WO2022032360A1 - Composition based on plant oils to replace lanolin - Google Patents

Abstract

The present invention relates to a composition based on plant oils for use in the cosmetic or pharmaceutical industry to replace lanolin. The composition has cicatrizing properties, which is noteworthy when used in the pharmaceutical industry, The composition based on plant oils replaces lanolin and includes the following components: (a) coconut oil, (b) sunflower oil, and (c) soy lecithin.

Description

COMPOSITION BASED ON VEGETABLE OILS REPLACEMENT FOR LANOLIN

Field of Invention

[001] The present invention refers to a composition based on vegetable oils with application in the cosmetic or pharmaceutical industry, as a substitute for lanolin. Particularly in the pharmaceutical industry, the composition has healing properties.

Background of the Invention

[002] Lanolin is the fat in wool that is manufactured from the sebaceous secretions of sheep's fat. It is a mixture of sterols and long-chain fatty alcohols. This mixture sometimes contains other substances (nickel, chromium, copper, etc.) in the form of traces.

[003] Lanolin is a natural product obtained from raw wool wax generated by textile improvers as a by-product of the process. During processing, the wool is washed with a mixture of soaps and detergents, generating a mixture of water, soaps and various types of impregnated impurities.

[004] Normally, around 10 to 15% of wool fat can be obtained in this type of process. Lanolin is then obtained through a sophisticated process of wax refining the raw wool.

[005] Lanolin is a wax consisting of a mixture of high molecular weight esters. These esters that compose it are the result of countless combinations between different types of alcohols and acids, making lanolin a unique material.

[006] Lanolin is composed of esters whose acid fraction has a carbon chain ranging from C7 to C40 and the alcoholic fraction from C14 to C36. Therefore, the final combination of esters is very large, but the most important components are the hydroxy-esters from the combination of fatty acids with diols and sterols or fatty alcohols with hydroxy acids.

[007] These hydroxy-esters are largely responsible for the water absorption capacity of Lanolin, one of its main characteristics, responsible until today for its use and importance.

[008] Lanolin is a chemical specialty with high added value and due to the volume demanded by the cosmetic and pharmaceutical industries, there is a need for many flocks of sheep to meet this demand. [009] Lanolin is a yellowish to gray semi-solid containing 25 to 30% water in its hydrated form and a yellow-brown semi-solid in its anhydrous form. Lanolin contains cholesteryl esters of higher fatty acids.

[0010] Due to its emollient, moisturizing, emulsifying properties and its ability to absorb water, lanolin is used as a component of pharmaceutical products, leather finishing compositions, soaps and detergents, face creams, facial tissues, hair compositions, suntan preparations and the like.

[0011] Despite all these properties the animal origin of lanolin is less and less satisfactory for the consumer, bothered by scrapie. Allergic reactions stemming from pesticide residues, strong odor, variable composition, unreliable supply, etc. are additional factors that have led scientists to look for lanolin substitutes.

[0012] Attempts to replace lanolin with oleochemicals are numerous.

[0013] So far, the proposed substitutes do not offer total satisfaction because of the properties, the complexity of their composition, certain high physicochemical characteristics, such as the acidity index, and/or their manufacturing costs.

[0014] EP 0051148 teaches lanolin substitute product comprising short chain fatty acids and coconut fatty acid.

[0015] US 2005233015 A teaches lanolin substitute based on shea butter.

[0016] WO 2004065533 teaches lanolin substitutes that are obtained from saturated and/or unsaturated fatty acids, or their esters, or hydrocarbons, and may contain vegetable oils, which are subjected to heat treatment from 100 °C to 400 ° C, particularly between 230°C to 350°C.

[0017] DE 10143948 teaches a substitute product for lanolin based on polyisobutene, which may contain vegetable oils.

[0018] The present invention deals with a substitute product for lanolin that has advantages over products known to man in the art.

