Galactose-mediated oridonin albumin nanoparticle and preparation method thereof
A technology of albumin nanoparticles and oridonin A, which is applied in the directions of medical preparations containing active ingredients, pharmaceutical formulas, powder delivery, etc., can solve problems such as difficulties in preparation methods, and achieves simple and feasible preparation methods and reduced size. Administering dosage, expanding the effect of clinical application
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Embodiment 1
[0038] Example 1: Preparation of galactose-mediated oridonin albumin nanoparticles
[0039] Proceed as follows:
[0040] Dissolve 0.12g lactobionic acid in distilled water containing 0.12g EDAC and 0.06g NHS, adjust the pH to 4.5 with TMEA, adjust the pH to 7 with NaOH solution after activation for 0.5h, then add 0.08g bovine serum albumin, 500r / min After stirring for 48 hours, the resulting solution was dialyzed in a dialysis bag for 2 days. The water was changed three times a day, and then freeze-dried (dilute the dialyzed solution into vials according to 2 mL / bottle, and quickly put it in an ultra-low temperature refrigerator at -80℃ Freeze for 24 hours, then take it out and quickly put it on the shelf of the freeze dryer whose temperature has dropped to -50°C, cover the vacuum cover, turn on the vacuum pump, freeze-dry for 48 hours, take it out) to obtain galactosylated albumin.
[0041] Weigh 6.0 mg of oridonin and add it to 1.5 ml of ethanol, and dissolve oridonin under ultras...
Embodiment 2
[0043] Example 2: Preparation of galactose-mediated oridonin albumin nanoparticles
[0044] Proceed as follows:
[0045] Dissolve 0.15g lactobionic acid in distilled water containing 0.15g EDAC and 0.75g NHS, adjust the pH to 4 with TMEA, adjust the pH to 7 with NaOH solution after activation for 0.5h, then add 0.1g bovine serum albumin, 500r / min After stirring for 48 hours, the obtained solution was dialyzed in a dialysis bag for 2 days, the water was changed three times a day, and then freeze-dried to obtain galactosylated albumin.
[0046] Weigh 6.0 mg of Rubescensine A into 2.0 ml of ethanol, and dissolve Rubescensine A under ultrasound. Dissolve 100.0 mg of galactosylated albumin in 10 ml of water for injection, adjust the pH to 9 with NaOH solution, add oridonin ethanol solution drop by drop, and drop at 0.75 ml / min under magnetic stirring at 600 rpm Add absolute ethanol until nano opalescence appears, then add 1.2 mg of glutaraldehyde for chemical cross-linking for 24 hours;...
Embodiment 3
[0047] Example 3: Preparation of galactose-mediated oridonin albumin nanoparticles
[0048] Proceed as follows:
[0049] Dissolve 0.12g lactobionic acid in distilled water containing 0.12g EDAC and 0.06g NHS, adjust the pH to 5 with TMEA, adjust the pH to 7 with NaOH solution after activation for 0.5h, then add 0.08g bovine serum albumin, 500r / min After stirring for 48 hours, the obtained solution was dialyzed in a dialysis bag for 2 days, the water was changed three times a day, and then freeze-dried to obtain galactosylated albumin.
[0050] Weigh 8.0 mg of oridonin and add it to 2.0 ml of ethanol, and dissolve oridonin under ultrasound. Dissolve 75.0mg of galactosylated albumin in 5ml of water for injection, adjust the pH to 9 with NaOH solution, add oridonin ethanol solution drop by drop, and drop by 0.75ml / min under magnetic stirring at 500rpm Add absolute ethanol until nano opalescence appears, and add 1.4 mg of glutaraldehyde for chemical cross-linking for 24 hours; after cr...
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