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Naringenin nano lipid carrier and its preparation method and application

A nano-lipid carrier, naringenin technology, applied in the field of medicine, can solve the problems of low drug loading, drug leakage, etc., achieve the effect of simple preparation method, easy control and operation, and improved dissolution and absorption characteristics

Active Publication Date: 2020-12-18
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

SLN is only composed of solid lipids, a single lipid component forms an orderly and compact lattice, and the drug loading capacity is low; during storage, solid lipids are prone to transformation from α crystal form to β crystal form, resulting in drug leakage

Method used

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  • Naringenin nano lipid carrier and its preparation method and application
  • Naringenin nano lipid carrier and its preparation method and application
  • Naringenin nano lipid carrier and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Embodiment 1, the preparation of naringenin nano lipid carrier (method 1)

[0066] Accurately weigh 0.021g of naringenin, 0.060g of soybean lecithin, 0.020g of medium-chain triglycerides, and 0.004g of glyceryl trilaurate, add 3.3mL of chloroform and 1.7mL of methanol, fully dissolve, and rotate under reduced pressure in a water bath at 37°C The solvent was removed by evaporation until a uniform lipid film formed on the sides of the eggplant-shaped flask. Add 3 mL of 0.01M phosphate buffer (pH=7.4) containing 230 mg of polyoxyethylene castor oil, and sonicate for 15 min (80% of full amplitude) in an ice bath to obtain the naringenin nano-lipid carrier 1 (NGN- NLC1).

Embodiment 2

[0067] Embodiment 2, the preparation of naringenin nano lipid carrier (method 2)

[0068] Accurately weigh 0.025g naringenin, 0.040g soybean lecithin, 0.020g stearic acid, 0.020g glyceryl monostearate, 0.020g oleic acid, add 2mL ethanol, fully dissolve, add 3% Pluronic F68 In 20mL of 0.01M phosphate buffer (pH=7.4), form an emulsion at 75°C until the concentration of naringenin is 8.3mg·mL -1 . The naringenin nano-lipid carrier 2 (NGN-NLC2) of the present invention was obtained by depositing and solidifying in an ice bath for 1 h.

Embodiment 3

[0069] Embodiment 3, the application of naringenin nano lipid carrier

[0070] 1. Quality evaluation of naringenin nano-lipid carrier

[0071] Particle size measurement: get an appropriate amount of NGN-NLC1 in Example 1 of the present invention, adopt a Malvern Zeta potentiometer to measure its particle size, and record the particle size as (120.8 ± 1.9) nm; get an appropriate amount of NGN-NLC2 in Example 2 of the present invention, and use a Malvern Zeta potentiometer to measure the particle size. The Zeta potential meter measures its particle size, and the measured particle size is (147.5±7.4) nm, and its particle size distribution diagram is as follows figure 1 shown.

[0072] Determination of Encapsulation Efficiency EE (%):

[0073] (1) HPLC method establishes naringenin standard curve:

[0074] Chromatographic conditions: Measuring instrument: LC-15 high performance liquid chromatography (Shimadzu Corporation, Japan) (with UV detector); Chromatographic column: C18 (...

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Abstract

The invention provides a naringenin nano lipid carrier as well as a preparation method and application thereof. The naringenin nano lipid carrier comprises naringenin and a nano lipid carrier. When the naringenin nano lipid carrier is prepared by using a rotational evaporation method, the nano lipid carrier comprises phospholipid, glycerol trilaurate, medium chain triglyceride and polyoxyethylatedcastor oil; and when the naringenin nano lipid carrier is prepared by using an emulsification evaporation-low temperature curing method, the nano lipid carrier comprises phospholipid, glyceryl monostearate, stearic acid, oleic acid and pluronic F68. The naringenin nano lipid carrier provided by the invention has high encapsulation efficiency and a large medicine carrying capacity, and the orallytaken bioavailability of naringenin can be improved. Compared with free naringenin and a naringenin nano lipid of a reference file 3, the naringenin nano lipid carrier prepared by using the emulsification evaporation-low temperature curing method has higher trans-enterocyte single-layer transfer efficiency and better small intestine absorption effects. Therefore, the carrier has a good inhibitionfunction on non-alcoholic fatty liver diseases with a small dosage.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a naringenin nano-lipid carrier, a preparation method thereof, and an application thereof in the preparation of medicines for preventing and / or treating non-alcoholic fatty liver. Background technique [0002] Naringenin (Naringenin, NGN) is a natural flavonoid widely present in Rutaceae and other plants, which has anti-nonalcoholic fatty liver effect. The dissolution in the gastrointestinal tract is low, resulting in drug loss and waste, affecting the clinical efficacy and application of naringenin. At present, pharmaceutical researchers have devoted themselves to improving the solubility of naringenin through preparation technology. The reported dosage forms include solid dispersions, multilamellar liposomes, β-cyclodextrin complexes, phospholipid complexes, nano self-emulsifying drug delivery systems, and degradable nanoparticles. The above dosage forms have imp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/352A61K47/24A61K47/14A61K47/44A61P1/16
CPCA61K9/0053A61K9/127A61K31/352A61K47/14A61K47/24A61K47/44A61P1/16
Inventor 祁荣胡睿
Owner PEKING UNIV
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