Objectives of the Invention

[0019] A substitute composition for lanolin was developed in the pharmaceutical industry or cosmetic, which presented:

- attractive final price;

- a sustainable product;

- use raw material available on the market and non-toxic;

- employ a process to obtain low energy consumption and without the production of effluents.

Summary of the Invention

[0020] A composition based on vegetable oils to replace lanolin was developed, which surprisingly has healing properties. The composition comprises coconut oil, sunflower oil and soy lecithin.

Brief Description of Figures

- Figure 1 illustrates the representative images of the respective groups and times.

- Figure 2 illustrates the percentage of wound closure over time, between groups.

Detailed Description of the Invention

[0021] The present invention will now be described more fully. The composition based on vegetable oil substitutes for lanolin according to the invention comprises:

(a) coconut oil;

(b) sunflower oil; and

(c) soy lecithin.

[0022] Coconut oil, coconut oil or coconut butter is a vegetable oil that contains about 90% of fatty acids extracted by pressing the pulp or core of coconuts (Cocos nucifera).

[0023] It is widely used in the cosmetics industry (for making soaps and creams).

[0024] It is raw material for the production of coconut fatty acid diethanolamides, lauric alcohol derivatives such as sodium lauryl sulfate, corrosion inhibitors, sulfonated oil and several other products in the raw material industry for cosmetics.

[0025] Virgin oil

[0026]_Coconut oil can be extracted through "dry" or "wet" processing. Dry processing requires the dough to be extracted from the shell and dried using fire, sunlight, or an oven to create copra. Copra is processed or dissolved with solvents, producing coconut oil and a pulp with high protein and fiber content. Pulp is generally used to feed ruminants, as it is not of sufficient quality by industrial standards. There is no process to extract the protein from the pulp.

[0027] The "wet" process uses raw coconut instead of copra, and the proteins present in the coconut create an emulsion of water and oil. The emulsion is then broken down by prolonged boiling, centrifugation or pretreatments including cold, heat, acids, salts, enzymes, electrolysis, shock waves, steam distillation, or some combination.

[0028] Refined oil

[0029]_ Refined oil is usually made from dried coconut kernels, which are pressed in a heated hydraulic press to extract the oil. This produces virtually all of the oil present, representing more than 60% of the coconut's dry weight. This "crude" coconut oil is not suitable for consumption because it contains contaminants and must be refined with further heating and filtration.

[0030] Another method for extracting coconut oil involves the enzymatic action of alpha-amylase, polygalacturonase and proteases in a diluted coconut paste.

[0031] Hydroaenacao

[0032] Refined oil can be further processed into partially hydrogenated oil or hydrogenated oil, to increase its melting point. As virgin and refined oils melt at a temperature of 24°C, foods containing coconut oils tend to melt in hot climates. Therefore, a higher melting point is desirable in these climates. The melting point of hydrogenated coconut oil varies between 36°C and 40°C.

[0033] The composition of refined coconut oil comprises C6 - C20 fatty acids, such as: caproic acid, caprylic acid, lauric acid, myristic acid, palmitoleic acid, stearic acid, oleic acid, linoleic acid and arachidic acid.

[0034] For example, refined coconut oil extracted from the almond fruit of the oil palm Elaeis guineensis and subjected to the refining process, has the fatty acid composition indicated in Table 1 below:

TABLE 1

[0035] About 40% of coconut fat is composed of lauric acid. In the human body, it is transformed into monolaurin, a monoglyceride of antibacterial, antiviral and antiprotozoal action, used by the body to destroy the lipid layer of various microorganisms.

[0036] The coconut oil according to the invention must have a maximum acidity Mg KOH/g of 0.1% measured by the AOCS Method Ca 5a-40.

[0037] The present invention deals with a composition that comprises, in relation to its total mass, from 50% to 85% by weight of coconut oil. Refined coconut oil is preferably used.

