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Digestive tract environment response type nanostructure lipid carrier as well as preparation and application thereof

A nano-structured lipid and environmental response technology, which is applied in the direction of microcapsules, effective ingredients of hydroxyl compounds, non-effective ingredients of oil/fat/wax, etc., can solve the problem of limited bioavailability and low digestion efficiency of fat-soluble active substances , low digestibility and other issues, to achieve the effect of improving bioavailability, high encapsulation efficiency and small particle size

Active Publication Date: 2022-03-01
SOUTH CHINA AGRI UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has also been found in practical applications that quite a few nanostructured lipid carriers also have the problems of low digestibility and limited bioavailability of fat-soluble active substances when they are used as delivery systems for active substances.
Such as Raquel F.S. et al. used beeswax and medium-chain triglycerides to prepare nanostructured lipid carriers containing 2.5%wt of beeswax [Lipid-based nanostructures as strategy to enhance curcumin bioaccessibility: Behavior under digestion and cytotoxicity assessment], but the lipid-based nanostructures in the nanostructured The solid fat beeswax used in the mass phase has a high melting point. After being digested in the small intestine for two hours, the release rate of free fatty acids of the nanostructured lipid carrier is only 32.8 ± 3.58%, and the digestion efficiency is low. Nanoemulsion

Method used

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  • Digestive tract environment response type nanostructure lipid carrier as well as preparation and application thereof
  • Digestive tract environment response type nanostructure lipid carrier as well as preparation and application thereof
  • Digestive tract environment response type nanostructure lipid carrier as well as preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] The nanostructure lipid carrier of embodiment 1 load curcumin

[0079] 1. Preparation method

[0080] S1. Preparation of water phase W: Add 2 g of Tween 80 into 78 mL of deionized water, stir at 45°C for 10 min until dissolved, and the emulsifier concentration accounts for 2 wt% of the whole system to obtain water phase W;

[0081] S2. Preparation of lipid phase O: Mix 14g of cocoa butter and 6g of medium-chain triglycerides and heat to 45°C to obtain a mass ratio of solid fat to liquid oil in the lipid phase of 7:3; then add 50mg of curcumin , to obtain curcumin accounting for 0.25% (w / w) of the lipid phase, stirred at a constant temperature of 45° C. for 10 min, which is the lipid phase O;

[0082] S3. Mixing of water phase W and lipid phase O: at 45°C, mix lipid phase O and water phase W at a mass ratio of 2:8, and stir at 45°C for 10 minutes to mix;

[0083] S4. Preparation of colostrum O / W: the mixed milk obtained in S3 was mixed at a speed of 10000 rpm for 3 min...

Embodiment 2

[0087] The nanostructure lipid carrier of embodiment 2 load curcumin

[0088] 1. Preparation method

[0089]S1. Preparation of water phase W: Add 2 g of soybean lecithin into 88 mL of deionized water, stir at 60°C for 10 min until dissolved, and the emulsifier concentration accounts for 2 wt% of the whole system to obtain water phase W;

[0090] S2. Preparation of lipid phase O: Mix 9 g of cocoa butter and 1 g of medium-chain triglycerides and heat to 60 ° C to obtain a mass ratio of solid fat to liquid oil in the lipid phase of 9:1; then add 75 mg of curcumin , to obtain curcumin that accounts for 0.75% (w / w) of the lipid phase, and stir at a constant temperature of 60 ° C for 10 min, which is the lipid phase O;

[0091] S3. Mixing of water phase W and lipid phase O: at 60°C, mix lipid phase O and water phase W at a mass ratio of 1:9, and stir at 60°C for 10 minutes to mix;

[0092] S4. Preparation of colostrum O / W: the mixed milk of S3 was mixed at a speed of 8000 rpm for ...

Embodiment 3

[0096] The nanostructure lipid carrier of embodiment 3 loaded curcumin

[0097] 1. Preparation method

[0098] S1. Preparation of water phase W: Add 1 g of Tween 80 and 1 g of soybean lecithin into 78 mL of deionized water, stir at a constant temperature of 40°C for 10 min until dissolved, and the emulsifier concentration accounts for 2 wt% of the whole system to obtain water phase W;

[0099] S2. Preparation of lipid phase O: Mix 10 g of shea butter and 10 g of medium-chain triglycerides and heat to 40°C to obtain a mass ratio of solid fat to liquid oil in the lipid phase of 1:1; then add 100 mg Curcumin, to obtain curcumin accounting for 0.5% (w / w) of the lipid phase, stirred at a constant temperature of 40°C for 10min, which was the lipid phase O;

[0100] S3. Mixing of water phase W and lipid phase O: at 40°C, mix lipid phase O and water phase W at a mass ratio of 2:8, and stir at 40°C for 10 minutes to mix;

[0101] S4. Preparation of colostrum O / W: Mix the mixed milk o...

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Abstract

The invention provides a digestive tract environment response type nanostructure lipid carrier as well as preparation and application thereof. According to the nanostructure lipid carrier, edible solid fat with the melting point range of 35-40 DEG C and liquid oil serve as a core layer, and a water phase serves as a shell layer. By controlling the lipid phase, the water phase and the precise ratio of the solid lipid to the liquid oil in the lipid phase, the loading rate of the nanostructure lipid carrier to the fat-soluble active matter can be 10 times or more higher than the equilibrium solubility of the nanostructure lipid carrier. The nano-structure lipid carrier has oral cavity and digestive tract environment temperature responsiveness and has the digestion characteristic of nano emulsion, after the nano-structure lipid carrier is loaded with fat-soluble active matter, the bioavailability of the fat-soluble active matter reaches 57.80%-73.56%, in addition, the nano-structure lipid carrier has excellent storage stability, and the nano-structure lipid carrier can be applied to oral cavity and digestive tract oral cavity and digestive tract oral cavity and digestive tract oral cavity and digestive tract oral cavity and digestive tract oral cavity and digestive tract oral cavity and digestive tract oral cavity and digestive tract oral cavity and digestive tract oral cavity. And a new dosage form is provided for a nano-emulsion delivery system in the food field.

Description

technical field [0001] The invention belongs to the technical field of nanoemulsion preparation, and in particular relates to a digestive tract environment-responsive nanostructured lipid carrier and its preparation and application. Background technique [0002] Nanoemulsions prepared from liquid oil at room temperature as the lipid phase have the unique advantages of small particle size and high bioavailability after digestion in the small intestine when used as a delivery system for fat-soluble active substances, and are very useful in the fields of food and medicine. widely. However, due to the thermodynamic instability of nanoemulsions and the difficulty in the existence of fat-soluble active substances in a stable supersaturated state in nanoemulsion droplets, nanoemulsions usually have low storage stability and low sensitivity to fat-soluble active substances. The disadvantage of low load rate. Another nanoemulsion system, the "solid lipid nanoparticle" system, in wh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/107A61K31/05A61K31/12A61K31/122A61K31/352A61K47/14A61K47/44
CPCA61K9/5123A61K9/5192A61K9/1075A61K47/44A61K47/14A61K31/352A61K31/12A61K31/05A61K31/122
Inventor 肖杰郭燕琼
Owner SOUTH CHINA AGRI UNIV
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