NL2037325B1 - A nano-delivery system and preparation method for dietary supplements such as coenzyme q10 and astaxanthin - Google Patents
A nano-delivery system and preparation method for dietary supplements such as coenzyme q10 and astaxanthinInfo
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- NL2037325B1 NL2037325B1 NL2037325A NL2037325A NL2037325B1 NL 2037325 B1 NL2037325 B1 NL 2037325B1 NL 2037325 A NL2037325 A NL 2037325A NL 2037325 A NL2037325 A NL 2037325A NL 2037325 B1 NL2037325 B1 NL 2037325B1
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- NL
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- nano
- delivery system
- coenzyme
- vitamin
- astaxanthin
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L29/00—Foods or foodstuffs containing additives; Preparation or treatment thereof
- A23L29/10—Foods or foodstuffs containing additives; Preparation or treatment thereof containing emulsifiers
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/115—Fatty acids or derivatives thereof; Fats or oils
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/15—Vitamins
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2200/00—Function of food ingredients
- A23V2200/30—Foods, ingredients or supplements having a functional effect on health
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2250/00—Food ingredients
- A23V2250/18—Lipids
- A23V2250/184—Emulsifier
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2250/00—Food ingredients
- A23V2250/18—Lipids
- A23V2250/184—Emulsifier
- A23V2250/1842—Lecithin
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2250/00—Food ingredients
- A23V2250/18—Lipids
- A23V2250/194—Triglycerides
- A23V2250/1944—Medium-chain triglycerides
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2250/00—Food ingredients
- A23V2250/30—Other Organic compounds
- A23V2250/314—Ubiquinone, coenzyme Qn
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2250/00—Food ingredients
- A23V2250/70—Vitamins
- A23V2250/708—Vitamin C
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2250/00—Food ingredients
- A23V2250/70—Vitamins
- A23V2250/712—Vitamin E
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- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Nutrition Science (AREA)
- Engineering & Computer Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Mycology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A NANO-DELIVERY SYSTEM AND PREPARATION METHOD FOR DIETARY SUPPLEMENTS SUCH AS COENZYME Q10 AND ASTAXANTHIN The invention discloses a nano-delivery system and preparation method for dietary supplements such as coenzyme Q10 and astaxanthin. The invention provides an innovative nano-delivery system, which is composed of a stabilizer, a composite oil emulsifier, and a grease solvent. The stabilizer is vitamin E and vitamin C, the composite oil emulsifier is lecithin and Tween 80, and the grease solvent is medium. Chain triglyceride can significantly improve the sustained-release effect and bioavailability of dietary supplements such as coenzyme Q10 and astaxanthin, and solve the problem of stability, absorption and utilization of dietary supplements such as coenzyme Q10 and astaxanthin in the existing technology. It can achieve high bioavailability through oral administration, it provides a nano-delivery system With the optimal ratio, Which has the best stability and maximum bioavailability under this ratio, and provides the advantages of the nano-delivery system. The preparation method is simpler and is beneficial to industrial production.
Description
A NANO-DELIVERY SYSTEM AND PREPARATION METHOD
FOR DIETARY SUPPLEMENTS SUCH AS COENZYME Q10
AND ASTAXANTHIN
The invention relates to the field of nano-delivery technology, specifically a nano-delivery system and preparation method for dietary supplements such as coenzyme Q10 and astaxanthin.
The use of dietary supplements has become an increasingly common way for people to pursue health. Coenzyme Q10, also known as ubiquinone, is an endogenous antioxidant svnthesized by cells themselves. Because it participates in energy synthesis and transfer, it is crucial in the life process of the body. A large number of studies have shown that coenzyme Q10 has the functions of improving human immunity, antioxidant and delaying aging. It can be used medically to treat cardiovascular and cerebrovascular diseases, immune damage, and cancer. It is also widely used in nutritional and health products. As an essential nutrient, the average total content of coenzyme Q10 in the human body 1s about 1.4~1.8 g, and the body’s synthesis ability is strongest around the age of 20. Usually, aging or high metabolic stress will deplete the endogenous supply of coenzyme Q10 1n the body, causing it to be unable to meet the body's operating needs. Therefore, exogenous supplementation of coenzyme Q10 is considered to be a more effective and indispensable way.
However, free coenzyme Q10 has poor water solubility and slow absorption in the gastrointestinal tact, so its industrial application faces challenges. At present, the clinical preparation types of coenzyme Q10 are mainly soft capsules, tablets and water-soluble injections. Although the reduced form of coenzyme Q10 is better absorbed than the oxidized form. But the poor form of coenzyme Q10 severely limits its effectiveness, with low oral bioavailability.
