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Folic acid modified ABT-737 loaded mesoporous silica nanoparticles, and preparation method thereof

A technology of ABT-737 and mesoporous silica, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve low bioavailability, poor solubility of ABT-737, etc. problem, to achieve good killing effect, improve bioavailability, and obvious effect

Inactive Publication Date: 2020-04-21
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to provide a folic acid-modified ABT-737-loaded mesoporous silica nanoparticles and a preparation method thereof to solve the technical problems of poor solubility and low bioavailability of ABT-737

Method used

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  • Folic acid modified ABT-737 loaded mesoporous silica nanoparticles, and preparation method thereof
  • Folic acid modified ABT-737 loaded mesoporous silica nanoparticles, and preparation method thereof
  • Folic acid modified ABT-737 loaded mesoporous silica nanoparticles, and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0028] The preparation method of carrying ABT-737 mesoporous silica nanoparticles, comprising:

[0029] (1) Preparation of FA-MSN: 200 mg of folic acid was dissolved in 12 mL of dimethyl sulfoxide, reacted with 180 mg of NHS (N-hydroxysuccinimide) and 100 mg of DCC (dicyclohexylcarbodiimide) at room temperature for 10 h , centrifuged to collect the precipitate, washed and freeze-dried. The activated folic acid was dissolved in 5 mL of dimethyl sulfoxide, and 350 mg of NH 2 -PEG-NH 2 , stirred at room temperature, reacted for 22 hours, centrifuged, and freeze-dried to obtain functionalized folic acid NH 2 -PEG-FA.

[0030] Another 50mg of carboxyl-modified silica mesoporous nanoparticles (MSN / COOH) with a particle size of about 180nm was dispersed in 2-(N-morpholine)ethanesulfonic acid buffer (0.1M, pH=5), and 70mg of EDAC (1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride) reacted with 35mg of NHS for 1.5h, centrifuged, and added 45mg of NHS 2 -PEG-FA, stirred ...

Embodiment 2

[0046] H22 in vitro cytotoxicity test

[0047] Take the H22 in the logarithmic growth phase, collect the suspended cell liquid, adjust the cell concentration, and inoculate in a 96-well plate at a seeding density of 1×10 4 / well; after the 96-well plate was incubated in a constant temperature incubator for 24 hours, the original drug (ABT-737) and the ABT-737@FA-MSN group were treated with different concentrations (1, 5, 25, 125, 625 μg / mL, (based on the weight of ABT) was added, and three replicate wells were set up for each concentration to calculate the average value; 0.2 mL of sterilized PBS buffer solution was added to the outermost well of the 96-well plate to resist the edge effect; the 96-well plate was respectively Continue to incubate for 24 and 48 hours, take a 96-well plate according to the time point, add 20 μL / well of 5 mg / ml MTT solution, and continue to incubate at 37°C for 4 hours; carefully suck out the liquid in the well, then add DMSO, 100 μL / well; The ins...

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Abstract

The invention relates to the field of pharmaceutical preparations, and discloses folic acid modified ABT-737 loaded mesoporous silica nanoparticles. The preparation method comprises the following steps: adding folic acid modified mesoporous silica nanoparticles into an ABT-737 chloroform solution, stirring, carrying out centrifugation, and taking the precipitate, wherein the obtained folic acid modified ABT-737-loaded mesoporous silica nanoparticles have the particle size of 180-220 nm, the Zeta potential of 20-25 mV, the encapsulation efficiency of 75-80% and the drug loading capacity of 7-12%. According to the invention, the prepared ABT-737@FA-MSN has obvious slow release effect and long-acting tumor inhibition effect, and has good application prospect as an ABT-737 tumor targeted drugdelivery system.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to folic acid-modified ABT-737-loaded mesoporous silica nanoparticles and a preparation method thereof. Background technique [0002] ABT-737 is an analogue of ABT-263, which has been reported in preclinical and clinical trials of tumors, and is a targeted drug with clinical prospects. At present, it is known that ABT-737 has a molecular mechanism of inducing protective cell autophagy, which can kill tumor cells. However, its poor solubility and low bioavailability limit its clinical application. [0003] Mesoporous silica nanoparticles (MSNs) are a new type of inorganic mesoporous material with large specific surface area and pore volume, highly ordered mesoporous structure, and can achieve sustained and long-term release of drugs; at the same time, There are a large number of easily modified silanol groups on its inner and outer surfaces, which has the advantages of ea...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/04A61K47/22A61K31/495A61P35/00
CPCA61K9/5115A61K9/5123A61K31/495A61P35/00
Inventor 刘敏臣冯怡张继全
Owner SHANGHAI UNIV OF T C M
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