Neo-gambogic acid SLN (solid lipid nanoparticle) and preparation method thereof

A technology of solid lipid nanoparticles and lipid nanoparticles, which is applied in liquid transportation, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of large blood vessel irritation, low solubility, short half-life, etc., and achieve improved treatment The effect of index, mature preparation process and low solubility

Inactive Publication Date: 2011-01-19
彭代银 +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the low solubility of neogambogic acid in aqueous solution, it is highly irritating to blood vessels after injection and has a short half-life in vivo, which limits its clinical application.

Method used

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  • Neo-gambogic acid SLN (solid lipid nanoparticle) and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Dissolve 10mg neogambogic acid and 100mg monostearic acid in chloroform, dissolve 200mg lecithin with a small amount of ethanol, and mix the two parts again to form the organic phase. Dissolve 300mg of poloxamer-188 and 2ml of glycerol in water for injection to form the aqueous phase. Slowly drop the organic phase at 70-80°C into the water phase at the same temperature (70-80°C), and stir at constant temperature until a transparent system is formed. The organic solvent was evaporated under reduced pressure with a rotary evaporator. The concentrated system is quickly mixed in the water phase at 0-2° C., stirred and cooled for 2 hours to obtain a solid lipid nanoparticle suspension. Filter through a microporous membrane to remove large particles, and store in a sealed container at 4°C.

[0059] Detection: the average particle diameter of neotectinic acid solid lipid nanoparticles is 221.8nm, and the encapsulation efficiency is 87.31%.

Embodiment 2

[0061] Dissolve 15mg neogambogic acid and 120mg monostearic acid in n-hexane, dissolve 300mg lecithin with a small amount of ethanol, and mix the two parts again to form the organic phase. Dissolve 400mg of poloxamer-188 and 2ml of glycerol in water for injection to form the aqueous phase. Slowly drop the organic phase at 70-80°C into the water phase at the same temperature (70-80°C), and stir at constant temperature until a transparent system is formed. The organic solvent was evaporated under reduced pressure with a rotary evaporator. The concentrated system is quickly mixed in the water phase at 0-2° C., stirred and cooled for 2 hours to obtain a solid lipid nanoparticle suspension. Filter through a microporous membrane to remove large particles, and store in a sealed container at 4°C.

[0062] Detection: the average particle size of neotectinic acid solid lipid nanoparticles is 184.5nm, and the encapsulation efficiency is 83.47%.

Embodiment 3

[0064] Dissolve 10mg neogambogic acid and 100mg monostearic acid in chloroform, dissolve 200mg lecithin with a small amount of ethanol, and mix the two parts again to form the organic phase. Dissolve 300mg Tween-80 and 2g glycerol in water for injection to form the aqueous phase. Slowly drop the organic phase at 70-80°C into the water phase at the same temperature (70-80°C), and stir at constant temperature until a transparent system is formed. The organic solvent was evaporated under reduced pressure with a rotary evaporator. The concentrated system is quickly mixed in the water phase at 0-2° C., stirred and cooled for 2 hours to obtain a solid lipid nanoparticle suspension. Filter through a microporous membrane to remove large particles, and store in a sealed container at 4°C.

[0065] Detection: the average particle diameter of neotectin solid lipid nanoparticles is 193.6nm, and the encapsulation efficiency is 85.34%.

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Abstract

The invention relates to a neo-gambogic acid SLN (solid lipid nanoparticle) and a preparation method thereof. The neo-gambogic acid SLN comprises a therapeutically effective amount of neo-gambogic acid, medicinal phosphatide, a surfactant and a lipid material. In the invention, the neo-gambogic acid is prepared into SLNs (solid lipid nanoparticles), thereby improving the solubility of the neo-gambogic acid, reducing the irritability, improving the bioavailability, and prolonging the action time of medicaments in a human body, in addition, the neo-gambogic acid SLNs can be gathered partially in the human body so as to play the targeted action of the SLNs and exert the anti-cancer therapeutic action of the SLNs better.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid lipid nanoparticle of an active ingredient of a traditional Chinese medicine and a preparation method thereof. Background technique: [0002] Neo-gambogic acid (Neo-gambogic) is a compound with high anti-tumor activity isolated from the traditional Chinese medicine Garcinia cambogia. 1210 , S180 ascites cancer, Lewis lung cancer, La795 lung adenocarcinoma and other solid tumors have good inhibitory effect. Among them, the effect on lung cancer is the most significant. After intravenous injection of 4-16mg / kg neogambogic acid, it can significantly inhibit the proliferation of transplanted lung cancer A549 cells in nude mice. However, due to the low solubility of neogambogic acid in aqueous solution, it is highly irritating to blood vessels after injection and has a short half-life in vivo, which limits its clinical application. Therefore, it is nec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/10A61K31/35A61K47/24A61K47/28A61K47/34A61K47/44A61P35/00A61K47/06A61K47/26
Inventor 彭代银陈卫东王效山李庆林陈延杰
Owner 彭代银
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