WO2023108232A1

WO2023108232A1 - Liquid dietary supplement composition with functional active ingredients in lipstick form

Info

Publication number: WO2023108232A1
Application number: PCT/BR2021/050549
Authority: WO
Inventors: Viviane SALVETTI
Original assignee: Salvetti Viviane
Priority date: 2021-12-13
Filing date: 2021-12-13
Publication date: 2023-06-22

Abstract

The present invention relates to functional dietary supplement formulations comprising (a) a phase consisting of a mixture of nanosome spheres produced by bioengineering added to low molecular weight hyaluronic acid in a concentration of 5-10% by weight, (b) a phase consisting of plant active ingredients in a concentration of 10%-30% by weight, in each case in relation to the total weight of the formulation, and optionally comprising other auxiliaries and additives, and to the use of this formulation in lipstick form.

Description

COMPOSITION OF LIQUID FOOD SUPPLEMENT WITH FUNCTIONAL ACTIVES IN LIPSTICK FORM

FIELD OF THE INVENTION

[001] The present invention relates to functional formulations comprising a) a phase composed of a mixture of nanosome spheres of biotechnological origin added to low molecular weight hyaluronic acid in a concentration of 5 to 10% by weight, b) a multivitamin phase in a concentration of 10 to 30% by weight, in each case based on the total weight of the formulation, which may optionally further comprise other auxiliaries and additives, and the use of this formulation in the form of a liquid lipstick as a food supplement, weight loss aid and cellulite control agent.

[002] The present invention also relates to functional formulations comprising a) a phase composed of a mixture of nanosome spheres of biotechnological origin added to low molecular weight hyaluronic acid in a concentration of 5 to 10% by weight, b) a active phase consisting of chromium picolinate 100 mg, green tea 50 g, Garcinea cambodia 150 g, taurine 50 g Fucus 40 g, the active phase being at a concentration of 10 to 30% by weight, in each case based on in the total weight of the formulation, optionally also including other auxiliaries and additives, and the use of this formulation in the form of a liquid lipstick as a food supplement, weight loss aid and cellulite control agent.

[003] The present invention also relates to functional formulations comprising deionized water, Klucel HXF, xanthan gum, alginate, picolinate, thyryptophan, molybdenum, beetroot, capsicum, Nipagim, Nipasol, glycerin, soy lecithin, polysorbate 80, citric acid, ascorbic acid, sucralose, strawberry aroma, carmine, Pomceau R4, Bordeaux S and pigment red 40, optionally also including other auxiliaries and additives, and the use of this formulation in the form of liquid lipstick as a food supplement, weight loss aid and cellulite control agent.

[004] The composition is, ultimately, a liquid food supplement with functional assets, whose appearance resembles a cosmetic such as a lipstick, providing beautification of the lips, weight loss enhancer and cellulite control agent.

[005] The composition can also comprise natural or synthetic active principles, with medicinal activity, whose appearance resembles a cosmetic such as a lipstick, providing beautification of the lips, as well as well-being, optionally as a modified release formulation.

BACKGROUND OF THE INVENTION

[006] The desire to look beautiful and healthy has been a human quest for thousands of years. Although ideal beauty has changed over time, achieving an impeccable outer appearance has increasingly been a goal for human beings, especially in times of maximum exposure in the digital world as well. The term functional cosmetics refers to intermediate products between cosmetics and medicines, which act deeper on the skin, providing greater permeation of the ingredients contained therein. The vast majority do not have fragrance or dyes, that is, they are hypoallergenic products, especially suitable for people with allergies or sensitivity.

[007] Lipstick is one of the most used cosmetics in the world. In addition to normally highlighting the lips, a lipstick can be used for lip care. Just like conventional lipstick, lip gloss and contour pencils are also used. However, in addition to its function of beautifying the lips, there is a demand to expand the functionality of this cosmetic so present in the daily lives of consumers. [008] The skin of the lips comprises a thin horny layer and there are no sweat glands on the lips. They are mostly moistened by saliva. Additionally, only isolated sebaceous glands are noted, so that the surface of the lips is practically free of fat. The lips, therefore, tend to dry out and crack, especially in cold and dry climates. As a rule, lipsticks are composed of a wax matrix, in which liquid and semi-solid oils, as well as pigments and fillers are incorporated. These anhydrous systems have not, until now, allowed water-soluble constituents to be introduced into the formulations. To remedy this drawback of the prior art, a large number of attempts to formulate water-in-oil (W/O) type emulsions in stick form can be noted. As a general rule, in these cases, relatively large amounts of emulsifier should be used to obtain a stable emulsion and pigment dispersion, as disclosed in EP1018332 and EP1064908.

