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

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

Inactive Publication Date: 2014-08-13
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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

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

Embodiment 2

[0058] 5 mL of LAP ultrapure aqueous solution with a mass concentration of 2 mg / mL and 2 mg / mL and DOX ultrapure aqueous solution were mixed in equal volumes, and magnetically stirred at room temperature for 24 hours, and the reaction was completed. The suspension obtained by the reaction was centrifuged (8000 rpm, 5 min), washed (washed twice with distilled water), separated and precipitated to obtain LAP-DOX nanoparticles. Using a Lambda25 UV-Vis spectrophotometer to measure the absorbance of the supernatant and the washing liquid mixture at 480nm, calculate the remaining DOX concentration in the supernatant according to the standard curve, and then draw the load 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 load DOX.

Embodiment 3

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

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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 nanoparticle-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 distinguish between cancerous tissue cells and healthy cells, resulting in great damage to the body caused by chemotherapy. First of all, the distribution of antineoplastic drugs to the tissue cells of the whole body with no difference or small difference along with the blood circulation will lead to systemic toxic and side effects, and greatly limit the maximum dose allowed for administration. Secondly, the wide distribution of drugs in different tissue cells requires a relatively large dosage, which will not only cause waste of drugs, but also bring about toxic and side effects. In addition, some small-molecu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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