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Multifunctional composite nanometer medicine for tumor imaging and treatment and preparation method of composite nanometer medicine

A nano-drug, tumor imaging technology, applied in the field of medicine, can solve the problem of low drug loading

Inactive Publication Date: 2016-11-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, several nanocarriers for sorafenib delivery have been reported, but low drug loading (<10%) is their common defect

Method used

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  • Multifunctional composite nanometer medicine for tumor imaging and treatment and preparation method of composite nanometer medicine
  • Multifunctional composite nanometer medicine for tumor imaging and treatment and preparation method of composite nanometer medicine
  • Multifunctional composite nanometer medicine for tumor imaging and treatment and preparation method of composite nanometer medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Dissolve sorafenib (active molecule-1, 4.65 mg, 10 mMol) and indocyanine green derivative (active molecule-2, 6.64 mg, 10 mMol) in 10 mL of methanol, and stir for 20 hours at 20°C in the dark . After the reaction is complete, quickly add TPGS aqueous solution (9% mass fraction, 40 mL) under ultrasound. After the addition, keep stirring in a fume hood for 24 hours, freeze-dry and store at -4°C. Available as figure 2 The composite nano drug particles shown. By changing the concentration of the drug solution, the concentration of the stabilizer solution, etc., nanoparticles of different sizes (such as figure 2 Shown).

Embodiment 2

[0025] The multifunctional composite nanomedicine described in Example 1 was measured by transmission electron microscope (FEI, Tecnai G2 20S-TWIN, 200kV, USA), as figure 2 Shown. The multifunctional composite nanomedicine prepared in Example 1 was subjected to tumor cell killing experiments on the liver cancer cell Huh7. Culture the Huh7 hepatocellular carcinoma cells at a temperature of 37℃. Inoculate the Huh7 cells in the logarithmic growth phase into a 96-well culture plate at a density of 5000 cells / well. After 12 hours, add different concentrations of drug solution and multifunctional nanocomposite. Drugs, each concentration has 6 holes in parallel. DMEM medium containing 10% by weight of fetal bovine serum was used, 100 μL was added to each well, and after 48 hours of culture, the cell viability was measured using a CCK kit. The specific operation is carried out completely in accordance with the instructions of the kit.

[0026] The experimental results of the effect on...

Embodiment 3

[0028] The multifunctional composite nanomedicine prepared in Example 1 was used to perform tumor targeting and fluorescence imaging experiments on liver cancer models in nude mice. The PBS solution of the multifunctional composite nanomedicine prepared in Example 1 was injected through the tail vein of nude mice, and the small animal in vivo imaging system (Bruker, USA) in VivoXtreme ) Detect the fluorescence of indocyanine green (excitation 760 nm, emission 830 nm). The experimental results of tumor targeting and fluorescence imaging capabilities are as follows Figure 4 Shown. It can be seen from the experimental results that the multifunctional composite nanomedicine provided by the present invention has good tumor targeting and fluorescence imaging capabilities.

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to a multifunctional composite nanometer medicine for tumor imaging and treatment and a preparation method of the composite nanometer medicine. The composite nanometer medicine comprises an active component-1, an active component-2 and a stabilizing agent, wherein the active component-1 includes an antitumor drug of sorafenib or a derivative thereof, the active component-2 includes a near infrared fluorescent component of indocyanine green or a derivative thereof, and the stabilizing agent includes Pluronic, PLGA-PEG, TPGS, DPSE-mPEG, PVA, Tween, PEG, and Lipid. The composite nanometer medicine can be obtained through a simple and convenient nanometer precipitation method and has the size of 50-800 nm. The composite nanometer medicine has multiple functions of tumor chemotherapy and photo-thermal / photodynamic therapy, and indocyanine green is used for near infrared fluorescence imaging. The composite nanometer medicine is excellent in tumor targeting. The two components have an obvious synergistic effect, thereby improving the tumor treatment efficiency, and can be applied to tumor treatment and fluorescence imaging.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a multifunctional composite nano-medicine for tumor treatment and imaging and a preparation method thereof. Background technique [0002] Cancer is one of the major diseases that seriously endanger human health. In recent years, the incidence rate has increased at an alarming rate. Since 2010, it has become the "No. 1 killer" that causes human deaths in addition to cardiovascular diseases. Chemotherapy is one of the main ways to treat tumors in clinic, but chemotherapeutic drugs usually have disadvantages such as low drug bioavailability, poor tumor targeting, and large toxic side effects on normal tissues. With the rapid development of nanotechnology, the nanomedicine technology formed by combining it with tumor treatment opens up new ideas for cancer treatment. [0003] Nanomedicine refers to a drug delivery system with a particle size of 1-1000nm, including carrier-loade...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/22A61K31/44A61K49/00A61K41/00A61P35/00
Inventor 汪长春吴海秋金浩杰覃文新
Owner FUDAN UNIV
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