Similar to coenzyme Q10, dietary supplements such as astaxanthin, lutein, lycopene, and
P-carotene also suffer from slow gastrointestinal absorption, poor stability of oral preparations, and low absorption and utilization. How to improve the dissolution stability and absorption utilization rate of dietary supplements such as coenzyme Q10 1s still a hot research topic today.
Nano-encapsulation technology can significantly improve the delivery stability of insoluble substances due to its good biocompatibility and sustained-release capabilities, and 1s widely used in the fields of food and pharmaceuticals. In recent years, lipid-based nanodelivery systems have been used as a novel and practical approach. Compared with traditional emulsions and liposome encapsulation, the solidified cross-linked structure in the system further overcomes embedding instability and significantly extends the effective shelf life. However, nano-delivery systems for dietary supplements such as coenzyme Q10, astaxanthin, lutein, lvcopene, and p-carotene have still not been developed. There is an urgent need to develop a nano-delivery system for the above-mentioned dietary supplements to improve their effectiveness. Oral absorption and utilization.
In view of the shortcomings of the existing technology. the present invention provides a nano-delivery system and preparation method for dietary supplements such as coenzyme Q10 and astaxanthin. The lipid-based nano-delivery system effectively breaks through the bottleneck of low gastrointestinal absorption and utilization and poor functionality of dietary supplements such as coenzyme Q10 and astaxanthin. Nanotechnology refers to the use of atomic and molecular properties and interaction principles at the nanometer scale (0.1~100 nm) to create products with specific functions.
The nanosystem can not only increase the absorption efficiency of carrier substances in the body, but also has a sustained release function.
The present invention discloses a nano delivery system, consisting of a stabilizer, a complex oil emulsifier, a grease solvent, and a delivery substance, the stabilizer is vitamin E and vitamin C, the complex oil emulsifier is lecithin and Tween 80 , the oil solvent is medium-chain triglyceride: the delivery substance is the substance delivered by the nano-delivery system, which 1s any one or more of coenzyme Q10, astaxanthin, lutein, lvcopene, and B-carotene..
Amphiphilic lipids can solubilize guest molecules 1n either the oil phase or the aqueous phase, and have been widely used as ideal delivery vehicles for loading fat-soluble active mgredients. Some of the fatty acid esters not only have good compatibilization for fat-soluble components, but also have better ductility and oxidative stability than ordinary vegetable oils, and can be used as solvent payloads for coenzyme Q10. In addition, emulsifiers contribute to the formation of nanosystems, which can increase the repulsion between particles, prevent particles from aggregating with each other, and enhance stability. Phospholipids and nonionic surfactants can be combined with oil solvents for emulsification to improve the embedding environment and enhance system uniformity. The oil selected in the present invention can form a three-dimensional network structure through physical and chemical cross-linking,
which has the advantages of high loading capacity and stable embedding. It can significantly overcome the gastrointestinal barrier and improve the bioavailability of coenzyme Q10. Furthermore, the full-fat system can effectively avoid the interference of water on Coenzyme Q10 and significantly increase its storage stability. further, the delivery substances. vitamin E, and vitamin C account for 30% of the mass. and the mass ratio of the delivery substances, vitamin E. and vitamin C 1s 4:1:1; lecithin, Tween 80, and medium-chain triglycerides account for 70% of the mass, and lecithin, The mass ratio of Tween 80 and medium chain triglycerides is 2:1:10.
The present invention discloses a method for preparing a nano-delivery system, which 1s characterized by comprising the steps:
Sl, take lecithin and Tween 80 and stir them thoroughly at 50°C-60°C to form a uniform oil phase:
S2, cool the uniform oil phase obtained in S1 to 35°C-45°C, and drop the medium-chain triglveeride, delivery substance, vitamin E and vitamin C into it at the same time to form a mixture; the delivery substance is the substance delivered by the nano-delivery system , which is any one or more of coenzyme Q10, astaxanthin, lutein, lycopene, and B-carotene:
S3, the mixture obtained in S2 is sheared and homogenized at high speed at 10000 rpm, and then homogenized at high pressure at 750 bar;
S54, cool the homogenized mixture of S3 to room temperature to obtain a nano-delivery system.
The high-pressure homogenization method of the present invention uses elevated pressure and mechanical shear force to stretch. break, and disperse large droplets of ordinary emulsion into several small droplets to generate a huge interface area, effectively reducing the size of the internal phase droplets and obtaining nanometer-sized droplets. grade mobile phase system.
