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

Inactive Publication Date: 2014-11-26
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the absence of related reports in the prior art, a kind of Oridonium fruticosa has been developed with the advantages of good curative effect, good biocompatibility, high bioavailability, stable system, suitable for large-scale industrial production, and low cost. The albumin nanoparticle mediated by galactose and its preparation method are very difficult, requiring creative work, a large number of experiments and condition screening

Method used

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  • Galactose-mediated oridonin albumin nanoparticle and preparation method thereof
  • Galactose-mediated oridonin albumin nanoparticle and preparation method thereof
  • Galactose-mediated oridonin albumin nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

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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Abstract

The invention discloses a galactose-mediated oridonin albumin nanoparticle, which is prepared from the raw material and auxiliary materials, wherein the raw material is oridonin; the auxiliary materials consist of galactosylation albumin, crosslinking agent, cryoprotectant and water; the mass ratio of the use amount of the raw material and the auxiliary materials is as follows: by 10ml of nanoparticle preparation, the oridonin is 2.0-40.0mg, the galactosylation albumin is 50.0-400.0mg, the crosslinking agent is 0.4-8.4mg, the cryoprotectant is 0 or 0.1-0.5g, and the balance is water. The galactose-mediated oridonin albumin nanoparticle disclosed by the invention has a good biocompatibility. After the galactose-mediated oridonin albumin nanoparticle is made into injection-purpose nanometer solution, the bioavailability of the medicine is favorably increased, the medicine administration dose is reduced, the toxic and side effect is lowered, and the purpose on changing the in-vivo distribution of the medicine, prolonging the medicine acting time and improving the bioavailability can be achieved. The preparation method is simple and easy to realize and is suitable for large-scale production.

Description

Technical field [0001] The invention relates to a galactose-mediated oridonin albumin nanoparticle and a preparation method thereof. Background technique [0002] Liver cancer is one of the most common malignant tumors in the world, and its incidence and mortality are on the rise. According to statistics, there are approximately 6.35 million new malignant tumors each year, of which 300,000 are primary liver cancer, accounting for 4.7%. Both mainland China and Taiwan are areas with a high incidence of liver cancer. The annual incidence of liver cancer exceeds 130,000, accounting for 43.7% of the world's annual deaths from liver cancer. Therefore, it has become more urgent to find efficient methods to treat liver cancer. The current clinical treatments are generally surgery, radiotherapy, and chemotherapy. However, due to the insidious onset, high degree of malignancy, and rapid development of liver cancer, patients are often not aware of the disease at the early stage of illness...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/352A61K47/42A61P35/00
Inventor 张典瑞李彩云郭和坚郑丹丹郝蕾蕾刘光璞
Owner SHANDONG UNIV
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