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Preparation of sericine bound paclitaxel nano-drug sericin-PBLG-PTX-Nile-red and application thereof in tumor tracing and treatment

A technology of sericin and nano-drugs, which is applied in the field of biomedical materials, can solve problems such as sericin-paclitaxel nano-drug patent reports that have not yet been reported, and achieve excellent biocompatibility, tumor targeting optimization, and cheap raw materials Effect

Inactive Publication Date: 2017-07-21
胡彦锋 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there has been no patent report on sericin-paclitaxel nanomedicine

Method used

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  • Preparation of sericine bound paclitaxel nano-drug sericin-PBLG-PTX-Nile-red and application thereof in tumor tracing and treatment
  • Preparation of sericine bound paclitaxel nano-drug sericin-PBLG-PTX-Nile-red and application thereof in tumor tracing and treatment
  • Preparation of sericine bound paclitaxel nano-drug sericin-PBLG-PTX-Nile-red and application thereof in tumor tracing and treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] (1) Add the shredded silk cocoons into 0.02mol / L sodium carbonate solution and boil for 60min, filter to remove insoluble silk fibroin and other insoluble matter, put the filtrate into a cellulose dialysis bag with a molecular weight cut-off of 8000-14000Da, pure Dialysis in water for three days to remove ion salts, freeze-drying to obtain sericin.

[0044] (2) Under the protection of argon, dissolve the protected 2g of L-glutamic acid-r-benzyl ester in tetrahydrofuran dehydrated by NaH, add 1.4g of trimeric phosgene, react at 55°C for 1h, and cool to At room temperature, tetrahydrofuran was distilled off under reduced pressure, and the obtained oil soluble matter was dissolved in 100 mL of ethyl acetate, washed with saturated aqueous sodium bicarbonate solution, the organic phase was separated, dried with anhydrous magnesium sulfate overnight, filtered to remove the desiccant, and decompressed The solvent was distilled off to obtain benzyl glutamic acid anhydride.

[...

Embodiment 2

[0048] (1) Dissolve 10 mg of the sericin-polybenzyl glutamate polymer in Example 1 (the mass ratio of sericin to benzyl glutamate anhydride in the ring is 1:1) in 1 mL of DMSO, and stir 1h, then drop it into 4mL of deionized solution under magnetic stirring, put the mixed solution into a dialysis bag with a molecular weight cut-off of 3500, dialyze with deionized water at 25°C for 24h, dilute to 10mL, pass through a 0.45μm needle filtered through a filter and left for detection. The preparation method of Nile Red-loaded micelles (that is, Nile Red-labeled Sericine-PBLG nanomicelles) is similar, except that 5 μg of Nile Red is added while dissolving the sericin-polybenzyl glutamate polymer.

[0049] (2) Digest and resuspend gastric cancer cells (AGS) and adjust the cell concentration to 2×10 4 / L, the volume of culture solution added to each well of a 96-well culture plate was 200 μL. After the cells adhered to the wall, Sericine-PBLG carriers (ie, sericin carriers) with diff...

Embodiment 3

[0054] (1) 10 mg of the sericin-polybenzyl glutamate polymer in Example 1 (the mass ratio of sericin to benzyl glutamate anhydride in the loop is 1:1), 5 μg of Nile Red, and 1 mg of paclitaxel Dissolve in 1 mL of DMSO, stir for 1 h, then drop it into 4 mL of deionized solution under magnetic stirring, put the mixed solution into a dialysis bag with a molecular weight cut-off of 3500, and dialyze it with deionized water for 24 h at 25°C to prepare Sericin-bound paclitaxel nanomedicine was obtained. It was diluted to 10mL and filtered through a 0.45μm needle filter to obtain Sericin-PBLG-PTX-Nile-red micelles, which were left for detection.

[0055] (2) Culture gastric cancer cells (AGS) in a confocal dish to a density of 70-80%, add Sericin-PBLG-PTX-Nile-red micelles, and use a confocal microscope or an inverted microscope to observe the accumulation of micelles in the cells ability; results such as Figure 4 shown.

[0056] (3) Cultivate gastric cancer cells (AGS) to a dens...

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Abstract

The invention discloses preparation of a sericine bound paclitaxel nano-drug sericin-PBLG-PTX-Nile-red and application thereof in tumor tracing and treatment. According to the invention, sericine is adopted as the hydrophilic segment, hydrophobic polypeptide is taken as the hydrophobic segment, and alpha-amino acid-N-carboxyanhydride (NCA) ring-opening reaction is carried out to prepare an amphiphilic sericine polymer. At the same time, amphiphilic sericine is taken as the carrier to load a non-water soluble antitumor drug paclitaxel and a Nile red fluorescent agent by means of hydrophobic interaction, thus obtaining the sericin-PBLG-PTX-Nile-red. The sericin-PBLG-PTX-Nile-red is expected to be applied in the tumor field as a novel controlled release drug with excellent performance and efficient antitumor activity.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and in particular relates to the preparation of a sericin-binding paclitaxel nano-medicine (Sericin-PBLG-PTX-Nile-red) and its application in tumor tracing and treatment. Background technique [0002] China is a country with a large population in the world, and the total number of malignant tumors accounts for a considerable proportion of the global population, which seriously affects the health of our population. Traditional treatment options for malignant tumors currently mainly include surgical resection, chemotherapy, and radiotherapy. However, the prognosis of most malignant tumors is still poor and the mortality rate is high. Because it is difficult for traditional chemotherapy drugs to reach an effective concentration to control the growth of cancer cells in locally advanced tumor lesions, leading to adverse consequences such as tumor recurrence and metastasis, traditional treatment has...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/42A61K47/34A61K31/337A61P35/00A61K49/00
CPCA61K47/34A61K47/42A61K49/0028A61K49/0056A61K49/0082A61K9/1075A61K31/337
Inventor 胡彦锋郭伟洪邓立志张黎明李国新
Owner 胡彦锋
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