DERMOTROPIC COSMETIC COMPOSITIONS

Abstract: Dermotropic cosmetic compositions are described, having a normalizing, trophic and moisturizing action and essentially comprising as the active agent, a mixture of acid­ ic mucopolysaccharides and umbilical cord extract, option­ ally in association with common additives and auxiliary sub­ stances used in the cosmetic field. These compositions are particularly useful in prevent­ ing and treating baldness.

Description: "DERMOTROPIC COSMETIC COMPOSITIONS" The present invention relates to new cosmetic compost tions endowed with entrophic and moisturizing properties to be applied to skin for preventing or rep airing ageing threwf. In partIcular, the present invention relates to new cosmetic compositions suitable for strengthening hair, preventing its falling out and stimulating hair growth. It is known that cutis, due to the particular functions to which it is devoted, is structured in a particular way and is substantially comprised of two superimposed layers, namely the underlying derma and the epidermis forming the external surface of cutis. As epidermis is devoid of blood vessels, even if it has to carry out many of the most remarkable functions of the skin, such as the protective, secretive, thermore gulating, respiratory functions, and so on, metabolic impairments often occur, affecting its appearance and jeopardising its functions, also in a serious manner. It also known that hair, as the essential part of the human piliferous apparatus, is planted in epidermis, so that it also shares in a very considerable way its vicissitudes and deficiencies, and therefore falling out of hair is a more and more frequent phenomenon both in men and in women, also in not typically pathological situations. The multifactorial aetiogenesis of such a falling out, having a developing course (stress, atmospheric pollution, emotional factors, washing with strongly detergent shampoos, hormonal factors, etc.) is always connectable with a morphological alteration of the connective tissue surrounding the hair bulb which is determined, inter alia, by the decrease of specific acidic mucopolysaccharides (heparin, hyaluronic acid, A, B, C, chondroitinsulphates) in the connective tissue itself, with dehydration, consequent ageing of the tissue and dekeratinisation, together with fragility and poor elasticity of hair, and then sclerosis and death of the hair bulb. In order to prevent ageing of cutis and, particularly, falling out of hair, different criteria have been followed till now, such as the local use of degreasing, rubefacient and vasodilating agents, polyvitaminic compositions and vegatable extracts of different kinds, as well as mucopolysaccharide extracts with unspecified compositions and activity (with particular reference to the anticoagulant and lipasemic-activities, which are closely correlated and interdependent activities) alone or in combination. However, none of these compounds has ever faced in a rational way, and consequently solved, the problem of physiological hydration of cutis and of the tissue surrounding the hair bulb, which, as above mentioned, is an essential condition for the vitality of the bulb itself and of hair. Even if the use of sulphomucopolysaccharides, which notoriously possess hydrophilic properties, is already known, it is likewise known that they usually are substan tially not absorbed through cutis. The applicant has now discovered that it is possible to provoke and facilitate the cutaneous absorption of mucopolysaccharides by mixing them with an umbilical cord extract, which is notoriusly rich in chondroitinsul phates and hyaluronic acid, obtained under particular conditions. The purpose of this invention is therefore to produce a preparation substantially based on mucopolysaccharides (MPS) and extract of umbilical cord (ECO), able to promo te, by topical application, the