[009] Document CN108578278 discloses and claims an edible lipstick that can help you lose weight and a method of preparing it. Lipstick is prepared from: 300-500 parts carnauba wax, 200-400 parts candelilla wax, 50-80 parts olive oil, 50-80 parts sweet almond oil, 50-80 parts sunflower seed, 50-80 parts grapeseed oil, 50-80 parts shea butter, 100-150 parts natural vitamin E, 150-200 parts beeswax and red sorghum pigments. The purpose of this invention is to use pure natural raw materials, and it uses the properties of octacosanol (extracted from a plant native to Japan) which, after entering the body, can help to accelerate lipid metabolism, reduce lipid accumulation and achieve a good modeling effect.

[010] Document CN1 10693766 reveals and claims a lipstick containing beta-carotene and a method of preparing healthy cosmetics for lipstick containing beta-carotene. Healthy lipsticks containing beta-carotene comprise the following raw materials in parts by weight of 10 to 20 parts of octyldodecanol, 7.5 to 15 parts hydrogenated coconut oil, 1.5 to 4 parts polyisobutylene, 0.75 to

1.5 parts petrolatum, 2.5 to 5 parts polyethylene, 1 -2 parts glyceryl isostearate, 1 -2 parts isosteric acid, 2.5-5 parts cholesteryl oleate 1.5-10 parts diisostearyl malate, 1.5-3 parts synthetic wax, 5-15 parts synthetic wax, 2.5-6 parts bis-diglycerylpolyacyladipate-2, 5-10 parts hydrogenated olive oil, 4-8 parts oil of hydrogenated castor oil, 5-10 parts of beta-carotene, 5-10 parts of tocopherol vitamin E, 3-8 parts of bihydroxyl imidazolidinylurea, 1 -2 parts of essence, 0.4-2 parts of tartrazine n° 4 and 0.8-3 parts of Cl 16185.

[01 1] Thus, an objective of the present invention is to formulate food supplements in liquid form for topical application on the lips, with properties of functional hydration and food supplementation, containing a mixture of spheres of nanosomes of biotechnological origin added to low molecular hyaluronic acid weight that promotes softer, smoother and more luminous skin, together with vegetable extracts of gymnema (Gymnema sylvestre R. Br.) and garcinia (Garcinia cambogia L.).

[012] Hydroxycitric acid also has an appetite-reducing action and it is believed that this is due to the alteration of the metabolic flow, resulting from the diversion of dietary carbohydrates and their metabolites, lipid synthesis. To optimize glucose metabolism, some authors suggest the association of hydroxycitric acid with chromium picolinate, which acts in the regulation of insulin levels in the blood.

[013] Tryptophan is an essential amino acid used by the brain, along with vitamin B3, niacin (or niacinamide) and magnesium, to produce serotonin, an important neurotransmitter in the biochemical processes of sleep and mood. [008] Nutraceuticals are produced naturally and have been shown to have an enormous effect on people's health. Whether as a specific ingredient for the body to perform a certain action, or even as a food supplement. Nutraceuticals are pills that represent a wide range of components that help to improve people's health. Regardless of being with a certain food, they are recognized in a very natural way by the body that consumes them, and what is not necessary the body also eliminates with the same ease.

[014] Nutraceuticals are produced naturally and are shown to have a great effect on people's health. Whether as a specific ingredient for the body to perform a certain action, or even as a food supplement. Nutraceuticals are pills that represent a wide range of components that work to help people's health. Regardless of being close to a certain food, they are recognized in a very natural way by the organism that consumes them, as well as what is not necessary the body also eliminates with the same ease.

[015] In addition, it is clear that they are also recognized as functional foods, as they contain a certain substance that is biologically active, which helps the organism, benefiting it in some process, such as the metabolic one, for example.

[016] In summary, the so-called nutraceuticals are food supplements, which have in themselves the concentrated form of the so-called CBs, bioactive compounds out of their original form, and serve to improve or help to recover the health of a person's body.

[017] Gymnema sylvestre, a dicotyledonous medicinal herb belonging to the family Asclepiadaceae, is a woody vine found in tropical Africa, Australia, central and southern India, and China. Gymnema is known to have antimicrobial, anti-hypercholesterolemic and hepatoprotective effects and, in particular, effects on obesity and diabetes mellitus, it has an astringent, stomatal, tonic and refreshing action. It also has a stimulating action on insulin production and diuretic action. More recently, its use has been tried in the treatment of obesity, due to its effect reducing the sweet taste, which lasts from 1 to 2 hours, without interfering with the sensation of other flavors such as salty, acid and astringent. The leaves have moderate diuretic and laxative activity, due to the presence of flavonoids and anthraquinones.