[0038] The composition also comprises in relation to its total mass from 8% to 26% of sunflower oil.

[0039] Sunflower oil is extracted from the seed of the Heüanthus annuus plant.

[0040] It is used in cosmetics and due to its high concentration of vitamin E, it is recommended for use on the skin (topical use) for protection and strengthening.

[0041] The sunflower Heüanthus annuus is an annual plant of the Asteraceae family, genus Heliantheae. The name is derived from the shape of its inflorescence.

[0042] Sunflower oil comprises C12 - C22 fatty acids such as: lauric acid, myristic acid, palmitic acid, palmitoleic acid, stearic acid, oleic acid (Omega 9), linoleic acid (Omega 6), linolenic acid (Omega 3), arachidic acid, eicosenoic acid, behenic acid, erucic acid and lignoceric acid, as indicated in Table 2 below:

TABLE 2

[0043] Like all vegetable oils, sunflower oil is essentially made up of triacylglycerols (98 to 99%). It has a high content of unsaturated acids (about 83%), but a low content of linolenic acid (< 0.2%). Sunflower oil is essentially rich in essential fatty acid (EFA) or linoleic acid.

[0044] The sunflower oil according to the invention must have a maximum acidity Mg KOH/g of 2 measured by the AOCS Method Ca 5a-40 and comprise a C18:l grease chain from 75% to 90.7%.

[0045] The composition according to the invention comprises, in relation to the total mass of the composition, 5% to 22% by mass of soy lecithin.

[0046] Lecithin is a phospholipid found naturally in foods of animal and vegetable origin, with egg yolk, soy and wheat germ being the main sources.

[0047] The main phospholipids present in marketed lecithin (from soy or sunflower seeds) are phosphatidylcholine, phosphatidylinositol, phosphatidylethanolamine and phosphatidic acid (generally abbreviated as PC, PI, PE and PA, respectively). In order to adapt the action of the lecithin according to the product to which it will be added, the lecithin can be enzymatically hydrolyzed. In hydrolyzed lecithin, a portion of the phospholipids have a fatty acid removed by the action of a phospholipase. Such phospholipids are referred to as lysophospholipids. The most commonly used phospholipase for this purpose is called phospholipase A2, which removes the fatty acid at the sn-2 position.

[0048] Lecithins can also be modified by a process called fractionation, which consists of mixing the oil in an alcohol (usually ethanol). Some phospholipids have good solubility in ethanol (e.g. phosphatidylcholine), whereas other phospholipids are shown to be insoluble in the same solvent. The ethanol solution is then decanted and subjected to solvent evaporation in order to obtain a phosphatidylcholine-enriched lecithin fraction.

[0049] The soy lecithin used according to the invention must have an acidity Mg KOH/g of at most 2 measured by the AOCS Ja 6-55 method.

[0050] According to an embodiment of the invention, the composition comprises, by mass in relation to the total mass of the composition, the following components:

(a) from 50% to 85% by weight of coconut oil;

(b) from 8% to 26% by weight sunflower oil; and

(c) from 5% to 22% by weight soy lecithin.

[0051] According to yet another embodiment of the invention, the composition comprises, by mass in relation to the total mass of the composition, the following components:

(a) from 55% to 80% by weight of coconut oil;

(b) from 11% to 21% by weight sunflower oil; and

(c) from 7% to 15% by weight soy lecithin.

[0052] The lanolin substitute composition according to the invention has healing properties and can be used in the pharmaceutical industry in products that require this property, such as ointments, plasters, etc.

[0053] The method of obtaining the composition involves the following steps:

(a) 50% to 85% by mass of coconut oil and from 8% to 26% by mass of sunflower oil are introduced into a reactor;

(b) the mixture is heated to a temperature between 40°C and 60°C;

(c) still maintaining the temperature between 40°C and 60°C, the mixture is stirred with rotation between 30 and 50 rpm until homogenization;

(d) then 5% to 22% by mass of soy lecithin is added, and the mixture is stirred again with rotation between 30 and 50 rpm, keeping the temperature between 40°C and 60°C until homogenization;

(e) the product obtained is allowed to cool before filling.

