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
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[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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