UNITRIENOL T-27 UNITRIENOL T-272 WSL

Transcription

1 UITRIEL T-27 UITRIEL T-272 WSL IL SLUBLE R WATER SLUBLE BIACTIVE AGET CMPLEX WIT CELL REGEERATIG PRPERTIES FR TE PREPARATI F IG QUALITY CSMETIC CARE PRDUCTS WIT TE FLLWIG EFFECTS: SMTIG F WRIKLES IMPRVEMET F SKI ELASTICITY ICREASE F SKI MISTURE REGULATI F SEBACEUS MATTER FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

2 UITRIEL T-27/T-272 WSL Contents 1. Introduction Concept of the Agent Complex Unitrienol T Mode of Action Evidence of Effectiveness Measurement of Wrinkles Assessment of Skin Roughness Measurement of the Elasticity of the Skin Measurement of the Moisture Content of the Skin Measurement of Skin Sebum Summary of the Experimental Results Characteristics of Unitrienol T-27 (oil soluble) Characteristics of Unitrienol T-272 wsl (water soluble) References FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

3 UITRIEL T-27/T-272 WSL 1. Introduction ne of the most important processes occurring in our skin is regeneration. The only way in which the skin can become more youthful or younger is by intensifying skin renewal. Skin renewal is a continuous process. The intensity of regeneration of the cells their quantity and their structure govern the elasticity, plasticity, wrinkling and the condition of the skin. In a young skin, this natural regeneration process is so intensive that the entire epidermis is renewed, i.e. rejuvenated, within 22 to 28 days. Age and environmental effects reduce the renewal of skin cells as a result of a decrease in metabolic activity. The number of skin cells decreases and the cells themselves become increasingly inelastic, smaller and thinner; which is why the skin also becomes thinner, more wrinkled, tired-looking and rough. Modern scientific cosmetic care endeavours to delay the changes and substance displacements occurring in the skin due to age and environmental effects; replenish or compensate the missing substances; and actively preserve the healthy condition of the skin. The specific cosmetic application of specific organic agents makes it possible to maintain the natural balance of the skin metabolism and its activity. 2. Concept of the Agent Complex Unitrienol T-27 In nature and living things, substances are found which can be described as versatile, eg. multiple-effect, bioactivators. These bioactivators organise or influence the normal development of vital processes. The development of the agent complex Unitrienol T-27 has made it possible to provide such bioactivators in optimised proportions for the formulation of modern cosmetic care products with cell-regenerating properties. The objective of this novel product, Unitrienol T-27, is to provide the cosmetic chemist with a polypotent agent complex making it possible to prepare high-quality skin care products, which on the one hand delay skin ageing in a natural way through improved regeneration, and on the other hand simultaneously regulate or normalise the skin s moisture and sebaceous matter balance and hence smooth out wrinkles. It has been possible to achieve this extremely ambitious aim with the optimised combination contained in the agent complex Unitrienol T-27, consisting of farnesol, a farnesol derivate and a panthenol derivate. FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

4 UITRIEL T-27/T-272 WSL 3. Mode of Action Farnesol and farnesol derivates are natural substances of high biological potency which are also found in this form as bioactivators in human skin [1]. These components are therefore absorbed by the skin and can thus develop their effect to the full. Even the butterfly, for example, owes its beauty to such bioactivators. These natural substances determine, control and regulate the development of a butterfly from birth until its glorious colors have fully developed [2-6]. Farnesol and farnesol derivates are widespread in the plant world. They have been detected in countless flower oils and other ethereal oils [7]. For example, in lime blossom oil, acacia blossom oil, rose oil, in the flower oils from the lily of the valley, lilac, orange etc., in musk seed oil, sandalwood oil and so on. Substances of this type have also been detected in champagne [1]. The farnesol content is an important quality factor in the bouquet of a champagne. FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

