FR2892024A1 - Use of calcium for preparing cosmetic/pharmaceutical slimming compositions for topical usage - Google Patents

Abstract

Calcium is used for preparing cosmetic or pharmaceutical slimming compositions for topical usage. An independent claim is included for a natural compound containing calcium as active ingredient. ACTIVITY : Dermatological; Cosmetic. MECHANISM OF ACTION : None given.

Description

Use of calcium for producing cosmetic compositions or

  slimming pharmaceutical products for topical use. The field of the invention is that of the design and manufacture of compositions for cosmetic or pharmaceutical use.

  The invention relates more specifically to the field of compositions intended for topical application (creams, ointments, milks, etc.) for slimming purposes. The invention relates in particular, but not exclusively to the field of cosmetic or pharmaceutical compositions containing natural substances. Many prior art compositions for causing or inducing thinning are known in the art. Most of these compositions implement two modes of action. A first mode of action is to reduce the fatty tissue by hydrolysis of triglycerides. As the active ingredient used in such compositions, caffeine is also known, but also concentrated extracts of brown algae such as Laminaria digitata. A second mode of action implemented by the slimming compositions known in the state of the art consists in influencing the mechanism of lipogenesis. According to this mode of action, these compositions comprise compounds such as sterols or polyunsaturated fatty acids which intervene in the storage of fats to limit the increase in the volume of adipocytes. In particular, the use of compositions containing lipid extracts of the microalga Odontella aurita rich in eicosapentaenoic acid, or seeds of Polygonum fagopyrum rich in phytosterols is known. According to these two modes of action, the alternative is therefore either to stimulate lipolysis to allow destocking of lipid content of adipocytes, or to limit the storage capacity of adipocytes by modulating lipogenesis.

  However, recently, a new mode of action has been envisaged for producing slimming compositions consisting of the use of compounds capable of inhibiting the differentiation of preadipocytes into adipocytes.

  Adipocytes are derived from pluripotent mesenchymal stem cells. These stem cells have the ability to differentiate into different cell types: adipocytes constituting the fatty tissue, chondrocytes constituting the connective tissue, osteoblasts constituting the bone tissue, or myocytes constituting the muscle tissue. Differentiation to a given cell type requires the expression of specific transcription factors. By differentiation, these stem cells are first transformed into adipoblasts, undifferentiated cells, then into preadipocytes, cells that do not yet have the ability to accumulate triglycerides. The preadipocyte expresses the early genes, including those of the C / EBP or Enhancer Binding Protein and PPAR or Peroxisome Proliferator to Activated Receptor transcription factors. Finally, during terminal differentiation, the cell acquires the characteristic functions of the adipose cell, that is to say the capacities to synthesize and store triglycerides and to hydrolyze them in response to the hormonal environment.

  The Applicant has developed a product, called Scopariane (registered trademark), consisting of a hydroglycolic extract obtained from the brown alga Sphacelaria scoparia and implementing this mode of action. The object of the present invention is to provide novel cosmetic or pharmaceutical compositions for thinning also implementing it. In this context, the present invention proposes to use calcium as an active ingredient for producing cosmetic or pharmaceutical slimming compositions for topical use.

  The Applicant has discovered that, surprisingly, calcium applied topically to the skin allowed to inhibit the transformation of preadipocytes into adipocytes. Although it will be possible to envisage using calcium in the form of salts, for example in the form of calcium chloride added to any formulation of cosmetic or pharmaceutical compositions as a slimming active principle, a calcium-containing natural compound will preferably be used. bioavailable for the realization of these compositions. Among these natural compounds, it will be particularly advantageous to use water from marine sources. Such waters are indeed very high in calcium and also have the advantage of showing high purity. According to a preferred variant of the present invention, however, it will be used for the production of these cosmetic or pharmaceutical slimming compositions for topical use, plant extracts containing bioavailable calcium. (Bioavailable calcium means calcium in a natural product in the form of salts or low-chelated calcium). Among the plant extracts that may be used in the context of the present invention, use will advantageously be made of extracts of at least one halophyte plant, in particular, but not exclusively, salicornia, sea fennel, obione, soda, etc. These plants have the particularity of containing high levels of bioavailable calcium. In a most preferred manner, however, it will be used as calcium source an algae extract called limestone that is to say belonging to the family Corallinaceae. In a particularly advantageous manner, it will be used in the context of the present invention, a coralline extract including Corallina officinalis. Corallines are red algae that have an original appearance because of their calcified structure. This unique structure is due to carbonates contained in successive layers in their tissues. Corallines build a calcium carbonate support that is covered by a thin layer of plant tissue. This tissue is responsible for the secretion of a jelly that will precipitate carbonates. This hard carbonates form a protective shell.

