Nanocomposite with oxidative stress self-amplification function, preparation method and application
A nano-composite, amplifying function technology, applied in non-active ingredients medical preparations, active ingredients-containing medical preparations, drug combinations, etc., can solve the problem of reducing the efficiency of artemisinin to kill tumor cells, etc. High selectivity, good water solubility, and the effect of increasing oxidation state levels
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Embodiment 1
[0029] Example 1: Combining image 3 , to synthesize Tf-MSN@AB, the steps are as follows:
[0030] 1. Synthesis of polypeptide-transferrin complex (Pep-Tf).
[0031] Weigh 2 mg of Pep and dissolve it in 4 mL of N,N-dimethylformamide (DMF) solution. Add 5 mM N-hydroxysuccinimide and 1 mM N-ethyl-N'-(3-(dimethylaminopropyl) carbodiimide to the Pep solution, and sonicate for 10 min to activate the carboxyl group. After activation , add 4 mg Tf to the above solution and stir vigorously, make it react in the dark at room temperature for 24h. After the reaction, centrifuge (8500rpm, 10min), discard the organic solution, and rinse three times with DMF, and finally vacuum-dry to obtain Pep-Tf .
[0032] 2. Amino groups on the surface of mesoporous silicon (MSN-NH 2 ).
[0033]Dissolve 300mg of mesoporous silicon powder in 30mL of methanol, and ultrasonically assist the dissolution. After dissolution, 2 mL of N-[3-(trimethoxysilyl)propyl]ethylenediamine was added to the solution,...
Embodiment 2
[0039] Example 2: Characterization of Tf-MSN@AB.
[0040] The prepared Tf-MSN@AB was characterized by Fourier transform infrared spectrometer, the results are as follows Figure 4 As shown, MSN in the figure indicates the purchased mesoporous silicon nanoparticles; MSN-NH 2 represents the amino-modified mesoporous silicon nanoparticles prepared in step 2; MSN-alkyne represents the alkyne-modified mesoporous silicon obtained in step 3; Tf-MSN@AB represents the nanocomposite finally prepared in step 4, by As can be seen in the figure:
[0041] When the surface of mesoporous silicon is not modified, the infrared spectrum of MSN is at 3000-2800cm -1 The absorption peak of -C-H- appears at the place, and the absorption peak of -C-H- is modified by amination in MSN (MSN-NH 2 ) significantly decreased, when adding the alkynylated mesoporous silicon (MSN-alkyne) obtained after the reaction of propargyl bromide and triethylamine, MSN-alkyne was at 2123cm -1 A strong absorption peak...
Embodiment 3
[0047] Example 3: In vitro release experiment of artemisinin and butionine-sulfoximine.
[0048] This example is to explore the in vitro drug release behavior of Tf-MSN@AB prepared in Example 1 in response to cathepsin B under different pH environments. The specific method is:
[0049] The in vitro release profiles of ART and BSO from Tf-MSN@AB were measured by dialysis. Tf-MSN@AB was dissolved in different pH citrate buffers (pH 7.4 and pH 5.0) containing 10% fetal bovine serum (FBS). Different pH groups were further divided into two groups containing cathepsin B and not containing cathepsin B. The prepared solution was placed in a dialysis bag (Mn=30kDa, Millipore), and then the dialysis bag was put into citrate buffer containing the same pH value, and the buffer was stirred at 100 rpm at 37°C. Samples were taken at pre-set time points and replaced with the same volume of release medium.
[0050] Determination of drug release of artemisinin:
[0051] 500 μL of the sample...
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