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Anthocyanin nanoparticles based on marine polysaccharide carrier and its preparation method and application in targeted delivery

A nanotechnology of marine polysaccharides and glycosides, applied in the field of nanometers, can solve the problems of loss of functional active ingredients and poor stability of lingonberry anthocyanins, etc., and achieve improved retention rate, good photostability, biocompatibility, and strong stability Effect

Active Publication Date: 2022-04-01
DALIAN POLYTECHNIC UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention provides anthocyanin nanoparticles based on marine polysaccharide carrier and its preparation and application in fluorescent tracing and colon targeted delivery, so as to solve the poor stability of bilberry anthocyanins in the prior art and the vulnerability of functional active ingredients to loss , and the application of anthocyanin nanoparticles pretreatment in protecting lipopolysaccharide (LPS)-mediated apoptosis of RAW 264.7 macrophages and alleviating colonic inflammatory injury induced by dextran sodium sulfate (DSS)

Method used

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  • Anthocyanin nanoparticles based on marine polysaccharide carrier and its preparation method and application in targeted delivery
  • Anthocyanin nanoparticles based on marine polysaccharide carrier and its preparation method and application in targeted delivery
  • Anthocyanin nanoparticles based on marine polysaccharide carrier and its preparation method and application in targeted delivery

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preparation example Construction

[0039] 1. Preparation of anthocyanin nanoparticles

[0040] S1. Dissolve 5-30 mg of sodium alginate in pH 4.75-6 phosphate buffered saline, add 35-70 mg of EDC and 25-50 mg of HOBt in sequence, and perform magnetic stirring at room temperature at a stirring speed of 500-800 r / min After 60-80 minutes, add 1-5 mg of the food-derived fluorescent nanoparticles, perform magnetic stirring at room temperature at a stirring speed of 500-800 r / min for 24-30 hours, then dialyze with deionized water for 24-72 hours and freeze-dry , to obtain the fluorescent-alginic acid complex;

[0041] S2. Hyaluronic acid can be further conjugated to the backbone of alginate through esterification, using diisopropylcarbodiimide (DIC) as a coupling agent and dimethylaminopyridine (DMAP) as a catalyst. Eliminate the water produced during the chemical reaction. Add 40-60 mg of the fluorescent-alginic acid complex to 4-6 ml of a mixture of DMF and DCM with a volume ratio of 1:1-1.5, add 8-16 mg of DIC an...

Embodiment 1

[0047] Embodiment 1: Preparation of anthocyanin nanoparticles

[0048] S1: Marine polysaccharide sodium alginate (30 mg) was dissolved in phosphate buffered saline (pH 4.75), and EDC (35 mg) and HOBt (25 mg) were added in sequence. After stirring at room temperature for 1 h, food-derived fluorescent nanoparticles (5 mg) were added and stirred for 24 h. Afterwards, the product was dialyzed against deionized water for 24 hours and freeze-dried to obtain a fluorescent-alginic acid complex.

[0049] S2: 40 mg of the fluorescent-alginic acid complex prepared in step S1 was added to 4 ml of a mixture of dimethylformamide DMF and DCM mixed at a volume ratio of 1:1. Subsequently, DIC (8.1 mg) and DMAP (25 mg) were added thereto. The reaction mixture was allowed to stir gently at room temperature for 1 h to activate the carboxyl group of alginic acid.

[0050] S3. Slowly add 1 mg anthocyanin and 8 mg hyaluronic acid to the mixture prepared in S2, and the reaction is further carried ...

Embodiment 2

[0052] Embodiment 2: Preparation of food-borne fluorescent nanoparticles

[0053] Cut 1kg of pork belly evenly into 1×1×1cm 3 Bake the small pieces at 280°C for 30 minutes, soak the baked meat in 3L of absolute ethanol, and keep stirring for 12 hours, select the soluble part filtered by three layers of filter paper and use a rotary evaporator to remove the ethanol , then redissolve the treated soluble part with chloroform: water=3:1 configuration solution, add chloroform to extract and degrease repeatedly until the oil phase is clear, and select the clear water phase part to pass through D101 macroporous adsorption resin column For chromatography, the fluorescent part was pre-cooled at -80°C for 2h, and then freeze-dried at -50°C under a vacuum of 40Pa for 48h.

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Abstract

The invention provides an anthocyanin nanoparticle based on a marine polysaccharide carrier. The marine polysaccharide, food-derived fluorescent nanoparticle, and hyaluronic acid are used as a composite carrier to combine with anthocyanin. The preparation method is: S1, dissolving sodium alginate in phosphoric acid In salt-buffered saline, add EDC and HOBt and food-derived fluorescent nanoparticles in sequence to obtain a fluorescent-alginic acid complex; S2, adding the fluorescent-alginic acid complex to a mixture of DMF and DCM, then adding DIC and DMAP; S3, removing the solvent after adding anthocyanin and the hyaluronic acid; S4, removing unreacted small molecules, and freeze-drying. The present invention can improve the stability of anthocyanin, control the slow release of anthocyanin, has the characteristics of fluorescent tracer, can be used as a fluorescent marker for in vivo imaging of animal tissues and organs, and can also be targeted for delivery to the colon of animals to alleviate the symptoms induced by DSS. Inflammatory damage to the colon.

Description

technical field [0001] The present invention relates to the field of nanotechnology, more specifically, to a marine polysaccharide carrier-based anthocyanin nanoparticle and its preparation and application in fluorescent tracing and colon-targeted delivery. Background technique [0002] Anthocyanin is a bioactive compound belonging to flavonoids, which exists in human nutrition through plant foods, and the fruit components of lingonberry are rich in anthocyanins. It has strong antioxidant properties and regular consumption has health benefits. However, environmental conditions such as pH and temperature have a great influence on the color stability and properties of anthocyanins. The anthocyanins prepared by the prior art have poor stability, especially the sodium alginate microspheres prepared by the emulsification method, the residence time in the upper digestive tract is insufficient, resulting in low bioavailability, which needs to be improved. [0003] Nanotechnology,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/352A61K47/36A61K47/46A61K49/00A61P39/06B82Y20/00B82Y30/00B82Y40/00
CPCA61K31/352A61K9/19A61K47/36A61K47/46B82Y20/00B82Y30/00B82Y40/00A61P39/06A61K49/0054A61K49/0093Y02A50/30A61P1/00A61K9/5161A61K31/728A61K47/6939
Inventor 谭明乾赵雪张雪迪铁珊珊曹纪鋆李运
Owner DALIAN POLYTECHNIC UNIVERSITY
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