  Preferentially, but not exclusively, the extracts used in the context of the present invention will be water-soluble extracts. The invention also covers any cosmetic or pharmaceutical slimming composition for topical use containing as active principle calcium, preferably in a proportion of 0.1 mg / l to 1000 mg / l (expressed as Cal +). The invention, as well as the various advantages that it presents, will now be more easily understood thanks to the following description of a nonlimiting example of embodiment thereof given with reference to the drawings in which: FIG. a diagram showing the effect of a concentrate of Coralline and retinoic acid on the differentiation of adipocytes according to a first experiment; FIG. 2 represents a diagram showing the effect of a concentrate of Coralline and Scopariane on the differentiation of adipocytes according to a second experiment; FIG. 3 represents a diagram showing the effect of calcium chloride and Scopariane on adipocyte differentiation according to a third experiment; FIG. 4 represents a diagram showing the effect of magnesium chloride and Scopariane on adipocyte differentiation according to a fourth experiment. 1) Evaluation of the effect of calcium on the differentiation of adipocytes. At first, the Applicant evaluated in vivo the effect of calcium on the differentiation of adipocytes.

  To do this, mouse pre-adipocytes (line 3T3-L1) from the ATCC American Type Culture Collection were cultured at 37 ° C. in an atmosphere at 5% CO2 and 95% humidity, in a suitable culture medium (DMEM Dulbecco's Modified Eagle's Medium) containing a mixture of ingredients known to induce differentiation into adipocytes (according to the method described by JM Mc Donald et al., 1976, Proc Natl Acad Sci USA, 73: 1542). This mixture allows the transformation of pre-adipocytes into adipocytes. This positive control is hereinafter referred to as the induced control.

  In parallel, various test products were added in this culture medium and the cells were incubated for 7 days at 37 ° C. After 7 days, the culture media were removed and the cells were fixed with formalin and the contents lipid was stained with a red oil solution, and the cells were lysed to release the lipids. The amounts of lipids produced were evaluated by a spectrophotometric assay. A culture medium to which no product known to induce the transformation of preadipocytes into adipocytes was used as a negative control. This negative control is hereinafter referred to as non-induced control. 1.1 Experiment No. 1 In a first experiment, one used: on the one hand calcium, according to the present invention, in the form of coralline concentrate (Corallina officinales) at a rate of 1% or 2% by weight; and, on the other hand, according to the prior art, a compound known to inhibit the conversion of pre-adipocytes into adipocytes, namely retinoic acid at a concentration of 10 -5 M. retinoic acid from Sigma Company - reference R2625 was used.

  The Coralline concentrate used was produced by reverse osmosis. This concentrate of Coralline is very rich in minerals and in particular very rich in calcium since it contains about 0.1 gram of calcium per liter. It is also rich in magnesium and trace elements such as iron and zinc. The absorbance of the medium was observed after 7 days of culture and lysis of the cells. The results are given in FIG. 1. This clearly shows that the presence of a concentrate containing 1% by weight of coralline completely inhibited the transformation of the pre-adipocytes into adipocytes, and consequently the production of lipids by these cells since the absorbance observed in this case, namely 0.265 is similar to that observed in the absence of any induction (uninduced control), namely 0.269. These results also show that the action of coralline at 1% by weight is equal to that of 10-5M retinoic acid, a compound known for its effectiveness in inhibiting the transformation of pre-adipocytes into adipocytes, and for which a absorbance of 0.265 was noted. It will also be noted that the coralline used at only 0.50% by weight also has an effect since the absorbance observed in its presence is significantly lower than that observed in the case of the induced control. 1.2 Experiment No. 2 An experiment similar to that described above was carried out by comparing the effects of coralline concentrates at 1% and 2% by weight on the production of lipids, with reference no longer to retinoic acid, but to another compound also known to strongly inhibit the transformation of preadipocytes into adipocytes, namely Scopariane (manufactured and marketed by Depositor-reference E03-101 lot 240703SD) at a concentration of 2% by weight.