Compared with the prior art, the beneficial effects of the present invention are:
I. Discloses a new nano-delivery system, which on the one hand significantly improves the sustained-release effect of coenzyme QI, astaxanthin, etc. and on the other hand increases their bioavailability, solving the problems of coenzyme QI10, astaxanthin, etc. in the existing technology.
Problems with low stability and low absorption and availability can be achieved through oral administration to achieve high bioavailability; 2. Discloses a nano-delivery system with the optimal ratio. which has the best stability and maximum bioavailability under this ratio: 3. Discloses a preparation method of the nano-delivery system, which is simpler and conducive to dustrial production.
The following 1s a clear and complete description of the technical scheme in the embodiments of the invention in combination with the appended drawings in the embodiments of the invention.
Obviously, the described embodiments are only part of the embodiments of the invention, but not all of them. Based on the embodiments in the invention, all other embodiments obtained by ordinary technicians in the field without making creative work fall within the scope of protection of the invention.
Example 1
Take a certain amount of lecithin (PC) and Tween 80 and stir them thoroughly at S0C~60°C to form a uniform oil phase. Finally, the mixture is cooled to 35° C-45° C, and medium-chain triglycerides (MCT) and delivery substance (can be selected from any one or more of coenzyme Q10, astaxanthin, lutein, lycopene, and B-carotene), vitamin E, and vitamin C were dropped into it at the same time, and homogenized by high-speed shearing at 10,000 rpm for 5 min, followed by 750 bar high-pressure homogenization cvcles for 6 times, and the nano-delivery system was obtained after cooling at room temperature.
In the above preparation, the delivery substance, vitamin E, and vitamin C account for 30% of the mass, and the mass ratio of the delivery substance, vitamin E, and vitamin C is 4:1:1; lecithin, Tween 80, and medium-chain triglycerides account for 70% of the mass, and the mass ratio of lecithin, Tween 80, and medium chain triglvcerides is 2:1:10.
The nanodelivery system prepared above was diluted 50 times with distilled water and stirred magnetically for 5 min (100 r/min). Zeta potential. particle size and polydispersity index (PDI) were measured with a Malvern nanoparticle size analyzer.
Table 1. Characterization of Nanodelivery Systems
Delivery Substance Particle size/nm Zeta potential PDI coenzyme Q10 404.15+4.6 -3340.17 0.07£0.06 astaxanthin 432.64+4.5 -3040.25 0.08+0.02 lutein 576.9545.3 -29+0.62 0.14+0.09 lycopene 454 95+£2.7 -31+0.47 0.0940.04
B -carotene 543.8843.8 -32+0.51 0.10£0.05
The characterization results show that the nano-delivery systems for delivering coenzyme Q10, astaxanthin, lutein, lycopene, and B-carotene were successfully constructed. and the absolute value of the electrostatie repulsion between particles is large, indicating the physical stability of the prepared 5 nano-delivery system. Good stability; PDI value is small, indicating that the particle size distribution of the prepared nano-delivery system is uniform, which is conducive to in vivo absorption.
Example 2
Taking the nano-delivery system constructed in Example 1 to deliver coenzyme Q10 as an example, a simulated gastrointestinal sustained-release test was conducted in commercially available simulated gastric juice. The method is as follows:
Set up a control group and an experimental group respectively. The control group is a nano-delivery system using only lecithin-embedded coenzyme Q10 (prepared with reference to the method of Example 1. without other ingredients, the mass ratio of lecithin to coenzyme Q10 is 7:3), The experimental group is the nano-delivery system of coenzyme Q10 prepared in Example 1. put into simulated gastric juice, take samples at intervals to measure the content of active substances in the simulated gastric juice, (total amount - released amount) / total amount is the release rate, released m the stomach The lower the rate, the better.
Table 2. In vitro simulated gastrointestinal sustained release experiment
Group /release rate lh 2h 4h 8h 12h 24h 48h control group 19% 26% 54% 70% 82% 80% 78% experimental group 6% 9% 18% 26% 32% 31% 31%
In vitro simulated gastrointestinal sustained-release tests show that the lipid-based nanodelivery system constructed in the present invention can achieve a higher sustamed-release effect, and in practical applications can avoid the extraction and release of Coenzyme Q10 due to gastric juice destruction, thereby improving the delivery efficiency of Coenzyme Q10 : Because based on the same nano-delivery system, the sustained-release effect of other dietary supplements is similar to that of
Coenzyme Ql0, and the sustained-release effect can be significantly enhanced through the nano-delivery system.