5 UITRIEL T-27/T-272 WSL Farnesol and farnesol derivates are compounds and intermediates in the sterol biosynthesis taking place in the skin [1]. The starting material for sterol biosynthesis is acetic acid in the activated form of acetyl coenzyme A. Two molecules of acetyl coenzyme A condense to acetoacetyl coenzyme A in the following way: 2x CoA S S + SCoA CoA Figure 1: Formation of acetoacetyl-coa The acetoacetyl-coa condenses with a further molecule of acetyl-coenzyme A at the keto group, and ß-hydroxy-ß-methylglutaric acid-coenzyme A is formed with the elimination of one molecule of coenzyme A: S CoA S CoA C 3 C S CoA + + SCoA Figure 2: Formation of ß-hydroxy-ß-methylglutaric acid-coenzyme A In a further step the CoA group is eliminated and the carboxyl group is converted to the alcohol, consuming 2 ADP : 2 ADP ADP + C 3 C S CoA C 3 C C 2 + CoA Figure 3: Formation of mevalonic acid ADP = reduced nicotinamide adenine dinucleotide phosphate ADP + = nicotinamide adenine dinucleotide phosphate FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

6 UITRIEL T-27/T-272 WSL The mevalonic acid formed is converted to active isoprene (isopentenyl pyrophosphate) via several stages. By the successive condensation of three active isoprenes farnesyl pyrophosphate is formed. C 3 C C 2 3 ATP 3 ADP + P i + C2 P P Isopentyl pyrophosphate Isopentenyl PP i PP i Isopentenyl PP i PP i PP i = Pyrophosphate group P i = Phosphate group Farnesyl pyrophosphate P P Figure 4: The formation and conversion of active isoprene The condensation of two molecules of farnesyl pyrophosphate produces squalene: 2x P ADP P ADP + + 2PP i Figure 5: The production of Squalene FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

7 UITRIEL T-27/T-272 WSL The squalene chain, folded in a particular way by intermediate stages, is transformed to Lanosterol by hydroxylation and cyclization. Lanosterol is converted to cholesterol by the oxidative elimination of three methyl groups. Cholesterol forms the basis of all steroids. Squalene Lanosterol Cholesterol Figure 6: The formation of cholesterol FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

8 UITRIEL T-27/T-272 WSL It has been possible to prove the further steroid biosynthesis which follows, the pathway and the individual steps of steroid metabolism which lead to the formation of estrogen [8, 9]: Cholesterol Pregnenolone Progesterone Desoxycorticosterone 17 -ydroxy- progesterone 17 -ydroxy- pregnenolone Aldosterone 11-Desoxy- hydrocortisone 4 -Androsten- dione Dehydroepiandrosterone ydrocortisone Testosterone 5 -Androstenediol Estrogens Figure 7: The pathway of steroid metabolism FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

9 UITRIEL T-27/T-272 WSL Panthenol and panthenol derivates are converted to pantothenic acid after application to the skin in vivo. owever, this conversion takes place considerably more slowly in the case of the panthenol derivative contained in Unitrienol T-27 than in the case of panthenol, i.e. it displays a sustained action or depot effect. Pantothenic acid is classed as part of the vitamin B complex [10] and is a characteristic natural product of the human metabolism. C Figure 8: Pantothenic acid Pantothenic acid is one of several precursor substances forming coenzyme A, which is an important cofactor for acylation reactions in numerous biochemical processes in the body [11]. Coenzyme A also plays a decisive part in the cholesterol synthesis described above. 2 Adenine C S Cysteamine Pantothenic acid P P C P Ribosephosphate Pantetheine Figure 9: Coenzyme A FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

10 UITRIEL T-27/T-272 WSL The biosynthesis of coenzyme A starting from pantothenic acid proceeds according to the following scheme [12]: 2 C Pantothenic Acid C ATP ADP P 4'-Phosphopantothenic Acid C S C ATP 2 Cysteine ADP + P i P C S 4'-Phosphopantothenylcysteine C 2 P 4'-Phosphopantetheine S ATP PP i P P 2 S ATP ADP Dephosphocoenzyme A Coenzyme A Figure 10: The biosynthesis of coenzyme A FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