hydration and trophism of skin, and particularly of hair. The present invention is based on the ascertainment that an extract of umbilical cord, besides possessing its own high hydrophilic and hydrating properties, allows the absorption of the essential MPS by skin, owing to the presence of the peptide chains of proteohyaluronic acid therein contained, which, by promoting an increase in the peripheral blood microcirculation, allows an effective absorption of the aforesaid substances. A further problem solved by this invention is that of choosing the acidic mucopolysaccharides which have to be supplied to skin and must be such as to correct the typical deficiency of these substances occurring in concomitance with falling out of hair and ageing of cutis. The MPSs chosen for topic application have furthermore to act, through their clarifying (i.e. anticoagulating/normolipe mising) activity, as regulators for the sebaceous secretion which is a contributory cause of hair weakening and of sclerosis of hair bulb, all causes bringing to the common baldness or androgenetical or seborrhoical alopecia. The complex of extractive acidic mucopolysaccharides of animal origin according to this invention is rich in chondroitinsulphates and heparin-like substances and is characterised by the following essential analytical parameters: pH in 5% aqueous solution : 5 to 7.5 rotatory power : 0 to +150 proteins : absent total N : < 4.5% S : > 6% inorganic P : < 0.5% hexuronic acids : > 20% hexosamines : > 20% anticoagulating activity : 40-50/mg I.U. USP, XX The extract of umbilical cord to be mixed with the MPSs according to this invention is an aqueous extract of human or animal umbilical cord containing, on average, 5 to 7 g/litre of hyaluronic acid, principally in the form of proteohyaluronic acid (proteoglycane), and containing, moreover, C chondroitinsulphate. The hyaluronic acid, as contained in this extract, shows a molecular weight between 2.5 and 3 million. An aqueous extract of human umbilical cord shows, for instance, the following essential analytical features: viscous, transparent, slightly yellowish solution Ph : 5 to 7 viscosity at 300C : 10 to 25 centistokes residue at evaporation : 2 to 3% hyaluronic acid titre : 500 to 700 mg/dl ashes : 0.1 to 0.5% S : absent proteins : 0.5 to 1.0% total N : 0.15 to 0.30% aminic N : 0.10 to 0.20% hexosamines : 0.010 to 0.050% The process for obtaining the extract of umbilical cord according to the invention is as follows: A certain quantity of umbilical cord is washed with water, crumbled by means of a triturator and conveyed into a mixer, to which a volume of water twice as much as that of the crumbled tissue is added. The obtained aqueous mush is milled and the whole is well mixed at low temperature. The mixed suspension is then filtered and the filtrate is concentrated at reduced pressure and low temperature. 4.5% of methyl-para-hydroxybenzoate and 0.5% of propyl-parahydroxybenzoate are separately dissolved in a volume of ethanol equivalent to 5% by volume of the concentrated solution. The two solutions are mixed and filtered, and the filtrate is then sterilized by filtration through a membrane. The sterilized solution is at last closed into hermetic vessels for subsequent use. The enclosed figures 1 and 2 show the graphs obtained from two samples of extract of umbilical cord according to the present invention by high speed gas-chromatography with a mobile phase consisting of an aqueous solution of KC1 0.1M buffeered at pH 7.0 with a solution of phosphate 1/15M; figure 3 shows the gas-chromatographic graph obtained from a standard solution containing blue dextran 2000, gammaglobulin, lactoalbumin, eggalbumin, myoglubulin and alanine in the same operational conditions. The following examples, which by no means have te be considered as limiting, illustrate the particular properties of