[018] Garcinia acts by inhibiting fatty acid synthesis and is a well-known appetite suppressant. Helps in pancreatic function and glucose regulation, in the reduction of serum levels of triglycerides and cholesterol. It also has a laxative action due to the presence of pectins (emollient action). Hydroxycitric acid is an inhibitor of fatty acid synthesis, as it decreases the supply of acetyl coenzyme A in cellular metabolism. This occurs by competitive inhibition of the citratolyase enzyme by hydroxycitric acid, as it binds more tightly to the enzyme than citric acid. In addition to inhibiting fatty acid synthesis, hydroxycitric acid enhances fat reduction by reducing levels of malonyl coenzyme A, which activates the enzyme carnitine acetyltransferase. L-carnitine also facilitates the activation of this enzyme, which is why some authors suggest the association of L-carnitine with Garcinia sp extract, to promote greater oxidation of fatty acids.

SUMMARY OF THE INVENTION

[019] Surprisingly, the set of a phase composed of a mixture of nanosome spheres of biotechnological origin added to low molecular weight hyaluronic acid with a multivitamin complex phase, in the form of a formulation of a liquid nutraceutical in the form of lipstick, showed an excellent feeling of application on the lips in addition to excellent hydration, with the difference that said lipstick can be used as a food supplement, optionally as a modified release formulation.

[020] The amount of hyaluronic acid decreases in the dermis with age and, thus, this decrease leads to deterioration in tissue quality and repair processes and accelerates the skin aging process. As an example, the viscoelastic properties that work as a shock absorber preventing excessive skin breakdown (responsible for wrinkles) are diminished and as a consequence the skin becomes aged. There are also consequences in the hydration of cells that lose water and electrolytes that are essential for their life.

[021] The plant extracts phase may comprise gymnema and garcinia extracts. As mentioned earlier, gymnema is a dicotyledonous medicinal herb belonging to the Asclepiadaceae family, known to have antimicrobial, anti-hypercholesterolemic and hepatoprotective effects and, in particular, effects on obesity and diabetes mellitus, which has an astringent, stomatal, tonic and refreshing effect. . It also has a stimulating action on insulin production and diuretic action. More recently, its use has been tried in the treatment of obesity, due to its sweet taste reducing effect, which lasts from 1 to 2 hours, without interfering with the sensation of other flavors such as salty, acidic and astringent. According to KIM, Hyeon-Jeong et al. Effects of feeding a diet containing Gymnema sylvestre extract: Attenuating the progression of obesity in C57BL/6J mice, Asian Pacific Journal of Tropical Medicine, v. 9, no. 5, pg. 437-444, 2016, the administration of gymnema extracts in the diet of rats did not produce changes in the blood pressure levels of the animals. Gymnema dry extract (75%) is well tolerated and can be combined with other plants. Garcinia extract standardized in 50% hydroxycitric acid. In addition to hydroxycitric acid, it has its isomers I, II, III and IV and the anthocyanins: B1 and B2, present in the pericarp of the fruit; resin, with about 70%, composed of red and yellow benzophenones and xanthones (including morelic acid, isomorelic acid and alpha-gambogic acid) in addition to mucilages, present in the plant. According to ASTELL, KT and collaborators A review of botanical species and chemical compounds with appetite suppressant properties for body weight control, Plant Foods Hum Nutr. 2013, 68(3): 213-21 , garcinia hydroxycitric acid is well tolerated. DETAILED DESCRIPTION OF THE INVENTION

[022] The functional formulations of the present invention comprise: a) a phase composed of a mixture of nanosome spheres of biotechnological origin added to low molecular weight hyaluronic acid in a concentration of 5 to 10% by weight, b) a complex phase multivitamin in a concentration of 10 to 30% by weight, in each case based on the total weight of the formulation, optionally further comprising other auxiliaries and additives.

[023] The functional formulations of the present invention may also comprise chromium picolinate, amino acids, essential minerals and plant extracts in the so-called "plant complex phase".

[024] Mixtures of spheres of nanosomes of biotechnological origin added to low molecular weight hyaluronic acid are commercially available, the mixture of ethylhexyl palmitate, silica dimethyl silylate; butylene glycol and sodium hyaluronate obtained from BASF under the trade name Epiderfill is particularly preferred.

[025] Depending on the use in question, the term "modified release" refers to any release modification from an immediate release profile and may include controlled or sustained release and/or delayed release characteristics. Depending on the usage at hand, the term “controlled release” and “sustained release” are used interchangeably and refer to the release of functional actives presented from a composition over an extended period of time, e.g. 1 to 8 hours or even longer periods.

[026] Additional ingredients beneficial to the skin and body, such as other anti-aging ingredients, vitamins, hormones, analgesics, anesthetics, botanical extracts, drugs, processing aids, minerals, plant extracts, plant extract concentrates, emollients, Moisturizers, Protectors skin, humectants, silicones, skin soothing ingredients, dyes, perfumes and the like can be added to the formulation. The amounts of such ingredients may be as needed and not limited to any specific limits.