11 UITRIEL T-27/T-272 WSL Pantothenic acid is essential for the synthesis and natural function of the skin. It penetrates the lower cell layers of the skin, stimulates cell formation [13] and accelerates cell regeneration [14]. Pantothenic acid furthermore increases the moisture retention capacity of the skin [15]. This improves the tonicity of the skin, tightens loose skin, reduces wrinkling and makes the skin visibly smoother. By means of dermatological and experimental tests and measurements, it has been possible to show unambiguously that the regenerative processes in the skin are enhanced by the action of Unitrienol T-27 (see section 4). Cell division and cell proliferation, or the rejuvenation of the cells, are activated. In other words, Unitrienol T-27 effectively delays the skin modifications due to ageing. The components present in Unitrienol T-27 also have a relaxing, soothing and antiinflammatory action on tired skin, resulting in a particularly beneficial effect [16-19]. In general, the effects of Unitrienol T-27 add up to an increase in the ability of the cells to develop and function, and an increase in the regenerative power and resistance of the tissue, consequently resulting in an active rejuvenation of the skin. FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

12 UITRIEL T-27/T-272 WSL 4. Evidence of Effectiveness The activity of Unitrienol T-27 - integrated in standard test creams - was verified by means of extensive clinical tests. 4.1 Measurement of Wrinkles The experiments relating to the influence on wrinkle depth and wrinkle width were carried out in accordance with the method (profilometry) described by. Tronnier [20]. The initial values of the wrinkle depth and wrinkle width in the region of the corner of the eye were measured on twenty test subjects. The treatment was then applied twice a day for a total of twenty-eight days, on the right forehead with a preparation containing Unitrienol T-27 and on the left forehead with the same cream base not containing the agent complex. At the end of the experimental period, the measurements showed that both, wrinkle width and wrinkle depth had been reduced by 5-7% in the case of application of the cream not containing the agent complex, whereas a reduction of more than 17% had been achieved in the case of application of the cream containing Unitrienol T Assessment of Skin Roughness The experiments relating to the influence on the roughness values of the skin were carried out in accordance with the method of Prof. Dr. med. G. opf (Skin Clinic of the eidberg General ospital, amburg). 66 subjects, divided into two groups, were treated twice a day with a face cream containing Unitrienol T-27 or with the same cream base not containing the agent complex, in a double-blind trial over a period of thirty days. After 14, 21 and 30 days, the wrinkle depth and number of wrinkles were assessed by means of the roughness factor. The results are shown in Figure 11. The roughness of the skin (wrinkle depth and number of wrinkles) in the case of application of the cream containing Unitrienol T-27 was reduced by 28% after 14 days, 51% after 21 days and 64% after 30 days. FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

13 UITRIEL T-27/T-272 WSL Figure 11: Roughness values of the skin, i. e. wrinkle depth and number of wrinkles, after application of a cosmetic cream with and without Unitrienol T-27 FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

14 UITRIEL T-27/T-272 WSL 4.3 Measurement of the Elasticity of the Skin These measurements were carried out in accordance with the method described by. Tronnier and.. Wagener [21]. The principle of the measurement is that one of two measuring probes placed on the skin transmits a variable frequency and the other absorbs and records part of the intensity. The higher the elasticity and/or the water content of the skin, the lower is the frequency at which the whole system resonates. Thus, a drop in the resonant frequency (negative values) corresponds to a better elasticity and/or an increased water content of the horny layer, while an increase (positive values) is to be evaluated in terms of elasticity decrease or drying. The measurements were carried out on ten subjects at ten-minute intervals for sixty minutes before and after the application of a care preparation containing Unitrienol T-27. The measured values are shown in Figure 12. There is an immediate improvement in the mechanical properties of the skin after application of the cream containing Unitrienol T Elasticity in z Time in minutes after application before treatment after treatment before treatment after treatment Figure 12: Elasticity and basic tonicity of the skin before and after application of the cream containing Unitrienol T-27 FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

15 UITRIEL T-27/T-272 WSL 4.4 Measurement of the Moisture Content of the Skin The measurements were carried out with Bingmer s dermatometer in accordance with the method of A. Winkler and.. Wagener [22].This apparatus - designed according to the principle of the stray field capacitor - makes it possible to determine the relevant water content of the upper dermal layers. The moisture retention capacity of the skin, increased by a preparation, can be determined by means of repeated measurements over a period of a few hours. The water content of young elastic skin is 10-12%, which corresponds on the measuring apparatus to a value of scale divisions. An extremely dry skin containing about 6% water shows scale divisions in the measurements. The tests were carried out on a total of forty subjects with predominantly dry skin. First the mean base values were determined and then the areas treated with a preparation containing Unitrienol T-27 and with the cream base not containing the agent complex were measured over a period of a few hours. These measured values are shown in Figure 13. The moisture retention capacity of the skin persists for twice as long with the cream containing Unitrienol T-27 as with the cream not containing the agent complex. Figure 13: Moisture content of the skin after application of test creams FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

