Active Publication Date: 2015-05-13
上海纳奥生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the past, the "targeting ligands" for modifying tumor drugs were molecules such as antibodies, polypeptides, and folic acid, but these ligand-modified targeting drugs had insurmountable defects in practical applications

Method used

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  • Targeted EGFR (epidermal growth factor receptor) modified platinum drug supported albumin nanoparticle as well as preparation and application thereof
  • Targeted EGFR (epidermal growth factor receptor) modified platinum drug supported albumin nanoparticle as well as preparation and application thereof
  • Targeted EGFR (epidermal growth factor receptor) modified platinum drug supported albumin nanoparticle as well as preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Preparation of albumin nano-preparation targeting EGFR-loaded cisplatin drug

[0034] Mix 2 mL of 25% (w / w) human serum albumin aqueous solution and 4 mL of 0.5 mg / ml cisplatin aqueous solution, add 6 mL of absolute ethanol, stir at room temperature for 2 hours, and add pentadiene at a final concentration of 0.01% (w / w) after 2 hours Aldehyde, stirred overnight at room temperature. Centrifuge at 12000 rpm for 30 min at 4°C, discard the supernatant, and redisperse in 10 mL of normal saline to prepare a cisplatin-loaded albumin nanoparticle solution.

[0035] Take 2 mL of cisplatin-loaded albumin nanoparticle solution, add 100 μM EDC and NHS, fully activate the reaction for 20 min under magnetic stirring, then add 1 mg / ml EGFR nucleic acid aptamer (sequence: 5'-NH 2 -

[0036] C6-UGCCGCUAUAAUGCACGGAUUUAAUCGCCGUAGAAAGCAUGUCAAAGCCGUU-3') solution 1mL and 5mg / ml aminated PEG molecule (molecular weight 4000Da) 1mL, after 2 hours of reaction, take the reaction sol...

Embodiment 2

[0037] Example 2: In vitro sustained-release experiment of polymer nanoparticles loaded with cisplatin

[0038] A certain amount of cisplatin-loaded nanoparticles was put into a pre-treated dialysis bag (MWCO, 3500), placed in a conical flask filled with 18ml of PBS (pH=7.4), and dialyzed at a constant temperature of 120rpm / min at 37°C. 2 ml of dialysate was taken out at predetermined time intervals, and 2 ml of 37° C. PBS solution was supplemented at the same time, and the content of platinum in the dialysate was measured by an inductively coupled plasma emission spectrometer. Calculate the cumulative drug release at different times, and draw the drug release curve in vitro. The result is as figure 2 As shown, it can be seen from the figure that the cisplatin-loaded nanoparticles can achieve the slow release effect of loaded platinum-based drugs in a neutral environment in vitro.

Embodiment 3

[0039] Example 3: In vitro uptake experiment of cervical cancer HELA cells to cisplatin albumin nanoparticles

[0040] 10% FCS DMEM medium routinely cultured human cervical cancer HELA cells, containing 1% (v / v) penicillin-streptomycin (100 U / ml penicillin G and 100 μg / ml streptomycin), in a 37°C incubator ( 5%CO 2 ) incubation, and the cells in the logarithmic growth phase were taken for experiments. HELA cells were seeded in a 24-well plate at a density of 3 × 10 cells per well 4 / ml, 37°C, 5% CO 2 cultured overnight in a cell culture incubator. Under dark operation, targeted nanoparticles containing fluorescently labeled EGFR aptamers were added to different wells, and cultured in a 37°C cell culture incubator for 1 hour. Aspirate the culture medium and wash 3 times with PBS at 37°C. The uptake of nanoparticles by cells was observed under a confocal fluorescence microscope, and the results are shown in image 3 .

[0041] From image 3 It can be observed that the sp...

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Abstract

The invention belongs to the field of a medicinal preparation, and relates to an EGFR (epidermal growth factor receptor) modified platinum drug albumin nano preparation with a target tumor cell identification function. According to the invention, albumin is used for supporting platinum drugs, medical PEG (polyethylene glycol) is taken as a dispersing and cross-linking agent, and amination EGFR aptamer is taken as a target modifying molecule, so that the soluble albumin nano (Apt-PtNPs) preparation is prepared. The nanoparticle can be specifically combined with the EGFR on the surface of the tumor cell and has a cell endocytosis function, so that the toxic and side effects of the platinum drugs can be reduced, the purposes of toxicity reduction and efficacy enhancement are achieved, EGFR expression can be inhibited by prompting EGFR protein phosphorylation, and the anti-tumor effect of the nanoparticle in combination of the platinum drugs is achieved; the nanoparticle can be used for preparing the anti-tumor drugs, and particularly, the treatment research of the nanoparticle in the aspects of cervical cancer and ovarian cancer proves that the nanoparticle is good in targeting and good in killing effect and has good application prospect in gene therapy of tumors and combined treatment by chemotherapeutic drugs.

Description

(1) Technical field [0001] The invention relates to a platinum-based drug-loaded albumin nanoparticle specifically targeting human epidermal growth factor receptor (EGFR), a preparation method and application thereof. (2) Background technology [0002] Cervical cancer is the second most common malignant tumor after breast cancer in women worldwide, and its incidence rate ranks first among Chinese women. Worldwide, more than 200,000 women die from cervical cancer every year. According to the survey of 29 provinces, municipalities and autonomous regions, the death rate of cervical cancer in my country ranks fourth in the total cancer death rate and the second in female cancer. The age of onset is the most from 40 to 50 years old. Ovarian cancer is the most malignant disease among gynecological tumors, and ranks first in the mortality rate of gynecological malignant tumors, seriously threatening women's reproductive health. Ovarian cancer has an insidious onset and is prone ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K33/24A61K47/42A61K47/34A61K47/18A61P35/00
Inventor 亓立峰
Owner 上海纳奥生物科技有限公司
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