Example 3
Taking the nano-delivery system constructed in Example 1 to deliver Coenzyme Q10 as an example, an 1n vivo absorption kinetics experiment was performed. Rats were orally administered the
Nano-delivery system constructed in Example 1 to deliver Coenzyme Q10, and the concentration of
Coenzyme Ql0 in the blood was used to represent its biological Availability, the higher the concentration of coenzyme Q10 1n the blood, the higher its bioavailability. The specific methods are as follows:
Six SPF male rats (body weight 300 g) were divided into two groups, three in the control group and three in the experimental group, and were fed adaptively for 7 days. After fasting for 12 hours, the rats were mtragastrically treated (80 mg/kg). The experimental group was intragastrically intragastric with the coenzyme Q10 lipid nano-delivery system (prepared in Example 1), and the control group was mtragastrically intragastric with an equal amount of physiological saline. Orbital puncture was performed to collect blood 4 hours after intragastric administration. Centrifuge at 10,000 r/min for 5 min at 4°C, and take the supernatant to determine the UQ concentration. During the experiment, the rats were kept in an animal room with a 12-h day-night cycle, a temperature of (26£2)°C, a humidity of (55+5)%, and a noise level below 60 beeps.
Table 3. Absorption kinetics experiment in rats rat number Blood coenzyme Q10 concentration/pg/mL control group -1 2.08 control group -2 2.11 control group -3 2.04 experimental group -1 2.89 experimental group -2 2.86 experimental group -3 2.81
In vivo absorption kinetics tests show that the lipid-based nano-delivery system constructed in the present invention can significantly increase the oral bioavailability of Coenzyme Q10; since it is based on the same nano-delivery system, the oral bioavailability of other dietary supplements is similar to that of Coenzyme Q10. Nanodelivery systems significantly enhance their bioavailability.
Claims (3)
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| Application Number | Priority Date | Filing Date | Title |
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| NL2037325A NL2037325B1 (en) | 2024-03-25 | 2024-03-25 | A nano-delivery system and preparation method for dietary supplements such as coenzyme q10 and astaxanthin |
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| NL2037325A NL2037325B1 (en) | 2024-03-25 | 2024-03-25 | A nano-delivery system and preparation method for dietary supplements such as coenzyme q10 and astaxanthin |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2432020A1 (en) * | 2001-02-22 | 2002-09-06 | Raj K. Chopra | Coenzyme q products exhibiting high dissolution qualities |
| US20140295046A1 (en) * | 2011-08-11 | 2014-10-02 | Dsm Ip Assets B.V. | Emulsions comprising carotenoid for transparent and pasteurization-stable liquid formulations, especially beverages |
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2024
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2432020A1 (en) * | 2001-02-22 | 2002-09-06 | Raj K. Chopra | Coenzyme q products exhibiting high dissolution qualities |
| US20140295046A1 (en) * | 2011-08-11 | 2014-10-02 | Dsm Ip Assets B.V. | Emulsions comprising carotenoid for transparent and pasteurization-stable liquid formulations, especially beverages |
Non-Patent Citations (4)
| Title |
|---|
| BOONLAO NUNTARAT ET AL: "Enhancing bioaccessibility and bioavailability of carotenoids using emulsion-based delivery systems", COLLOIDS AND SURFACES B: BIOINTERFACES, ELSEVIER AMSTERDAM, NL, vol. 209, 13 November 2021 (2021-11-13), XP086893362, ISSN: 0927-7765, [retrieved on 20211113], DOI: 10.1016/J.COLSURFB.2021.112211 * |
| DATABASE GNPD [online] MINTEL; 2 November 2016 (2016-11-02), ANONYMOUS: "Advanced CO-Q10 Ubiquinol Spray", XP093223804, retrieved from https://www.gnpd.com/sinatra/recordpage/4389019/ Database accession no. 4389019 * |
| SANI MAHMOOD ALIZADEH ET AL: "Nano-enabled plant-based colloidal delivery systems for bioactive agents in foods: Design, formulation, and application", ADVANCES IN COLLOID AND INTERFACE SCIENCE, ELSEVIER, NL, vol. 305, 26 May 2022 (2022-05-26), XP087093908, ISSN: 0001-8686, [retrieved on 20220526], DOI: 10.1016/J.CIS.2022.102709 * |
| SHARIF HAFIZ RIZWAN ET AL: "Physicochemical stability of [beta]-carotene and [alpha]-tocopherol enriched nanoemulsions: Influence of carrier oil, emulsifier and antioxidant", COLLOIDS AND SURFACES A : PHYSIOCHEMICAL AND ENGINEERINGS ASPECTS, ELSEVIER, AMSTERDAM, NL, vol. 529, 26 May 2017 (2017-05-26), pages 550 - 559, XP085148001, ISSN: 0927-7757, DOI: 10.1016/J.COLSURFA.2017.05.076 * |
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