[0054] According to another embodiment of the invention, the method of obtaining the composition involves the following steps:

(a) 55% to 80% by mass of coconut oil and from 11% to 21% by mass of sunflower oil are introduced into a reactor; (b) the mixture is heated to a temperature between 45°C and 55°C;

(c) still maintaining the temperature between 45 °C and 55 °C, the mixture is stirred with rotation between 30 and 50 rpm until homogenization;

(d) then 7% to 15% by mass of soy lecithin is added, and the mixture is stirred again with rotation between 30 and 50 rpm, keeping the temperature between 45 °C and 55 °C until homogenization;

(e) the product obtained is allowed to cool to around 35°C to proceed with packaging.

[0055] The following are merely illustrative examples, which should not be taken for the purpose of limiting the invention.

Example 1

[0056] A lanolin substitute composition according to the invention was reproduced comprising the components as indicated in Table 3 below:

TABLE 3

Example 2

[0057] The composition indicated in example 1 was obtained through a protocol that involved the following steps:

- in a stainless steel reactor, 75% by mass of coconut oil and then 15% by mass of sunflower oil were introduced;

- the mixture was heated to a temperature of 50 °C, until the components became liquid (the temperature was not increased further as the carbon chains of the components could break);

- with the temperature maintained at 50 °C, the components were mixed with a rotation of 35 rpm for 30 minutes until the mixture was homogeneous;

- then 10% by mass of soy lecithin was slowly added and mixed with a rotation of 35 rpm for 40 minutes, keeping the temperature at 50 °C; - the mixture obtained in the previous step was allowed to cool to 35 °C, as the final product must be filled with the product in a liquid state. It is not recommended to let it cool completely, as the product can solidify in the equipment, thus making packaging difficult.

Example 3

[0058] With the aim of simulating a wound in vitro, an assay was carried out from the cell monolayer. From this monolayer, a wound was made and the investigational product presenting the composition indicated in example 1 was applied, in the supplemented culture medium and compared to the control group. Wound closure was monitored over different time periods using images for wound analysis. This methodology mimicked the wound healing process in vivo.

[0059] 1. RELEVANCE OF THE STUDY

[0060] The experimental conditions used are accepted and consistent with the methodologies currently applied in the international scientific community, as well as the use of cells under appropriate cultivation conditions.

[0061] 2. METHODOLOGY

[0062] 2.1 Cell culture

[0063] In this study, human keratinocyte cells from the epidermis were used, maintained in culture with DMEM (Dulbecco's Modified Eagle's Medium) with the addition of supplements, in an oven at 37°C and 5% CO2 and manipulated inside a laminar flow hood. In passage 03 after thawing, the cells were distributed in 35mm plates.

[0064] 2.2 Sample preparation Sample NV.52.02

• Sample preparation conditions in the starting solution: 10 mg/ml in supplemented culture medium.

• Appearance of the solubilized sample: fully solubilized.

• Expected sample concentrations (mg/ml): 10mg/ml.

• Presence of additional solvent at the highest tested concentration of the sample: not applicable.

• pH measurement at the highest tested concentration of the sample: not determined.

[0065] 2.3 Preparation of control groups Control group: supplemented culture medium

[0066] 2.4 Wound realization and follow-up [0067] At the time the cultures reached 100% confluence, an in vitro wound was performed and this was considered the 0h time. At this time, supplemented culture medium was added to the control group and the solution prepared from sample NV.52.02 was added to the experimental group. Cultures were maintained at 37°C for 48 hours, and images were taken every 15 minutes.

[0068] 2.5 Analysis of results

[0069] The images were evaluated with the help of Image! Wound areas were analyzed at 0, 12, 24, 36 and 48 hours to assess the percentage of wound closure over time, with 0% being considered at 0h and 100% wound closure when it was not possible to observe the bottom of the plate.

