Polyethylene glycol-lactobionic acid modified aminated hectorite nano particle as well as preparation method and application thereof
A technology of amide lithium saponite and polyethylene glycol is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, organic active ingredients, etc. Material stability, improved drug release properties, and improved affinity effects
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Embodiment 1
[0055] (1) Dissolve 32 mg of lactobionic acid (LA) (purchased from Sinopharm Chemical Reagent Co., Ltd.) with 20 mL of pH=6 buffer solution, add 1 mL of 1-ethyl-(3-dimethyl Aminopropyl) carbodiimide (EDC) was stirred for 0.5h, then 1mL of 10.1mg / mL N-hydroxysuccinimide (NHS) was added for activation for 3h, and 2mL of 44.20mg / mL was added slowly NH 2 -PEG-COOH (MW=2000) solution, after 72 hours of reaction, the reaction product was dialyzed in phosphate buffer with a 1000 dialysis bag for 24 hours, then dialyzed with distilled water for 48 hours, and finally the purified product was freeze-dried to obtain lactobionic acid modification Polyethylene glycol solid product (LA-PEG-COOH);
[0056] (2) Take a certain quality of LAP powder and disperse it in a certain volume of ultrapure water to prepare a dispersion with a concentration of 10 mg / mL, take 40 μL of (3-aminopropyl) dimethylethoxysilane and shake it while dripping Add 10mL LAP dispersion liquid, then place in 50 ℃ wate...
Embodiment 2
[0059] Prepare a DOX aqueous solution with a concentration of 1 mg / mL, add 2 mL of DOX aqueous solution to 2 mL of LM-PEG-LA aqueous solution with a concentration of 3 mg / mL, and react with magnetic stirring for 24 hours under the condition of avoiding light. After the reaction, the solution was transferred to a 15mL centrifuge tube, centrifuged (10min) at a rotational speed of 5000rpm, and the obtained precipitate was washed 3 times with deionized water to obtain drug-loaded nanoparticles LM-PEG-LA / DOX.
Embodiment 3
[0061]Prepare LM-PEG-LA / DOX with pH = 7.4 and pH = 5.4 buffers respectively to form a solution with a DOX concentration of 1 mg / mL, take 1 mL of the above solution into a dialysis bag, and place it in 9 mL of the same pH 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 1mL of the liquid outside the dialysis bag each time, and then add 1mL of the corresponding buffer solution to the outside of the dialysis bag. The absorbance value at 480nm of the dialysate taken out was measured, and the release curve of DOX released from LM-PEG-LA / DOX under different pH conditions in vitro was calculated. ( Figure 4 )
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