Magnetic resonance imaging nanometer drug carrier, and nanometer drug loading system and preparation method thereof

A nano drug carrier and magnetic resonance imaging technology, applied in the field of biomedicine, can solve the problems affecting the application of magnetic resonance imaging, lack of targeting, fast metabolism of magnetic resonance imaging contrast agents, etc., achieve low toxicity treatment effect, and simple preparation method Ease of operation, overcoming the effect of poor selectivity

Active Publication Date: 2018-02-23
JINAN UNIVERSITY
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  • Abstract
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Problems solved by technology

However, MRI contrast agents have the characteristics of fast metabolism and lack of targeting, which affect the clinical application of MRI.

Method used

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  • Magnetic resonance imaging nanometer drug carrier, and nanometer drug loading system and preparation method thereof
  • Magnetic resonance imaging nanometer drug carrier, and nanometer drug loading system and preparation method thereof
  • Magnetic resonance imaging nanometer drug carrier, and nanometer drug loading system and preparation method thereof

Examples

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preparation example Construction

[0092] The above-mentioned tri-block polymer is made into tri-block polymer nanoparticles of the NMR antitumor drug carrier of the present invention, and the preparation method comprises the following steps:

[0093] S1. Preparation of PLGA, nuclear magnetic imaging drugs, and fat-soluble antitumor drugs in acetone; wherein the concentration of PLGA is 1-10 mg / mL, and the concentration of ultra-small superparamagnetic iron oxide nanoparticles (SPIO) is 1-20 mg / mL, the concentration of doxorubicin (DOX) is 10~500 μ M; The nuclear magnetic imaging drug comprises ultrasmall superparamagnetic iron oxide nanoparticle (SPIO) and gadopentetate meglumine injection; The antineoplastic drug Daunorubicin, doxorubicin, demethoxydaunorubicin, epirubicin, paclitaxel, lentinan, vinblastine, vincristine, tamoxifen, formestane, anastrozole, flutamide, 5-fluorouracil, methotrexate, cisplatin, carboplatin, oxaliplatin, carmustine, toremifene, tegafur, curcumin, demethoxycurcumin, bimethoxycurcu...

Embodiment 1 3

[0102] Example 1 Preparation and Characterization of Triblock Polymer Nanoparticles cRGD-PLGA-SPIO@DOX

[0103] (1) Under normal temperature and pressure (15-35°C, 1 standard atmospheric pressure), polylactic acid-glycolic acid copolymer (PLGA), ultra-small superparamagnetic iron oxide nanoparticles (SPIO) (purchased from Sigma Company) and A Mymycin (DOX) was added to the acetone solution, the mass concentration of polylactic-co-glycolic acid (PLGA) was 5 mg / mL, the mass concentration of ultra-small superparamagnetic iron oxide nanoparticles (SPIO) was 1 mg / mL, and Adriamycin Acetone solution with DOX concentration of 10 mM.

[0104] (2) Add 3 mL of the prepared acetone solution dropwise to 10 mL of Tween-80 aqueous solution (5 mg / mL), at a rate of 1 to 5 seconds between each drop, and stir overnight at 400 rpm to obtain Adriamycin The concentration of 0.3mg / mL is PLGA aqueous solution.

[0105] (3) Add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) and N...

Embodiment 2 3

[0108] Example 2 In vitro anti-human lung cancer cell activity of triblock polymer nanoparticles cRGD-PLGA-SPIO@DOX

[0109] In this implementation example, cRGD-PLGA-SPIO@DOX (prepared in Example 1) was used. After A549 cells and HeLa cells (purchased from the American Type Culture Collection, ACTT) were cultured for 24 h, respectively, 0.0625-2 μM drug (cRGD-PLGA-SPIO@DOX) was added for pretreatment for 72 h, and doxorubicin (DOX ) as a control. The result is as Figure 8 As shown, visible, the IC of cRGD-PLGA-SPIO@DOX in A549 cells 50 It is 0.19μM, which is more than 3 times of the activity of DOX alone.

[0110] After being fixed by PI staining, the cell cycle of A549 treated with DOX, cRGD-PLGA-SPIO@DOX was analyzed by flow cytometry. The result is as Figure 9 As shown, it can be seen that the treatment of 1 μM concentration of cRGD-PLGA-SPIO@DOX caused the apoptosis peak, that is, the apoptosis peak increased from 2.5% of the control group to 36.2%, which was highe...

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Abstract

The invention discloses a magnetic resonance imaging nanometer drug carrier, and a nanometer drug loading system and a preparation method thereof. The magnetic resonance imaging nanometer drug carrieris a triblock polymer nanoparticle, wherein the triblock polymer is PLGA-PEI-PEG, and has active groups on the surface, and the active groups comprise amino, hydroxyl and carboxyl. According to the present invention, the drug carrier can efficiently load a nuclear magnetic resonance imaging drug and an antitumor drug to make the antitumor drug specifically reach the tumor lesion site, such that the nuclear magnetic resonance positioning of the superparamagnetic ferroferric oxide nanoparticle at the tumor region can be achieved while the high-selectivity and low-toxicity treatment effect can be achieved, and the disadvantages of poor selectivity, strong toxic-side effect, easy drug-resistance generation and the like of the traditional cytotoxic drugs can be overcome; and the preparation method is simple and is easy to perform, the prepared triblock polymer nanoparticle can be stably stored in the aqueous solution so as to be easily stored, and various functional groups exist on the surface of the particle, such that the prepared triblock polymer nanoparticle can be easily subjected to surface modification or surface functionalization.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a magnetic resonance imaging nano drug carrier, a nano drug loading system and a preparation method thereof. Background technique [0002] Tumors seriously endanger human health and hinder social and economic development. Therefore, how to effectively prevent, diagnose and treat cancer has become a top priority for biomedical research. In 2002, J. Funkhouser first proposed and defined the integration of diagnosis and treatment (Theranostic). The integration of diagnosis and treatment is to integrate the diagnosis (Diagnosis) and treatment (Therapy) of diseases to improve the comprehensive treatment effect of diseases. [0003] The integrated nano-reagent for diagnosis and treatment is a multi-functional platform that provides tumor diagnosis and treatment at the same time. This can provide a large amount of rapid verification of disease and accurate location information o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/12A61K49/18A61K31/704A61K45/00A61K47/34A61K47/42A61P35/00C08G81/02
CPCA61K31/704A61K45/00A61K47/34A61K47/42A61K49/126A61K49/1827C08G81/025C08G81/027
Inventor 罗良平陈填烽史长征肖泽宇陈樑张冬
Owner JINAN UNIVERSITY
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