moisture retention shown by extracts of human umbilical cord which have been used in the formulations according to the present invention, in comparison with similar properties shown by other known substances having similar characteristics. EXAMPLE 1 The tests were carried out by using the following materials: A) Extract of human umbilical cord (HA) with residue at evaporation = 2.238 B) Solution of sodium chondroitinsulphate (CS-Na) with residue at evaporation = 3.0% C) Solution of sodium pyrrolidonecarboxylate (PCA-Na) with residue at evaporation = 3.08 Carefully weighed samples of 20 g of A, B and C, respectively placed in glass capsules having an inside diameter of 85 mm and a depth of 20 mm, were put into a drier adjusted at 300C and 80% of relative humidity. The so prepared samples were then weighed every 24 hours so as to evaluate the undergone weight changes. The hydrating effect was obtained on the basis of the following ratio: Hydrating effect (8) = Residual water x x 100 Residue at evaporation The obtained results are shown in the following Table 1 and schematically illustrated in the relevant graph 1. TABLE 1 EMI7.1 <tb> <SEP> Days <tb> Sample <tb> <SEP> 1 <SEP> 2 <SEP> 3 <SEP> 4 <SEP> 5 <tb> <SEP> Residue <SEP> at <SEP> evapora <SEP> 446 <SEP> mg <SEP> 4116 <SEP> mg <SEP> 446 <SEP> mg <SEP> 446 <SEP> mg <SEP> 446 <SEP> mg <tb> <SEP> tion <tb> <SEP> A <tb> <SEP> Residual <SEP> water <SEP> 4254 <SEP> nig <SEP> 1854 <SEP> mg <SEP> 554 <SEP> mg <SEP> 554 <SEP> mg <SEP> 554 <SEP> ing <SEP> <tb> <SEP> Hydrating <SEP> effect <SEP> (%) <SEP> 953.8% <SEP> 415.7% <SEP> 124.2% <SEP> 124.2% <SEP> 124.2% <tb> <SEP> Residue <SEP> at <SEP> evapora <SEP> 600 <SEP> mg <SEP> 600 <SEP> mg <SEP> 600 <SEP> mg <SEP> 600 <SEP> mg <SEP> 600 <SEP> mg <tb> <SEP> tion <tb> <SEP> B <tb> <SEP> Residual <SEP> water <SEP> 1400 <SEP> mg <SEP> 200 <SEP> mg <SEP> 100 <SEP> mg <SEP> 100 <SEP> mg <SEP> 100 <SEP> mg <tb> <SEP> Hydrating <SEP> effect <SEP> (z) <SEP> 233.3% <SEP> 33.3% <SEP> 16.6% <SEP> 16.6S <SEP> 16.6% <tb> <SEP> Residue <SEP> at <SEP> evapora <SEP> 600 <SEP> mg <SEP> - <SEP> 600 <SEP> mg <SEP> 600 <SEP> mg <SEP> 600 <SEP> mg <SEP> 600 <SEP> mg <SEP> <tb> <SEP> tion <tb> <SEP> Residual <SEP> water <SEP> 4800 <SEP> mg <SEP> 2400 <SEP> mg <SEP> 500 <SEP> mg <SEP> 447 <SEP> mg <SEP> 363 <SEP> mg <SEP> <tb> <SEP> Hydrating <SEP> effect <SEP> (%) <SEP> 800.0% <SEP> 400.0% <SEP> 83.3% <SEP> 74.5S <SEP> 60.5S <SEP> <tb> EXAMPLE 2 Tests similar to those of Example 1 were carried out on the same substances A, B and C, and, furthermore, on the following substance: : D) A solution of sorbite (SORB) with residue at evapora tion = 3.0% Some samples of l.0g of substances A, B, C and D, respectively collected into glass vessels with a diameter of 30 mm and depth of 30 mm, were put into a drier in the presence of a saturated solution of K"CO . The sam 23 ples so treated were then weighed after 1, 2, 3, 5, 8, 24, 32 and 48 hours so as to record the undergone weight changes. The hydrating effect was calculated on the basis of the ratio reported in Example 1. The obtained results are shown in the following Table 2 and schematically illustrated in the corresponding graph 2. TABLE 2 EMI9.1 <tb> <SEP> Tire <SEP> Sample <SEP> A <SEP> B <SEP> C <SEP> D <tb> <SEP> Residual <SEP> water <SEP> (mg) <SEP> 912.9 <SEP> 931.5 <SEP> 989.7 <SEP> 986.4 <tb> 3 <SEP> hours <tb> <SEP> O <SEP> hours <SEP> Residue <SEP> at <SEP> evapora- <SEP> 20.25 <SEP> 28.81 <SEP> 30.61 <SEP> 30.51 <tb> <SEP> tion <SEP> (mg) <tb> <SEP> Residual <SEP> water <SEP> (mg) <SEP> 901.2 <SEP> 921.7 <SEP> 980.7 <SEP> 975.8 <tb> 1 <SEP> hours <SEP> Hydrating <SEP> effect <SEP> (t) <SEP> 4450.5 <SEP> 3199.3 <SEP> 3203.9 <SEP> 3198.6 <tb> 2 <SEP> hours <SEP> Residual <SEP> water <SEP> (mg) <SEP> 885.2 <SEP> 909.4 <SEP> 969.8 <SEP> 967.4 <tb> <SEP> Hydrating <SEP> effect <SEP> (z) <SEP> 4371.0 <SEP> 3156,6 <SEP> 3168.3 <SEP> 3171.1 <tb> <SEP> Residtal <SEP> water <SEP> (mug) <SEP> 868.5 <SEP> 897.3 <SEP> 957.6 <SEP> 952.5 <tb> 3 <SEP> hours <tb> <SEP> ydratiIng <SEP> effect <SEP> () <SEP> 4288.6 <SEP> 3114,6 <SEP> 3128,5 <SEP> 3122'. <SEP> 3 <tb> <SEP> Rsidual <SEP> water <SEP> (mg) <SEP> 36,9 <SEP> 872.6 <SEP> 933.0927.4 <tb> <SEP> Hydrating <SEP> effect-(z) <SEP> 4132,5 <SEP> 3028.9 <SEP> -3048.1 <SEP> 3039.9 <tb> <SEP> Ydrating <tb> 8 <SEP> hours <SEP> Residual <SEP> water <SEP> (n) <SEP> 788.1 <SEP> 830.4 <SEP> 892.3 <SEP> 883.9 <tb> <SEP> Hydrating <SEP> effect <SEP> (z) <SEP> 3892.0 <SEP> 2882.4 <SEP> 2915.1 <SEP> 2897.3 <tb> <SEP> i <SEP> Residual <SEP> water <SEP> mg) <SEP> 555.6 <SEP> 591.5 <SEP> 657.4 <SEP> 658. <SEP> 1 <tb> 24 <SEP> hour:; <tb> <SEP> Hydrating <SEP> effect <SEP> ($) <SEP> 2743.9 <SEP> 2053,2 <SEP> 2147.7 <SEP> 2157.2 <tb> <SEP> Hydrating <SEP> effect <SEP> (z) <SEP> 2213.0 <SEP> 1654.0 <SEP> 1756.3 <SEP> 1740.6 <tb> 48 <SEP> hour <SEP> Residual <SEP> water <SEP> (mg) <SEP> 225.4 <SEP> 244.5 <SEP> 305.7 <SEP> 295.0 <tb> <SEP> Hydrating <SEP> effect <SEP> (z) <SEP> 1112.8 <SEP> 848.7 <SEP> 998.7 <SEP> 967.0 <tb> From the above shown and illustrated data it is clear that the extract of human umbilical cord, used according to this invention, shows water retention effects which are decidedly higher than those of substances already known for their properties of absorbing and retaining water. The mixtures of umbilical cord extract and mucopolysaccharide complex according to this invention normally contain also other active elements, adjuvants or additi ves, such as for instance vasodilators, preservatives, wetting agents, fungicidal agents, surfactants, bactericides, vitamins, pH regulating agents, etc. Some examples of presently preferred formulations, according to this invention are hereinafter given in the form of numerical data. EXAMPLE 3 Lotion for treating the scalp Extract of umbilical cord mg 120.00 Mucopolys accharide complex mg 8.58 Tetrahydrofurfuryl-nicotinate mg 4.50 Propyleneglycol mg 0.20 Methylparaben mg 8.10 Propylparaben mg 3.90 Sorbic acid mg 6.00 Sodium pantothenate mg 6.00 Biotin mg 0.15 Ethanol mg 0.44 Perfume q. s. Distilled water q.s. to ml 6.00 The above given formulation is prepared in the form of vials. EXAMPLE 4 Face moisturizing lotion Mucopolysaccharidic complex g 0.3 Extract of umbilical cord g 2.0 dl-a-tocopherol g 0.5 Ethanol g 13.0 Glycerine g 2.0 Propyleneglycol g 5.0 Polyoxyethylenesorbitane monolaurate (20 E.O.) g 2.0 Polyethyleneglycol monostearate g 1.0 Methylparaben g 0.2 Propylparaben g 0.1 Perfume q .s. PurifIed water q.s. to g 100 EXAMPLE 5 Face moisturizing cream Mucopolysaccharide complex g 2.0 Potassium glycerinizate g 0.1 dl-a-tocopherol acetate g 0.05 Extract of umbilical cord g 3.0 Squalene g 8.0 White vaseline g 3.0 Amitel LG-OD (di-2-octyldodecyl-N lauroyl-L-glutamat0) g 5.0 White wax g 1.0 Glyceryl-monostearate g 1.0 Propyleneglycol monostearate g 4.0 Sorbitane monostearate g 4.0 N-acyl-L-sodium-glutamate g 0.2 Solution of sorbitol (70%) g 5.0 Glycerin g 2.0 Stearic acid g 2.0 Silicone resin g 0.5 Propylparaben g 0.1 Methylparaben g 0.2 Perfume g 0.05 Purified water q.s. to g 100 EXAMPLE 6 Anticellulitis cream Stearic acid g 15.0 Cetyl palmitate g 8.0 anhydrous lanolin g 4.0 n-propyl p-oxybenzoate g 0.1 Tween 80 g 2.5 1.2-propylene glycol g 5.0 Triethanolamine g 2.0 Methyl p-oxybenzoate g 0.2 Mucopolysaccharide complex g 0.3 Escin g 1.0 Tetrahydrofurfuryl-nicotinate g 0.05 Distilled water g 61.0 Extract of umbilical cord g 1.0 Perfume 3 drops The weight ratio of the umbilical cord extract to the mucopolysaccharide complex contained in the formulations according to this invention ranges from about 1:1 to about 15:1. The cosmetic formulations according to this invention are characterized by a number of properties which may be resumed as follows: