A kind of drug-loaded fibrous ring and its preparation method and application

Abstract

The invention relates to a drug-loaded fiber ring and its preparation method and application, comprising: preparing DOX / PLGA drug-loaded nanofiber membrane by electrospinning, homogenizing treatment to obtain DOX / PLGA drug-loaded fiber ring, and the surface is chelated by hyperbranched PEI Gd(III) is used in MR imaging, and modified DNA aptamers serve as targeting molecules, which tightly bind to cancer cells and can effectively inhibit tumor metastasis and invasion. The invention has a simple preparation process and good biological safety of the material. The ring material is more likely to anchor cancer cells and reduce the shedding of tumor cells. The drug loaded inside can effectively act on tumor tissues for a long time, effectively inhibiting their metastasis while killing cancer cells. , has broad application prospects in the field of cancer therapy.

Description

Technical field

[0001] The present invention belongs to the field of cancer treatment, and in particular, the present invention relates to a cargo fiber ring and a preparation method thereof. Background technique

[0002] In recent years, cancer has become an important killer that endangers human life, and more than 90% of the cancer patients have died caused by tumors transfer and recurrence. Tumor cells have metastasis and invasive properties, and tumor cells enter the blood circulation system from the in situ local tumor lesion to become cycle tumor cell CTCs, and thereby reaching the bloodstream to the organs other than the pathogenesis and even spread to the whole body. Once the tumor is distant, most of the treatment is limited, and the prognosis is extremely poor. Once the tumor cells are removed from the blood, local treatment (surgery, radiotherapy) is ineffective, even with systemic treatment means - chemical treatment, the circulating tumor cells have certain kills, bu...

Examples

Embodiment 1

[0053] (1) 0.5 g of polylactic acid-hydroxyacetic acid PLGA particles were added to a mixed solution of 2 mL of N, N-dimethylformamide DMF and tetrahydrofuran THF, and the volume ratio of DMF: THF was 1: 3, magnetic stir stock 4 ~ At 8 h, it obtained a PLGA spinning liquid; weighed 50 mg hydrochloride DOX to add to PLGA spinning fluid, stirred vigorously for 48 h, resulting in DOX / PLGA spinning fluid; then electrospheric spun (spinning voltage 20 kV, injection pump flow rate 0.6 ml / h, the received distance was 15 cm, ambient temperature 25 ° C, a humidity of 30%, and then dried in vacuo to dry 48h, a DOX @ PLGA nanofiber film of the internal load anti-cancer drug was obtained.

[0054] (2) Soak the DOX @ PLGA nanofibers obtained by step (1) in ultrapure water 3min, from the aluminum foil paper, and cut into area of ​​approximately 0.25cm 2 Square fragments, then transferred to a polyvinyl alcohol PVA solution containing sodium chloride, wherein the concentration of sodium chlo...

Embodiment 2

[0059] The invention is characterized by scanning electron microscopy SEM, UV-visible light spectrometer UV-VIS, inductive coupling plasma spectrometer ICP, drug sustained release test, in vivo magnetic resonance MR imaging performance test, and tumor therapy and inhibiting metastasis and invasion evaluation Characterization The performance of the functionalized fiber ring prepared and its application potential in cancer treatment.

[0060] Scanning electron microscope test:

[0061] The morphology and size of the DOX @ PLGA nanofiber film obtained in Example 1 (1) is characterized by SEM, and the results are figure 2 As shown, it is understood that the surface of DOX @ PLGA nanofibers is smooth, uniform in shape, and the fiber diameter is around 934.6 nm; the average outer diameter of the DOX @ PLGA fiber ring obtained after homogeneous treatment is 11.1 μm.

[0062] Ultraviolet - visible light spectrometer test:

[0063] The DNA adapter has a feature ultraviolet absorption peak ...

Embodiment 3

[0071] Hemolysis test test:

[0072] The blood compatibility of the PLGA-PEI-GD / Aptamer in ratio 1 was characterized by hemolysis test. First, 1 ml of fresh healthy people, centrifugal, PBS was washed 3 times, and the plasma was discarded, and the red blood cell HRBCs was obtained. The resulting HRBCS was diluted 30 times with a PBS solution, and 0.2 ml of HRBCs dilution was removed from 0.8 mL of PBS, as a negative control; 0.2 mLHrBCs dilution was added to 0.8 ml of ultra-pure water as a positive control. The HRBCs dilution after the above dilution was diluted with PBS, then weighed 2 mg, 4 mg, 6 mg of PLGA-PEI-GD / APTAMER obtained by step (5), respectively, added to 1 mL again diluted 5 times In the post-HRBCS suspension, 5 parallels were provided for each concentration, incubated in a thermostatic closing of 37 ° C. Finally, the control group and the HRBCs suspension containing the fiber ring material were centrifuged at 10000 r / min for 1min, centrifuged, and taking a pho...

