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Method for loading doxorubicine (DOX) anti-cancer medicine by laponite (LAP) clay nanoparticles

A technology of doxorubicin hydrochloride and clay nanoparticles, which is applied in antineoplastic drugs, drug combinations, and pharmaceutical formulations, etc.

Inactive Publication Date: 2012-11-21
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Searching relevant literature and patents found that using LAP as a carrier to load the anticancer drug DOX and further studying its anticancer activity has not been reported

Method used

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  • Method for loading doxorubicine (DOX) anti-cancer medicine by laponite (LAP) clay nanoparticles
  • Method for loading doxorubicine (DOX) anti-cancer medicine by laponite (LAP) clay nanoparticles
  • Method for loading doxorubicine (DOX) anti-cancer medicine by laponite (LAP) clay nanoparticles

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Experimental program
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Effect test

Embodiment 1

[0055] 5mL of LAP ultrapure aqueous solution with mass concentrations of 6mg / mL and 2mg / mL were mixed with DOX ultrapure aqueous solution in equal volume, and the reaction was performed under magnetic stirring at room temperature for 24h. After the reaction, the suspension obtained by the reaction was centrifuged (8000 rpm, 5 min), washed (washed twice with distilled water), and separated and precipitated to obtain LAP-DOX nanoparticles. Use Lambda25 UV-Vis spectrophotometer to measure the absorbance of supernatant and washing solution mixture at 480nm, calculate the concentration of unwrapped DOX according to the standard curve, and then obtain the loading amount of LAP to DOX at this time, which is 98.3±0.77% .

[0056] in the attached figure 1 In the FTIR spectrum of LAP / DOX shown, 1610 cm -1 and 1580cm -1 N-H bending vibration peaks can be detected at 1410 cm -1 The C=O stretching vibration peaks at , these are the characteristic vibration peaks of DOX, which proves th...

Embodiment 2

[0058] 5mL of LAP ultrapure aqueous solution with mass concentrations of 2mg / mL and 2mg / mL were mixed with DOX ultrapure aqueous solution in equal volume, and the reaction was performed under magnetic stirring at room temperature for 24h, and the reaction was completed. The suspension obtained by the reaction was centrifuged (8000 rpm, 5 min), washed (washed twice with distilled water), and separated and precipitated to obtain LAP-DOX nanoparticles. Use a Lambda25 UV-Vis spectrophotometer to measure the absorbance of the supernatant and the washing solution mixture at 480 nm, calculate the remaining DOX concentration in the supernatant according to the standard curve, and then obtain the loading amount of LAP to DOX at this time, which is 72.4 ±0.89%. The characterization results of FTIR and XRD further prove that LAP can successfully realize the loading of DOX.

Embodiment 3

[0060] Dissolve LAP / DOX with pH=7.4 and pH=5.4 buffers respectively into a solution with a concentration of 1 mg / mL (the concentration of LAP / DOX), take 1 mL and put it in a dialysis bag to fix it, and place it in a container containing 9 mL of the corresponding buffer. in a shaker at 37°C. Samples were taken every 2h in the first 12h, and every 24h thereafter. Take 1 mL of the liquid outside the dialysis bag for each sampling, measure its absorbance value at 480 nm, and then add 1 mL of the corresponding buffer solution to the outside of the dialysis bag. The in vitro release profiles of LAP / DOX clay nanoparticles were obtained using this method, as shown in the appendix. image 3 shown. Depend on image 3 It can be clearly seen that the release rate of LAP / DOX in the pH=5.4 environment is higher than that in the neutral environment with pH=7.4, and the cumulative release rate increases almost linearly with the increase of time. In general, the microenvironment of healthy...

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Abstract

The invention relates to a method for loading doxorubicine (DOX) anti-cancer medicine by laponite (LAP) clay nanoparticles. The method comprises the following steps that (1) LAP water solution is prepared and is mixed with DOX, then, the stirring is carried out, and mixed solution is obtained, wherein the concentration of the DOX in the DOX water solution is 2mg / mL, and the concentration of the LAP in the concentration water solution is 2 to 8mg / mL; and (2) the mixed solution is centrifugally separated, supernate is sucked out, in addition, ultra-pure water is used for washing precipitation, and finally, LAP loaded with DOX is obtained. The method has the advantages that the condition is mild, the process is simple, the product is easy to operate and separate, the LAP / DOX obtained by the method can effectively control the release of DOX, the LAP / DOX anti-tumor activity is obviously improved through being compared with that of the pure DOX, and the application prospects are wide.

Description

technical field [0001] The invention belongs to the field of preparation of clay nanoparticles loaded drugs, in particular to a method for loading doxorubicine hydrochloride (Doxorubicine, DOX) anticancer drugs with laponite (Laponite, LAP) clay nanoparticles. Background technique [0002] In the process of using chemical drugs to treat tumors, anticancer drugs cannot differentiate between cancerous tissue cells and healthy cells, resulting in great damage to the body by chemotherapy. First, the indiscriminate or small difference distribution of antitumor drugs to systemic tissue cells with blood circulation will lead to systemic toxicity and side effects, and greatly limit the maximum allowable dose. Secondly, the wide distribution of drugs in different tissues and cells requires a relatively large dosage, which not only causes waste of drugs, but also brings toxic side effects. In addition, some small-molecule anticancer drugs, such as doxorubicine hydrochloride (DOX), du...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/704A61P35/00G01N21/33
Inventor 史向阳吴一伦王世革
Owner DONGHUA UNIV
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