Remarkable hydrating effect on cutis, which avoids the dehydratation of the horny layer, retains water, prevents dandruff, reduces statical electricity of hair making easier the action of the comb, increases hair elasticity making hair softer; ability to form membranes having greater strength and elasticity than those obtained with other products as polyvinyl alcohol, polyvinyl pyrrolidone or gelatine, and that increases the hydrating effect and facilitates the action of the comb; improvement of the subcutaneous microcirculation through topical peripheral vasodilation and permanent action on the connective tissue; antibacterial activity due to a phenomenon of anionic repulsion which is typical of the extract of umbilical cord, with consequent hindran ce to the dandruff formation. The sum of these properties and characteristics allows therefore to extend the use of the formulations according to this invention to all the morphological alterations of the subcutaneous connective tissue, which are characteristic of premature ageing of skin in different cutaneous districts. Therefore, both active agents, convenient ly chosen and mixed according to this invention (extract of umbilical cord and mucopolysaccharide complex) and rightly conveyed and combined with other substances, differentiated according to the use and the concerned district, may be usefully employed in the different forms of chronic alopecia and particularly in the androgenetic and seborrhoic alopecia, in the treatment of dry and arid skins in order to avoid the formation of wrinkles or to attenuate the already formed wrinkles, in the topical treatment of cellulitis, owing to the vasodilating action and metabolic activation which fa vours the elimination of adipose cushions, as well as in every other non-pathological skin unaesthetisms as they are sustained, in most cases, by an insufficient water content of derm. Although this invention has been described on the basis of some of its preferred embodiments, it is obvious that changes and/or variations can be made by those skilled in the art, without departing from the gist and scope of the invention.

Claims: CLAIMS 1. Dermotropic cosmetic compositions comprising mucopolysaccharide complexes, characterized in that the said mucopolysaccharide complexes are mixed with an aqueous extract of umbilical cord. 2. Cosmetic compositions according to claim 1, characterized in that the said mucopolysaccharide complexes do not contain proteins, have a pH ranging between 5 and 7.5 in 5% aqueous solution, a rotatory power between O and 150 and a sulphur content higher than 6%. 3. Cosmetic compositions according to claim 1, characterized in that the extract of umbilical cord is free from sulphur and has a pH between 5 and 7, a viscosity at 300C between 10 and 25 centistokes, a hyaluronic acid titre ranging from about 500 to 700 mg/dl and an ash content not higher than 0.5%. 4. Cosmetic compositions according to claim 3, characterized in that the said hyaluronic acid has a molecular weight between 2.5 and 3 million. 5. Cosmetic compositions according to claim 1, characterized in that the weight ratio between said aqueous extract of umbilical cord and said mucopolysaccharide complexes ranges between 1:1 and 15.1. 6. Cosmetic compositions according to claim 1, characterized in that they contain, besides the said mucopo lysaccharide complexes and aqueous extract of umbilical cord, also auxiliary substances, additives, drugs and other active agents. 7. Use of the cosmetic compositions according to any of the preceding claims for the treatment of chronic alopecia. 8. Use of the cosmetic compositions according to any of claims 1 to 6 for the treatment of cutaneous unaesthetisms.

Inventors: CASERO, ALESSANDRO, CASERO, RICCARDO
Applicants: FARMAKA S.R.L.
Application year: 1985
Main classification: A61K7
IPC codes: A61K8, A61Q7, A61Q5