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Glycyrrhetinic acid mediated curcumin long-circulating nanostructured lipid carrier and preparation method thereof

A nano-lipid carrier, glycyrrhetic acid technology, applied in the field of medicine, can solve the problems of cytotoxicity, low drug solubility, easy drug leakage, etc., and achieve the effects of increasing hydrophilicity, prolonging circulation time, and reducing phagocytosis.

Inactive Publication Date: 2015-06-10
沈阳医学院附属中心医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the research on liposome is relatively extensive. Liposome has the characteristics of good sustained release, targeting and biocompatibility in vivo, but liposome is unstable in vivo and in vitro, and the drug is easy to leak during storage; Toxic substances such as residual monomers, organic solvents, and polymer initiators will exist in the preparation process of nano-particles, and the biodegradable polymer materials used often produce cytotoxicity after phagocytosis and degradation; microemulsions have poor physical stability, The low solubility of the drug in the oil phase has limited its wide development and application

Method used

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  • Glycyrrhetinic acid mediated curcumin long-circulating nanostructured lipid carrier and preparation method thereof
  • Glycyrrhetinic acid mediated curcumin long-circulating nanostructured lipid carrier and preparation method thereof
  • Glycyrrhetinic acid mediated curcumin long-circulating nanostructured lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Glycyrrhetinic acid-phospholipid derivatives (GA-PEG 2000 -DSPE) synthesis:

[0040] Dissolve GA, DCC, and NHS in 10 mL of dehydrated dichloromethane, in which GA is 1.5 mmol, and the molar ratio of the three is 1.5:1.2:1.2, and the reaction is activated at room temperature for 3 h. Another 1mmol DSPE-PEG 2000 -NH 2 Dissolve in 5mL of dichloromethane solution, add dropwise to the above activator, and react for 48h at room temperature under the protection of nitrogen. Remove the reaction by-products by filtration, extract with glacial ether, and remove the unreacted GA in the supernatant. The precipitated substance is the target product. After reconstitution in DMF, put it into a dialysis bag for dialysis for 72 hours, and freeze-dry to obtain the product. Process route see figure 1 .

[0041] FTIR characterization: Bruker vector 22 infrared spectrometer was used to determine the reactants GA and DSPE-PEG respectively 2000 -NH 2 and the polymerization product DSPE...

Embodiment 2

[0046] (1), preparation of curcumin nano-lipid carrier (Cur-NLC):

[0047] raw material:

[0048]

[0049]

[0050] Weigh the prescribed amount of glyceryl monostearate, caprylic acid / capric triglyceride, soybean lecithin for injection and curcumin in a water bath and heat to 75°C, add 5ml of absolute ethanol to dissolve it, and remove the absolute ethanol by rotary evaporation to obtain Mix the molten phase evenly as the oil phase; weigh the prescribed amount of Polyoxyethylene 40 Strearate, add water for injection, stir it evenly with ultrasonic waves, and heat it in a water bath to 75°C as the water phase; at 3000r min -1 Add the water phase dropwise to the oil phase at the same temperature under magnetic stirring, and the drop rate is controlled at 10mL min -1 Stir at a constant temperature for 5 minutes to prepare colostrum, redisperse the colostrum with an ultrasonic cell pulverizer while it is hot, ultrasonic power 400W, ultrasonic 1s, interval 1s, time 5min, fil...

Embodiment 3

[0074] In vitro cytological evaluation of glycyrrhetinic acid-mediated long-circulating nanolipid carriers of curcumin:

[0075] Reagents and materials:

[0076]

[0077] Preparation of culture medium:

[0078] Phosphate buffered saline (PBS): Weigh 1.44 g of disodium hydrogen phosphate, 0.24 g of potassium dihydrogen phosphate, 8.0 g of sodium chloride, and 0.2 g of potassium chloride, dissolve them in 700 mL of double distilled water, mix and stir evenly. Use 1mol L -1 HCl to adjust the pH to 7.4, distilled water to 1000mL, and the concentration is 0.01mol L -1 Phosphate buffer (pH 7.4). Autoclave for 30 minutes, aliquot and store at 4°C for later use.

[0079] DMEM culture solution: Take 10.4g of DMEM dry powder, dissolve it in a small amount of double distilled water, add 3.7g of sodium bicarbonate, 2.0g of HEPES, 100units / mL penicillin, 100units / mL streptomycin, mix and stir to dissolve, and distill the volume to 1000mL. Use 1mol L -1 The pH was adjusted to 7.0 ...

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Abstract

The invention provides a glycyrrhetinic acid mediated curcumin long-circulating nanostructured lipid carrier and a preparation method thereof. The nanostructured lipid carrier is prepared from curcumin, glyceryl monostearate, caprylic / capric triglyceride, a glycyrrhetinic acid-phospholipid derivative, injection soybean lecithin and Polyoxyethylene 40 Strearate. The preparation method includes: firstly conducting water bath heating on lipid and curcumin to 75DEG C, adding anhydrous ethanol to conduct dissolution, performing rotary evaporation to eliminate anhydrous ethanol to serve as the oil phase; adding water for injection into the Polyoxyethylene 40 Strearate, carrying out ultrasonic stirring evenly, then conducting water bath heating to 75+ / - 2DEG C to serve as the water phase; under magnetic stirring, dripping the water phase into the oil phase at the same temperature, carrying out constant temperature stirring for 5min to obtain colostrum, conducting ultrasonic dispersion by an ultrasonic cell crusher for 5min while hot, performing sieving by a 0.22 micrometer microporous filtration membrane, and conducting ice-water bath cooling and curing at room temperature, thus obtaining the glycyrrhetinic acid mediated curcumin long-circulating nanostructured lipid carrier dispersion liquid.

Description

technical field [0001] The invention belongs to the field of medicine, and particularly provides a glycyrrhetinic acid-mediated curcumin long-circulation nano-lipid carrier and a preparation method thereof. Background technique [0002] Curcumin (Cur) is extracted from the dry rhizome of turmeric (Curcuma longa L.), which is a polyphenolic compound and the main active ingredient in curcumin. As a coloring agent and pigment dye, it is widely used in the food field. In recent years, a number of studies have shown that curcumin has diverse biological activities and pharmacological effects, and can be used as anti-inflammatory drugs, antioxidants, anti-tumor drugs, liver-protecting drugs, etc., with low toxicity and good potential for clinical application. However, curcumin has low solubility in water and poor stability, resulting in poor bioavailability in vivo, and the drug is quickly metabolized and inactivated in the gastrointestinal tract, and increasing the dosage and adm...

Claims

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Application Information

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IPC IPC(8): A61K47/24A61K47/28A61K47/34A61K31/12A61P29/00A61P39/06A61P35/00A61P1/16A61K47/54
Inventor 李丹
Owner 沈阳医学院附属中心医院
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