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Astaxanthin long-acting nano preparation prepared through micelle template method and preparation method for astaxanthin long-acting nano preparation

A nano-formulation, astaxanthin technology, applied in the directions of antitoxin, capsule delivery, micro-capsules, etc., can solve the problem of less research on the hepatoprotective effect of astaxanthin and its preparations, and achieve excellent liver protection effect and dispersion. Good property and the effect of improving solubility

Active Publication Date: 2021-08-13
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, there are few reports on astaxanthin long-acting preparations, and there are few studies on the hepatoprotective effect of astaxanthin and its preparations

Method used

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  • Astaxanthin long-acting nano preparation prepared through micelle template method and preparation method for astaxanthin long-acting nano preparation
  • Astaxanthin long-acting nano preparation prepared through micelle template method and preparation method for astaxanthin long-acting nano preparation
  • Astaxanthin long-acting nano preparation prepared through micelle template method and preparation method for astaxanthin long-acting nano preparation

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Effect test

Embodiment 1

[0033] The preparation of embodiment 1 astaxanthin nano-preparation

[0034] (1) Accurately weigh 5mg of astaxanthin and dissolve it in 0.5mL of dichloromethane, and make it homogeneous by ultrasonication for 10min. Accurately weigh 15 mg of phospholipids and 10 mg of sodium cholate and dissolve them in a mixed solvent of 0.5 mL of methanol, and ultrasonicate for 10 min to make them uniform. Accurately weigh 50 mg of PLGA and dissolve it in 2 mL of dichloromethane, and ultrasonicate for 10 min to make it uniform. Disperse the astaxanthin solution into the mixed solution of phospholipid and sodium cholate, and disperse it fully by ultrasonication for 10 minutes, then disperse this solution in the PLGA solution, and disperse it fully by ultrasonication for 10 minutes to obtain an organic phase with a total volume of 3 mL. Disperse the organic phase in 6 mL of 4% PVA403 aqueous solution to emulsify it, then disperse the emulsion in 10 mL of 0.5% PVA 403 aqueous solution, stir ov...

Embodiment 2

[0036] The preparation of embodiment 2 astaxanthin nano-preparations

[0037] (1) Accurately weigh 5 mg of astaxanthin and dissolve it in 2 mL of dichloromethane, and ultrasonicate for 10 min to make it uniform. Accurately weigh 35 mg of phospholipids and 25 mg of sodium cholate and dissolve them in a mixed solvent of 1 mL of dichloromethane and 3 mL of methanol, and ultrasonicate for 10 min to make them uniform. Accurately weigh 250 mg of PLGA and dissolve it in 4 mL of dichloromethane, and ultrasonicate for 10 min to make it uniform. Disperse the astaxanthin solution into the mixed solution of phospholipid and sodium cholate, and disperse it fully by ultrasonication for 10 minutes, then disperse this solution in the PLGA solution, and disperse it fully by ultrasonication for 10 minutes to obtain an organic phase with a total volume of 10 mL. Disperse the organic phase in 15 mL of 4% PVA403 aqueous solution to emulsify it, then disperse the emulsion in 50 mL of 1% PVA 403 aq...

Embodiment 3

[0039] The preparation of embodiment 3 astaxanthin nano-preparations

[0040] (1) Accurately weigh 10 mg of astaxanthin and dissolve it in 2 mL of dichloromethane, and ultrasonicate for 10 min to make it uniform. Accurately weigh 70 mg of phospholipids and 50 mg of sodium cholate and dissolve in a mixed solvent of 1 mL of dichloromethane and 3 mL of methanol, and ultrasonicate for 10 min to make them uniform. Accurately weigh 400mg of PLGA and dissolve it in 4mL of dichloromethane, and ultrasonicate for 10min to make it uniform. Disperse the astaxanthin solution into the mixed solution of phospholipid and sodium cholate, and disperse it fully by ultrasonication for 10 minutes, then disperse this solution in the PLGA solution, and disperse it fully by ultrasonication for 10 minutes to obtain an organic phase with a total volume of 10 mL. Disperse the organic phase in 15 mL of 4% PVA 403 aqueous solution to emulsify it, then disperse the emulsion in 40 mL of 1% PVA 403 aqueous ...

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Abstract

The invention discloses an astaxanthin long-acting nano preparation prepared through a micelle template method and a preparation method for the astaxanthin long-acting nano preparation, and relates to the field of nano pharmaceutical preparations. Phospholipid and sodium cholate are used as micelle templates, and a solubilizing and synergy carrier is provided for insoluble compound astaxanthin; the novel astaxanthin micelle-loaded PLGA nano preparation is prepared from astaxanthin, phospholipid, sodium cholate and PLGA in a mass ratio of 1: (3-7): (2-5): (10-50) through an emulsion solvent evaporation method by taking a polylactic acid-glycolic acid copolymer as a long-acting carrier, wherein the ratio of a total organic phase to a total water phase is 1: (5-25). According to the preparation, on the premise that the solubility of the astaxanthin is remarkably improved, the long-acting liver protection effect of the astaxanthin is achieved at the same time. The process is simple, the micelle template is innovatively applied to preparation of the insoluble medicine long-acting preparation, and has a good application prospect.

Description

Technical field [0001] The present invention relates to the field of nanomedicine preparations, in particular to long-acting nanopreparations of astaxanthin, a poorly soluble active ingredient, and a preparation method thereof. Background technique [0002] Astaxanthin, 3,3'-dihydroxy-4,4'-diketo-β,β'-carotene, is a ketone non-vitamin A source carotenoid, a reddish-brown terpene Ethylenically unsaturated compounds. As a chain-breaking antioxidant, astaxanthin can not only quench singlet oxygen and directly scavenge oxygen free radicals, but also block the chain reaction of fatty acids and has extremely strong antioxidant activity (see: Zuluaga, M. ,V.Gueguen,D.Letourneur,et al.,Astaxanthin-antioxidant impact on excessive Reactive Oxygen Species generation induced byischemia and reperfusion injury[J].Chemico-Biological Interactions,2018.279:145-158). Astaxanthin is a natural pigment carotenoid approved by the U.S. Food and Drug Administration (FDA) and has various biologica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/107A61K31/122A61K47/24A61K47/28A61K47/34A61P1/16A61P39/06
CPCA61K9/5153A61K9/5192A61K9/1075A61K31/122A61K47/24A61K47/28A61P1/16A61P39/06
Inventor 朱源廖有武李双顾正清薛媛媛彭后平
Owner JIANGSU UNIV
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