Technical field

[0001] The present invention belongs to the field of cancer treatment, and in particular, the present invention relates to a cargo fiber ring and a preparation method thereof. Background technique

[0002] In recent years, cancer has become an important killer that endangers human life, and more than 90% of the cancer patients have died caused by tumors transfer and recurrence. Tumor cells have metastasis and invasive properties, and tumor cells enter the blood circulation system from the in situ local tumor lesion to become cycle tumor cell CTCs, and thereby reaching the bloodstream to the organs other than the pathogenesis and even spread to the whole body. Once the tumor is distant, most of the treatment is limited, and the prognosis is extremely poor. Once the tumor cells are removed from the blood, local treatment (surgery, radiotherapy) is ineffective, even with systemic treatment means - chemical treatment, the circulating tumor cells have certain kills, bu...

Examples

Embodiment 1

[0053] (1) 0.5 g of polylactic acid-hydroxyacetic acid PLGA particles were added to a mixed solution of 2 mL of N, N-dimethylformamide DMF and tetrahydrofuran THF, and the volume ratio of DMF: THF was 1: 3, magnetic stir stock 4 ~ At 8 h, it obtained a PLGA spinning liquid; weighed 50 mg hydrochloride DOX to add to PLGA spinning fluid, stirred vigorously for 48 h, resulting in DOX / PLGA spinning fluid; then electrospheric spun (spinning voltage 20 kV, injection pump flow rate 0.6 ml / h, the received distance was 15 cm, ambient temperature 25 ° C, a humidity of 30%, and then dried in vacuo to dry 48h, a DOX @ PLGA nanofiber film of the internal load anti-cancer drug was obtained.

[0054] (2) Soak the DOX @ PLGA nanofibers obtained by step (1) in ultrapure water 3min, from the aluminum foil paper, and cut into area of ​​approximately 0.25cm 2 Square fragments, then transferred to a polyvinyl alcohol PVA solution containing sodium chloride, wherein the concentration of sodium chlo...

Embodiment 2

[0059] The invention is characterized by scanning electron microscopy SEM, UV-visible light spectrometer UV-VIS, inductive coupling plasma spectrometer ICP, drug sustained release test, in vivo magnetic resonance MR imaging performance test, and tumor therapy and inhibiting metastasis and invasion evaluation Characterization The performance of the functionalized fiber ring prepared and its application potential in cancer treatment.

[0060] Scanning electron microscope test:

[0061] The morphology and size of the DOX @ PLGA nanofiber film obtained in Example 1 (1) is characterized by SEM, and the results are figure 2 As shown, it is understood that the surface of DOX @ PLGA nanofibers is smooth, uniform in shape, and the fiber diameter is around 934.6 nm; the average outer diameter of the DOX @ PLGA fiber ring obtained after homogeneous treatment is 11.1 μm.

[0062] Ultraviolet - visible light spectrometer test:

[0063] The DNA adapter has a feature ultraviolet absorption peak ...

Embodiment 3

[0071] Hemolysis test test:

[0072] The blood compatibility of the PLGA-PEI-GD / Aptamer in ratio 1 was characterized by hemolysis test. First, 1 ml of fresh healthy people, centrifugal, PBS was washed 3 times, and the plasma was discarded, and the red blood cell HRBCs was obtained. The resulting HRBCS was diluted 30 times with a PBS solution, and 0.2 ml of HRBCs dilution was removed from 0.8 mL of PBS, as a negative control; 0.2 mLHrBCs dilution was added to 0.8 ml of ultra-pure water as a positive control. The HRBCs dilution after the above dilution was diluted with PBS, then weighed 2 mg, 4 mg, 6 mg of PLGA-PEI-GD / APTAMER obtained by step (5), respectively, added to 1 mL again diluted 5 times In the post-HRBCS suspension, 5 parallels were provided for each concentration, incubated in a thermostatic closing of 37 ° C. Finally, the control group and the HRBCs suspension containing the fiber ring material were centrifuged at 10000 r / min for 1min, centrifuged, and taking a pho...

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