16 UITRIEL T-27/T-272 WSL 4.5 Measurement of Skin Sebum The quantity of sebaceous matter on the skin surface was measured with a sebumeter in accordance with the method developed by. Schaefer and. Kuhn-Bussins [23]. The principle of the method is based on the fact that when roughened glass or roughened plastic film is pressed against the skin it absorbs grease from the latter and thereby becomes transparent. The degree of transparency depends on the amount of grease on the skin and is measured photometrically. The sebumeter is in principle a grease spot photometer. By pressing a matte plastic strip against the skin some of the latter s grease is taken up and can be photometrically measured by the brightening effect it produces on the roughened glass. Twenty subjects with a high content of sebaceous matter in the skin and twenty subjects with dry skin were selected and treated twice a day for 45 days with a cream containing Unitrienol T- 27. After cessation of the treatment, the content of sebaceous matter in the skin was observed for a further 35 days. The measured values are shown in Figure 14. When a cream containing Unitrienol T-27 is applied, the content of sebaceous matter returns to normal in both cases, greasy and dry skin. The normalisation of the content of sebaceous matter in the skin also persists after cessation of the treatment. Sebum content of the skin Duration of treatment (45 days) Persisting action after stopping the treatment greasy skin dry skin Days Figure 14: Content of sebaceous matter in the skin after application of a cosmetic cream with Unitrienol T-27 FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

17 UITRIEL T-27/T-272 WSL 4.6 Summary of the Experimental Results The activity experiments performed clearly show that the agent complex Unitrienol T-27 has skin-normalising properties in the modern cosmetological sense. In particular, it has been possible to show that preparations containing Unitrienol T-27 smooth out wrinkles improve the elasticity of the skin improve the moisture retention capacity of the skin normalise the content of sebaceous matter in the skin FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

18 UITRIEL T-27/T-272 WSL 5. Characteristics of Unitrienol T-27 (oil soluble) Composition Appearance Analytical data Solubility Properties Unitrienol T-27 contains no solvents or excipients of any kind and thus has a total active content of 100% consisting of farnesol, a farnesol derivative and a panthenol derivative in optimized proportions. Slightly viscous liquid See specifications. Readily soluble in ethanol (80-90%), isopropyl myristate, propylene glycol, polyethylene glycol, Cetiol V, Miglyol 812 and vegetable oils. Insoluble in water. Development of the agent complex Unitrienol T-27 has made it possible to provide polypotent bioactivators in optimized proportions for the formulation of modern cosmetic care products with cell regenerating properties and scientifically supported efficiency. Extensive activity tests clearly demonstrated that Unitrienol T-27 has skin normalizing properties in the modern cosmetic sense. Preparations containing Unitrienol T-27 have given the following effects when applied regularly: Activation of the renewal of the epithelial cells (epidermal cells) and the regenerative processes in the sense of rejuvenation Improvement in the mechanical properties of the skin (elasticity and plasticity) by increasing the tissue tonicity. Smoothing of the skin. Action against wrinkles, and flaccid and inelastic skin. ormalization of the oil content of the skin Improvement in the moisture retention capacity of the skin. Unitrienol T-27 is non toxic and has very good skin tolerance. FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

19 UITRIEL T-27/T-272 WSL Use Unitrienol T-27 is a high quality agent complex for cosmetic care products. Because of its solubility in oil, Unitrienol T-27 can be used in formulations such as emulsions (/W and W/), lotions, oils or sticks. Dosage 2-8% Storage Storage conditions: see safety data sheet Shelf life: see specifications Identification ICI name CAS-o. Farnesyl Acetate Farnesol Panthenyl Triacetate FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