[027] In a preferred embodiment, the functional cosmetic formulation of the present invention comprises the components as listed in Table 1.

TABLE 1: components of the preferred embodiment of the present invention

[028] In a preferred embodiment, the functional cosmetic formulation of the present invention comprises one or more elements of the multivitamin complex as listed in Table 2, optionally being prepared in order to perform a controlled or substantially constant release of the actives over a period of time extended. Examples of modified release multivitamin compositions are described in US8,207,149, US8,361,488, US8,426,391 and US14,213,285, incorporated herein by reference.

TABLE 2: components of the multivitamin complex

[029] The preparation of a modified release form of actives suitable for external use can be performed according to many different techniques. For example, the actives can be dispersed in a matrix, ie a unique blend of constituents and rate controlling excipients in carefully selected ratios in the matrix, and optionally trapped in a coating material. Alternatively, various coating techniques can be used to control the rate of release of the actives from the lipstick formulation. For example, dissolution of the coating can be triggered by the pH of the skin, and the resulting gradual dissolution of the coating over time exposes the matrix to fluid from the local environment. In one type of embodiment, after the coating becomes permeable, the actives dissipate from the outer surface of the matrix. When that surface becomes depleted or depleted of assets, the underlying stores begin to be depleted by diffusion through the disintegration matrix to the external solution. In another type of modality, the release of actives occurs by gradual disintegration or erosion of the matrix, for example, through the solubility of one or more components of the matrix and/or the lack of physical integrity.

[030] The invention relates, in addition to the composition itself, to the use of the functional food supplement formulation as a lipstick, in particular as a functional lipstick. The formulation can also act as a plant-based medicine, if specific active principles are added in the so-called plant complex phase.

[031] The invention further relates to the use of the functional cosmetic formulation according to the invention as a cellulite control and weight loss agent.

[032] The growing fat lobules push the upper tissues to the surface of the skin, causing a patchy appearance of the skin known as "orange peel". Although this phenomenon is physiological at a moderate pace, it is often considered a cosmetic and aesthetic problem to be eliminated. That's why the aim of this certificate of addition is to provide an effective cosmetic solution to reduce measurements, capable of visibly combating cellulite and the "orange peel" appearance. To respond to this, the invention proposes the use of vegetable extracts of gymnema (Gymnema sylvestre R. Br.) and garcinia (Garcinia cambogia L).

[033] In fact, surprisingly, a product obtained from plant extracts of gymnema (Gymnema sylvestre R. Br.) and garcinia (Garcinia cambogia L.) has significant effects on the skin with very interesting cosmetic properties, in particular a high efficiency lipolysis and a significant, novel and surprising effect on major pathways of fatty acid internalization and metabolism within adipocytes.

[034] The above description is intended to illustrate the present invention without limiting it. Unless otherwise indicated, all amounts of data, content and content Percentages are based on weight and total amount or total weight of formulations.

Claims

1. Composition of food supplement with functional actives in the form of lipstick characterized by the fact that it comprises: a) a phase composed of a mixture of spheres of nanosomes of biotechnological origin added to hyaluronic acid of low molecular weight in a concentration of 5 to 10% in weight, b) a multivitamin complex phase in a concentration of 10 to 30% by weight, in each case based on the total weight of the formulation, optionally further comprising other auxiliaries and additives.

2. Composition according to claim 1, characterized in that phase (a) comprises ethylhexyl palmitate, silica dimethyl silylate; butylene glycol and sodium hyaluronate.

3. Composition according to any one of claims 1 or 2, characterized in that the plant extract comprises gymnema and garcinia extracts.

4. Composition according to any one of claims 1 to 3, characterized in that the formulation is composed of: deionized water, Klucel HXF, xanthan gum, alginate, picolinate, tryptophan, molybdenum, beetroot, capsicum, Nipagim, Nipasol , glycerin, soy lecithin, polysorbate 80, citric acid, ascorbic acid, sucralose, strawberry flavor, carmine, Pomceau R4, Bordeaux S and pigment red 40.

5. Composition according to any one of claims 1 to 4, characterized in that the formulation is a lipstick.

6. Composition according to claim 5, characterized in that it is a lipstick in liquid form.

7. Use of the formulation as defined in any one of claims 1 to 6, characterized in that it is similar to a functional lipstick acting on lip hydration.

8. Use of the formulation defined in any one of claims 1 to 6, characterized in that it resembles a functional lipstick that acts as a food supplement.

9. Use of the formulation defined in any one of claims 1 to 6, characterized in that it is similar to a functional lipstick acting on fat loss and cellulite control.