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A kind of preparation method of multistage sustained-release drug-loaded nano-short fibers

A drug-loaded nano and short fiber technology, which is applied in fiber treatment, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of reducing the utilization rate of drugs, secondary harm to patients, etc., and overcome multi-drug resistance , low cost, and the effect of improving the treatment effect

Active Publication Date: 2021-05-11
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, electrospun nanofibers are usually used in the form of membranes, which can only be implanted or administered externally, which is likely to cause secondary harm to patients or reduce the utilization rate of drugs

Method used

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  • A kind of preparation method of multistage sustained-release drug-loaded nano-short fibers
  • A kind of preparation method of multistage sustained-release drug-loaded nano-short fibers
  • A kind of preparation method of multistage sustained-release drug-loaded nano-short fibers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] (1) 830.8mg Mg(NO 3 ) 2 ·6H 2 O and 603.8mg Al(NO 3 ) 3 9H 2 O was dissolved in 50 mL of ultrapure water, and stirred vigorously at 25 °C for 20 min to fully dissolve the two compounds. Mix the two solutions well. Nitrogen was flushed to catch oxygen 5 times, and then 15 mL of 1M NaOH solution was added in a nitrogen atmosphere to adjust the pH of the solution to 9.5. Stir vigorously at 25°C for 48 h to fully react. Collect the reacted solution in a centrifuge tube, set the rotation speed at 6000 rpm, and centrifuge for 10 minutes, and the white precipitate obtained is LDH. Add an appropriate amount of ultrapure water and use a vortex shaker to disperse the precipitate evenly, perform ultrasonic washing, and then set the rotation speed at 6000rpm for 10 minutes. Repeat the operation 3 times to obtain pure LDH precipitate. LDH nanoparticles were obtained by vacuum freeze-drying.

[0045] (2) Fully dissolve 20.3 mg DOX and 10.3 mg of LDH prepared in step (1) in 10...

Embodiment 2

[0049] The present invention uses scanning electron microscope (SEM), transmission electron microscope (TEM), X-ray diffraction (XRD), infrared spectrum analysis (FTIR), ultraviolet-spectrophotometer (UV-Vis), coagulation experiment, cell viability analysis ( CCK-8 test), laser confocal microscopy to characterize the morphology of LDH prepared by the present invention and multi-level slow-release drug-loaded nano-short fibers, the long-term multi-level drug release effect of short fibers and the effect of short fibers in drug-resistant cancer cells application potential.

[0050] Scanning Electron Microscopy Test:

[0051] The LDH obtained in step (1) of Example 1 and the DOX@LDH / α-TOS / PLGA short fiber obtained in step (5) were characterized by a scanning electron microscope. The SEM results of LDH are as follows figure 2 As shown in a-b, the diameter of LDH is 76±18.9nm, and it is relatively uniform hexagonal or disc-shaped. The SEM results of DOX@LDH / α-TOS / PLGA short fib...

Embodiment 3

[0059] In vitro release kinetics test

[0060] Using UV-spectrophotometer (UV-Vis) to measure drug release from short fibers in buffer solution with different pH at different time points. Add 5 mg of DOX / PLGA, α-TOS / PLGA and DOX@LDH / α-TOS / PLGA short fibers into 1 mL of PBS buffer solution with pH=7.4, 6.8 and 5.5, and ultrasonically disperse evenly, and put them into a dialyzer with a molecular weight cut-off of 5000 In the bag, put the dialysis bag filled with materials into a 50mL centrifuge tube, add 9mL of PBS buffer solution corresponding to the pH, and put it in a constant temperature shaker for drug sustained release experiments. Take the solution at 1, 2, 4, 8, 16, 24, 48, and 72 hours in the first 3 days, take the solution every two days from the 4th day to the 20th day, and take the solution every five days from the 20th day to the 60th day . Take 1 mL each time, and then add 1 mL of PBS buffer solution corresponding to the pH to the centrifuge tube. Measure the a...

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Abstract

The present invention relates to a preparation method of multi-level sustained-release drug-loaded nano-short fibers, comprising layered double hydroxide (LDH) loaded with anticancer drug doxorubicin (DOX) and P-gp inhibitor α-growth Phenolsuccinate (α-TOS) was mixed together in poly(lactic-co-glycolic acid) (PLGA) spinning solution for electrospinning and homogenized. The present invention constructs double-loaded multi-level slow-release drug-loaded nano-short fibers with organic and inorganic dual carriers. The anticancer drugs and P-gp inhibitors in the material can be released in multiple levels in the slightly acidic environment of the tumor, and are used to overcome cancer. The multi-drug resistance of cells, the double-carrier nanofiber prolongs the drug release path, realizes the long-term sustained release of anticancer drugs, and provides a new method for the long-term effective treatment of drug-resistant tumors.

Description

technical field [0001] The invention belongs to the field of drug carriers, and in particular relates to a preparation method of multi-level slow-release drug-loaded nano-short fibers. Background technique [0002] Cancer is one of the leading causes of death, and the World Health Organization (WHO) estimates that 13.13 million deaths will be related to cancer in 2030. Currently, cancer treatment options mainly include surgery, chemotherapy, radiation therapy, and combinations of these methods. Chemotherapy, as one of the most commonly used treatments, mainly causes the death of rapidly growing and dividing cancer cells by interfering with DNA synthesis and mitosis. Many primary tumors and metastatic lesions respond well initially to chemotherapy, but tumors often recur and develop drug resistance. Drug resistance is mainly reflected in the insensitivity of cancer cells to treatment, which is a key factor leading to the failure of anti-tumor chemotherapy. Because these tu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61K31/704A61K31/355A61K9/00A61K47/02A61K47/34A61P35/00D01D5/00
CPCA61K9/0019A61K31/355A61K31/704A61K45/06A61K47/02A61K47/34A61P35/00D01D5/003D01D5/0061A61K2300/00
Inventor 史向阳马玉培肖云超
Owner DONGHUA UNIV
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