20 UITRIEL T-27/T-272 WSL 6. Characteristics of Unitrienol T-272 wsl (water soluble) Composition Appearence Analytical data Solubility Properties Unitrienol T-272 wsl contains 33.4% active ingredients in the form of an optimally coordinated complex consisting of farnesol and farnesol derivative and a panthenol derivative. The remainder is made up of a highly efficient solubilizer complex which converts the lipophilic active ingredients into a water soluble form. Slightly viscous liquid See specifications. Soluble in water, aqueous and pure ethanol, aqueous propylene glycol and glycerol. The bioactive properties of Unitrienol T-272 wsl have been demonstrated with the aid of extensive activity studies and are described in detail in the Unitrienol T-27 documentation. Because of its solubilizer content, Unitrienol T-272 wsl is soluble in aqueous systems to give a clear solution. It is therefore possible for the exceptional properties of Unitrienol T-27 summarized briefly below, also to be utilized in hydrophilic media: Activation of the renewal of epidermal cells and the regenerative processes in the sense of rejuvenation. Improvement in the mechanical properties of the skin (elasticity and plasticity) by increasing the tissue tonicity. Smoothing of the skin. Action against wrinkles, and flaccid and inelastic skin. ormalization of the oil content of the skin Improvement in the moisture retention capacity of the skin. Unitrienol T-272 wsl is non toxic and tolerated by the skin without problem. FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

21 UITRIEL T-27/T-272 WSL Use Because of its hydrophilic properties, Unitrienol T-272 wsl is specifically suitable for incorporation into aqueous and hydroalcoholic skin and hair care products (hair lotions, hair tinctures, shampoos, shaving lotions etc.) Dosage 2-10% Storage 15 C - 25 C (see safety data sheet) Shelf life 2 years (see specification) Identification ICI name CAS o. PEG-12 Glyceryl Laurate PEG-36 Castor il Farnesyl Acetate Farnesol Panthenyl Triacetate FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22

22 UITRIEL T-27/T-272 WSL 7. References ** 1. Stryer, L.. Biochemie, pp Spektrum Akademischer Verlag, eidelberg (1994). 2. Karlson, P. Kurzes Lehrbuch der Biochemie, pp Georg Thieme Verlag, Stuttgart (1970). 3. Schmialek, P. Z. aturforsch. 18b, (1963). 4. Stein, G. Der aturwissenschaftler 50, 7, 305 (1963). 5. Dearden, M. J. Ins. Physiol. 10, (1964). 6. Trost, B.M. et al. J. rg. Chem. 40, 24, (1975). 7. Karrer, W. Konstitution und Vorkommen der organischen Pflanzenstoff, pp. 57. Birkhäuser Verlag, Basel (1958). 8. errmann, F. et al. Biochemie der aut, pp Georg Thieme Verlag, Stuttgart (1973). 9. Stüttgen, G. et al. Funktionelle Dermatologie, pp Springer Verlag, Berlin (1974). 10. ennies, K. Riechst. Aromen, Körperpflegem. 23, 8, (1973). 11. Korting, G.W. Dermatologie in Praxis und Klinik, Bd. III, Georg Thieme Verlag, Stuttgart (1979). 12. Brown, G.M. et al. Rev. Biochem. 32, (1963). 13. Korner, W.F. et al. Cosmet. and Perf. 89, 11, 35 9 (1974). 14. Mouchette, R. Rend. Soc. Biol. 147, (1953). 15. Idson, B. Cosmet. and Toil. 93, 3, (1978). 16. Sini, F. Med. Pract. 679, 10, (1977). 17. Borelli, S. et al. Der informierte Arzt 2, 12, (1974). 18. Kline, P.R. Western Medicine 4, 78-80, 100 (1963). 19. Binet, L. et al. Therapie 27, (1972). 20. Tronnier,. et al. Parf. und Kosm. 40, (1959). 21. Tronnier,. et al. Dermatologica 104, (1952). 22. Winkler, A. et al. Arch. Derm. Res. 254, (1975). 23. Tronnier,. Aerzt. Kosmetologie 6, (1976). ur indications and recommendations have been worked out to the best of our knowledge and conscience, but without any obligation from our part. In particular, we do not take any responsibility concerning protection rights of a third party. FM-097B TDS Unitrienol T-27 en(05) Version: 05 / /22