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Spherical micelle for packaging ginsenoside Rg3 and preparation method and application thereof

The technology of ginsenoside and micelle is applied in the field of spherical micelle encapsulating ginsenoside Rg3 and its preparation, which can solve the problems of low bioavailability, low water solubility of Rg3, etc. The effect of increasing intake

Inactive Publication Date: 2017-11-07
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention has designed and developed a spherical micelle encapsulating ginsenoside Rg3. The purpose of the invention is to provide the dosage form of ginsenoside Rg3 to solve the problems of low water solubility of Rg3 and low bioavailability after medication.

Method used

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  • Spherical micelle for packaging ginsenoside Rg3 and preparation method and application thereof
  • Spherical micelle for packaging ginsenoside Rg3 and preparation method and application thereof
  • Spherical micelle for packaging ginsenoside Rg3 and preparation method and application thereof

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Embodiment 1

[0043] The present invention takes ginsenoside Rg3 as a model drug, selects PluronicF127 micelles as a polymer material, prepares loaded ginsenoside Rg3 micelles, and takes the encapsulation efficiency, drug loading and the stability of the micellar solution as investigation indicators, and in the single factor test On the basis of , the formulation and preparation process of mixed micelles were optimized by star-point design, and the physicochemical properties of the optimal formulation were characterized.

[0044] experimental method

[0045] 1. Establishment of HPLC analysis method: the in vitro analysis method of ginsenoside Rg3 applies HPLC method, and the chromatographic conditions are as follows: (1) reversed-phase chromatographic column; (2) mobile phase is acetonitrile: water = 50:50; (3) flow rate 1mL / min; (4) Detection wavelength: UV-203nm; (5) Injection volume: 20μL; (6) Peak time: 9.3min; the method has good specificity, no interference to detection, and good res...

Embodiment 2

[0061] Doxorubicin can cause dose-dependent congestive heart failure and cardiomyopathy, resulting in myocardial damage, which seriously affects the systolic and diastolic functions of the myocardium. , to verify the therapeutic effect of Rg3 micelles and Rg3 monomers on doxorubicin cardiotoxicity.

[0062] Animal selection, experimental reagent configuration, and administration

[0063] 8-week-old healthy C57BL / 6J mice, half male and half female, weighing 18±2g, SPF grade, certificate number 11401300027002, provided by Beijing Huafukang Biotechnology Co., Ltd., license number SCXK (Beijing) 2014 -0004. All the above animals were raised in the clean-grade animal room of the Institute of Radiological Medicine, Chinese Academy of Medical Sciences, with a room temperature of 20-25°C and a relative humidity of 40-60%.

[0064] Pluronic F127Rg3 micelles containing Rg3 at a concentration of 10 mg / ml: weigh 210 mg of Pluronic F127 Rg3 micelles, dissolve in 1 ml of normal saline, an...

Embodiment 3

[0079] In this example, the in vivo mouse breast cancer model, isolated tumor cells and multidrug-resistant cells were used to evaluate the antitumor effect of Rg3 micelles combined with doxorubicin in vivo and in vitro.

[0080] experimental method

[0081] Animal source: 8-week-old healthy Bra-BC mice, half male and half female, weighing 18±2 g, SPF grade, certificate number 11401300027002, supplied by Beijing Huafukang Biotechnology Co., Ltd., license number SCXK ( Beijing) 2014-0004. All the above animals were raised in the clean-grade animal room of the Institute of Radiological Medicine, Chinese Academy of Medical Sciences, with a room temperature of 20-25°C and a relative humidity of 40-60%.

[0082] Configuration of the main solution: Pluronic F127Rg3 micelles containing 10mg / ml Rg3: weigh 210mg Pluronic F127 Rg3 micelles, dissolve in 1ml normal saline, store at 4°C for later use; 10mg / ml Rg3 suspension: weigh 10mg Ginsenoside Rg3 monomer, dissolved in 1ml of normal ...

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Abstract

The invention discloses a preparation method of a spherical micelle for packaging ginsenoside Rg3. The method includes the steps of weighing and fetching ginsenoside Rg3 and carrier materials to be dissolved in appropriate quantity of organic solvents, removing the organic solvent after the mixtures of ginsenoside Rg3 and the carrier materials are completely dissolved, and placing the mixtures in a vacuum drying box over a night; adding appropriate amount of deionized water into the mixtures for hydration, and conducting ultrasonic treatment when the mixtures are completely dissolved; using a filtering membrane to filter the hydration liquid after the ultrasonic treatment to obtain a transparent polymeric micelle solution, and then freezing and drying the solution to obtain the spherical micelle. The invention also discloses a spherical micelle for packaging the ginsenoside Rg3 and an application of the spherical micelle for packaging the ginsenoside Rg3.

Description

technical field [0001] The invention relates to a traditional Chinese medicine preparation, in particular to a spherical micelle encapsulating ginsenoside Rg3, a preparation method and application thereof. Background technique [0002] Doxorubicin (DOX) is an effective clinical anticancer drug, which has been widely used in the treatment of various blood and solid tumors. However, it shows dose-related cardiotoxicity in clinical application, which may affect the efficacy of chemotherapy and have a serious impact on the survival time and quality of life of patients. The mechanism of doxorubicin-induced cardiotoxicity is very complex and may involve the generation of reactive oxygen species (ROS), mitochondrial dysfunction, cell injury and apoptosis, and calcium overload. The quinones and quinone-like substances generated by doxorubicin during the redox cycle in vivo induce ROS production, trigger mitochondrial dysfunction in cardiomyocytes, and lead to DNA damage, lipid pero...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/704A61K47/10A61P35/00
CPCA61K9/1075A61K31/704A61K47/10A61K2300/00
Inventor 樊官伟李澜高秀梅朱美峰韩立锋毛静远张伯礼
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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