  The results are given in Figure 2.

  This shows that Coralline concentrate at 1% and 2% by weight has a significant effect on lipid production since the absorbance found in this case, namely respectively 0.213 and 0.199 is much greater than that observed for the control. induced, namely 0.277.

  This effect is certainly less than that observed with Scopariane at 2% for which an absorbance of 0.165 was recorded in the context of this experiment but remains very significant. 1.3 Experiment No. 3 In this third experiment, calcium was used, on the one hand, in accordance with the present invention, in the form of calcium chloride in a proportion of 100 g / ml of Caz +, and on the other hand, according to in the prior art, Scopariane at 2% by weight. In this context calcium chloride available from the Prolabo Company under the reference 22-313-394 was used.

  As for the experiments 1 and 2 described above, the absorbance of the medium was observed after 7 days of culture and lysis of the cells. The results are given in FIG. 3. This clearly shows that calcium chloride at a rate of 100 g / ml of Cal + inhibited lipid production by 55% since the absorbance observed in this case, namely 0.213 is much lower than that observed for the induced control, namely 0.275. This effect is certainly less than that observed with Scopariane at 2% for which an absorbance of 0.180 close to that observed with the uninduced control was noted but also remains very significant. 1.4 Experiment No. 4 For the sake of comparison, an experiment similar to experiment No. 3 was carried out by replacing the calcium chloride with magnesium chloride at 100 g / ml of Mg 2+. In this context, magnesium chloride obtained from the company Sigma (reference M2393 lot 86H08495) was used.

  As for the experiments 1 to 3 described above, the absorbance of the medium was observed after 7 days of culture and lysis of the cells. The results are given in FIG. 4. This FIG. 4 shows that the absorbance observed when magnesium chloride is added to the medium is quite similar to that observed on the induced control and that, therefore, this compound does not allow to inhibit the production of lipids. This experiment N 4 also proves that the effect observed during experiment n 3 is due to calcium and not to chloride ions. 2) Slimming composition for topical use The Applicant has developed, as a simple non-limiting example, the following composition of slimming gel for topical application according to the present invention: COMPOUND% by weight AQUA (water) 85,400 CYCLOMETHICONE 5,000 PROPYLENE GLYCOL 5,000 SODIUM POLYACRYLATE 1,100 PEG-40 HYDROGENATED CASTOR OIL 1,000 PHENOXYETHANOL 0,500 CYCLOPENTASILOXANE 0,425 METHYLPARABEN 0,300 DIMETHICONOL 0,075 BUTYLPARABEN 0,050 ETHYLPARABEN 0,050 ISOBUTYLPARABEN 0,050 PROPYLPARABEN 0,050 CORALLINA OFFICINALIS 1,00015

Claims (10)

  1. Use of calcium as an active ingredient for the production of cosmetic or pharmaceutical slimming compositions for topical use.   2. Use according to claim 1 of a natural compound containing calcium as active ingredient for the realization of cosmetic or pharmaceutical slimming compositions for topical use.   3. Use according to claim 2 characterized in that said natural compound is a water of marine source.   4. Use according to claim 2 characterized in that said natural compound is a plant extract containing bioavailable calcium.   5. Use according to claim 4 characterized in that said compound is an extract of at least one halophyte plant. 20   6. Use according to claim 5 characterized in that said halophyte plant is selected from the group consisting of salicornia, sea fennel, obione, soda.   7. Use according to claim 4 characterized in that said natural compound is an extract of at least one calcareous algae.   8. Use according to claim 7 characterized in that said natural compound is a coralline extract. 30   9. Use according to any one of claims 4 to 8 wherein said extract is a water-soluble extract.   10. Use according to any one of claims characterized in that said cosmetic or pharmaceutical composition comprises between 0.1 and 1000 mg / l of calcium.