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Allyl isothiocyanate nano-lipid carrier

A nano-lipid carrier, isothiocyanate technology, applied in the direction of nitrile/isonitrile active ingredients, medical preparations of non-active ingredients, capsule delivery, etc. Large, limited application and other problems, to achieve the effect of prolonging local aggregation, high drug loading, and clear targeting

Active Publication Date: 2013-12-25
上海海虹实业(集团)巢湖今辰药业有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Due to the low solubility of allyl isothiocyanate in aqueous solution, it is highly irritating to the body after injection and has a short half-life in vivo, which limits its clinical application. Therefore, it is necessary to use modern preparation technology to effectively increase the concentration of allyl isothiocyanate. The solubility of propyl ester reduces irritation, prolongs the drug's action time and local aggregation in the body, and better exerts its anticancer effect
[0006] Nanostructured lipid carriers (NLC) is a new type of drug loading developed from solid lipid nanoparticles (SLN), which can effectively avoid drug efflux during placement and has a low encapsulation efficiency. The problem with the solid lipid nanoparticle (SLN) system is that it is made of a single lipid material, and after high-pressure homogeneous cooling during the preparation process, the lipid tends to form more regular crystals, causing the trapped Drug efflux or crystallization in the dispersed aqueous phase of SLN

Method used

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  • Allyl isothiocyanate nano-lipid carrier

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preparation example Construction

[0033] When the allyl isothiocyanate nano lipid carrier of the present invention is prepared, its preparation method comprises the following steps:

[0034] (1) Dissolve allyl isothiocyanate, solid lipid material, liquid oil, and fat-soluble emulsifier in an organic solvent, then remove the organic solvent by vacuum rotary evaporation or vacuum drying, and heat to 60~ Melting at 100°C to form the organic phase;

[0035] (2) Dissolve long-circulation excipients, water-soluble emulsifiers, and additives in water for injection, and heat to 60-100°C to form the water phase;

[0036] (3) mixing the organic phase and the aqueous phase under stirring or high shear conditions at a temperature of 60-100° C. to prepare colostrum;

[0037] (4) Ultrasonic or high-pressure homogenization is performed on the colostrum to prepare the allyl isothiocyanate nano-lipid carrier.

[0038] The obtained allyl isothiocyanate nano-lipid carrier can be further lyophilized or kept sealed at 4°C, where...

Embodiment 1

[0040] An allyl isothiocyanate nano lipid carrier, which is composed of: allyl isothiocyanate 5mg, GMS60mg, MCT20uL, lecithin 150mg, absolute ethanol 5mL, PEG200020mg, Tween8040mg, water for injection 50mL.

[0041] The preparation method is as follows:

[0042] Dissolve allyl isothiocyanate, GMS, MCT, and lecithin in absolute ethanol, remove the absolute ethanol by rotary evaporation under reduced pressure, and heat to 80°C to melt to form an organic phase; dissolve PEG2000 and Tween80 in water for injection and heated to 80°C to form the water phase; at a temperature of 80°C, the organic phase and the water phase were mixed under stirring conditions to prepare colostrum; the colostrum was subjected to high-pressure homogenization , and poured into ice water to prepare allyl isothiocyanate nano lipid carrier.

[0043] The drug loading and encapsulation efficiency of allyl isothiocyanate nano-lipid carriers were determined to be 7.82% and 87.6% respectively

Embodiment 2

[0045] A nano-lipid carrier of allyl isothiocyanate, which is composed of: 5 mg of allyl isothiocyanate, 60 mg of GMS, 20 uL of MCT, 150 mg of lecithin, 5 mL of absolute ethanol, 20 mg of PEG2000, 40 mg of Tween8040 mg, and 100 mL of water for injection.

[0046] The preparation method is as follows:

[0047] Dissolve allyl isothiocyanate, GMS, MCT, and lecithin in absolute ethanol, remove the absolute ethanol by rotary evaporation under reduced pressure, and heat to 80°C to melt to form an organic phase; dissolve PEG2000 and Tween80 in water for injection and heated to 80°C to form an aqueous phase; at a temperature of 80°C, the organic phase and the aqueous phase were mixed under stirring conditions to prepare colostrum; the colostrum was subjected to high-pressure homogenization , and poured into ice water to prepare allyl isothiocyanate nano lipid carrier.

[0048] The drug loading and encapsulation efficiency of allyl isothiocyanate nanolipid carriers were determined to ...

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Abstract

The invention discloses an allyl isothiocyanate nano-lipid carrier. The allyl isothiocyanate nano-lipid carrier comprises the following components in percentage by weight: 0.01-8% of allyl isothiocyanate, 0.50-15% of solid lipid material, 0-15% of liquid oil, 0.10-15% of emulsifier, 0-15% of long-circulating auxiliary materials, 0-15% of additives and the balance of water for injection. According to the allyl isothiocyanate nano-lipid carrier disclosed by the invention, the allyl isothiocyanate is encapsulated in a lipid nucleus, the dissolubility of the allyl isothiocyanate is increased, the irritation is greatly reduced, a preparation can achieve the effects of clearer targeting, controlled release and the like to a certain extent, and the preparation further has stable physical and chemical properties.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, and discloses a nano-lipid carrier of allyl isothiocyanate. More specifically, the invention relates to an isothiocyanate nano-lipid carrier that helps avoid phagocytosis of the reticuloendothelial system in the body and can be stored stably. Allyl thiocyanate nanolipid carrier. Background technique [0002] Allyl isothiocyanate (AITC) is the main taste substance of mustard oil. Due to its unique taste and antibacterial properties, recent studies have found that it can inhibit the growth of cancer cells and can also be used in agriculture. Instead of methyl bromide, it is used as a soil disinfectant, so allyl isothiocyanate has broad application prospects in food additives, food antibacterial and antiseptic, medical anticancer and soil disinfection. [0003] Allyl isothiocyanate is a compound with high antitumor activity. It has a wide antibacterial spectrum and low toxicity. It can se...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/275A61K47/34A61K47/32A61K47/36A61P35/00A61K47/10A61K47/14A61K47/24A61K47/26
Inventor 陈卫东王雷方国民张先文朱婷婷林彤远罗晴蔡晓蕾
Owner 上海海虹实业(集团)巢湖今辰药业有限公司
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