[0070] 3. RESULTS

[0071] The wounds at time 0h in the Control group and the Sample NV.52.02 group showed a similar area. After 24 hours, it was observed that the Sample group

NV.52.02 performed around 81% of wound closure, while the control group had 53% closure. At the end of the 36 hours, the Sample group

NV.12.02 showed complete closure of the sham wound, while the control group needed 48 hours to close the wound completely.

[0072] Figure 1, attached, brings the representative images of the respective groups and times.

[0073] Figure 2 and Table 4 demonstrate the percentage of wound closure according to time between groups, with 0% being considered at time 0h and 100% when it was not possible to identify the bottom of the plaque in the image.

TABLE 4

[0074] 4. CONCLUSIONS

[0075] According to the results obtained, it is possible to state that: - The sample NV.52.02 reduced the time of total wound closure.

Example 4 [0076] A lanolin substitute composition according to the invention was reproduced comprising the components as indicated in Table 5 below:

TABLE 5

Claims

claims 1. Composition based on vegetable oils to replace lanolin characterized by comprising: (f) coconut oil; (g) sunflower oil; and (h) soy lecithin. 2. Composition based on vegetable oils replacing lanolin, according to claim 1, characterized in that it comprises: (a) from 50% to 85% by weight of coconut oil; (b) from 8% to 26% by weight sunflower oil; and (c) from 5% to 22% by weight soy lecithin. 3. Composition based on vegetable oil substitutes for lanolin, according to claim 1 or 2, characterized in that (a) from 55% to 80% by weight of coconut oil; (b) from 11% to 21% by weight sunflower oil; and (c) from 7% to 15% by weight soy lecithin. 4. Composition based on vegetable oil substitutes for lanolin, according to claims 1 to 3, characterized in that the coconut oil is refined and has a maximum acidity Mg KOH/g of 0.1% measured by the AOCS Method Ca 5a- 40. Composition based on vegetable oils replacing lanolin, according to claims 1 to 3, characterized in that the sunflower oil has a maximum acidity Mg KOH/g of 2 measured by the AOCS Method Ca 5a-40 and must comprise a chain C18 grease: l from 75% to 90.7%. 6. Composition based on vegetable oils replacing lanolin, according to claims 1 to 3, characterized in that the soy lecithin has an acidity Mg KOH/g of at most 2 measured by the AOCS Ja 6-55 method. 7. Method of obtaining a composition based on vegetable oils to replace lanolin according to claim 1, characterized in that it has the following steps: (a) 50% to 85% by mass of coconut oil and from 8% to 26% by mass of sunflower oil are introduced into a reactor; (b) the mixture is heated to a temperature between 40°C and 60°C; (c) still maintaining the temperature between 40°C and 60°C, the mixture is stirred with rotation between 30 and 50 rpm until homogenization; (d) then 5% to 22% by mass of soy lecithin is added, and the mixture is stirred again with rotation between 30 and 50 rpm, keeping the temperature between 40°C and 60°C until homogenization; (e) the product obtained is allowed to cool before filling. 10. Method of obtaining a composition based on vegetable oils to replace lanolin according to claim 9, characterized in that it has the following steps: (a) 55% to 80% by mass of coconut oil and from 11% to 21% by mass of sunflower oil are introduced into a reactor; (b) the mixture is heated to a temperature between 45°C and 55°C; (c) still maintaining the temperature between 45 °C and 55 °C, the mixture is stirred with rotation between 30 and 50 rpm until homogenization; (d) then 7% to 15% by mass of soy lecithin is added, and the mixture is stirred again with rotation between 30 and 50 rpm, keeping the temperature between 45 °C and 55 °C until homogenization; (e) the product obtained is allowed to cool to around 35°C to proceed with packaging.