A nonionic water-dispersible surfactant for lipid-based formulations to solubilize and increase oral bioavailability of poorly water-soluble APIs. Self-emulsifies in aqueous media forming a fine dispersion, i.e., microemulsion (SMEDDS).
Consists of a small fraction of mono-, di- and triglycerides and mainly PEG-8 (MW 400) mono- and diesters of caprylic (C8) and capric (C10) acids
Key characteristics
Product form
Liquid
Viscosity (mPa.s)
80 – 110 (20°C)
CMC (mg/L, 25°C)
42 ±24
HLB
12
Main functionalities
Solubilizer for poorly-soluble APIs and bioavailability enhancer. Single excipient formulation system: self-emulsifies in aqueous fluid into microemulsion—LFCS Type III (SMEDDS). High purity guaranteed for stability and capsule compatibility. Safety of use is inferred by extensive toxicological data and precedence of use in approved pharmaceutical products.
Poor solubility, poor permeability, and pre-systemic elimination are factors that can limit absorption of somedrugs. Lipid excipients have the capability to overcome these hurdles and enhance oral bioavailability throughdifferent mechanisms.
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How to develop lipid-based formulation?
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An optimized LBF enables solubilization of the entire therapeutic dose andmaintains the drug in solubilized state throughout the digestion process.
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To speed up LBF development, we have produced tools to guide you at each stageof development:
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1 – methods for saturation solubility screening
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2 – database of solubility of drugs in common pharmaceutical excipients
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3 – methods for miscibility and dispersability testing
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4 – miscibility table
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5 – in vitro lipolysis procedure
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6 – guideline for preclinical studies
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What are the different types of lipid-based formulations?
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Depending on their composition, LBF exhibit different in vivo behaviors. They typically consist of biocompatible excipients falling into four main categories: oils, low-HLB surfactants, high HLB surfactants and co-solvents. To facilitate their identification, Poutonet al. introduced the Lipid Formulation Classification System based on the composition, size of the droplets generated after the dispersion of the formulation in aqueous media, and the impact of natural lipid digestion process on the in vivo performance of the formulation classes.
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What functional excipients for oral bioavailability enhancement do Gattefossé deliver?
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Our range of functional excipients includes oils, low HLB surfactants, high HLB surfactants and solvents. They can be combined to formulate all types of lipid-based formulations
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What are self-emulsifying formulations?
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Self-emulsifying lipid formulations form emulsions upon contact with aqueous fluids without the need for mechanical or thermal energy.The size of the dispersion depends on the composition of excipients in the formulation.
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How to use lipid excipients and lipid-based formulations in early stage development?
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A vehicle or formula intended for preclinical studies must allow adequate administration of the test compound with little or no effect on the test species. The vehicle or formulation must be suitable for the intended route of administration, maintain the stability of the active ingredient, and preferably, maximize the systemic bioavailability of the drug. Lipid excipients provide a solution to these challenges and have proven utility in preclinical studies. Further information is available from Gattefossé guideline
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\n\n\n","box_links":[{"link":false,"title":"Download our brochure","external_link":"https://www.gattefosse.com/back/files/Brochure_Gattefosse_Lipid-based%20formulations%20a%20winning%20strategy%20to%20overcome%20oral%20bioavailability%20challenges.pdf","image":"https://www.gattefosse.com/wordpress/wp-content/uploads/2021/01/54370-e1612972328251.jpg"},{"link":false,"title":"Simple and effective design of SEDDS formulations","external_link":"https://www.youtube.com/watch?v=E2HnSAVyzHU&t=46s ","image":"https://www.gattefosse.com/wordpress/wp-content/uploads/2021/01/auto-self-emulsifying.jpg"}],"useful_links":[{"text_link":"Developing lipid-based formulations","link":"https://www.gattefosse.com/pharmaceuticals-special-content/lipid-based-formulations-development/","external_link":""},{"text_link":"Excipients for solubility and bioavailability enhancement ","link":"https://www.gattefosse.com/pharmaceuticals-content/excipients-for-solubility-and-bioavailability-enhancement/","external_link":""},{"text_link":"Guide for successful preclinical studies with Gattefossé excipients","link":"https://www.gattefosse.com/pharmaceuticals-content/guide-for-successful-preclinical-studies-with-gattefosse-excipients/","external_link":""},{"text_link":"Lipid-based formulations : a winning strategy for oral bioavailability enhancement","link":"https://www.gattefosse.com/pharmaceuticals-content/lipid-based-formulations-winning-strategy-oral-bioavailability-enhancement/","external_link":""}],"":false,"content_not_translated":true,"equivalent_fr":false,"equivalent_en":false},"_links":{"self":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages/22909"}],"collection":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages"}],"about":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/types/page"}],"author":[{"embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/users/36"}],"replies":[{"embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/comments?post=22909"}],"version-history":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/pages/22909/revisions"}],"wp:attachment":[{"href":"https://www.gattefosse.com/wp-json/wp/v2/media?parent=22909"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/categories?post=22909"},{"taxonomy":"post_tag","embeddable":true,"href":"https://www.gattefosse.com/wp-json/wp/v2/tags?post=22909"}],"curies":[{"name":"wp","href":"https://api.w.org/{rel}","templated":true}]}},"capryol-pgmc":{"id":2189,"date":"2017-04-20T09:08:42","date_gmt":"2017-04-20T09:08:42","guid":{"rendered":"https://www.gattefosse.com:443/wordpress/?page_id=2189"},"modified":"2022-05-09T10:27:24","modified_gmt":"2022-05-09T08:27:24","slug":"capryol-pgmc","status":"publish","type":"page","link":"https://www.gattefosse.com/pharmaceuticals-products/capryol-pgmc/","title":{"rendered":"Capryol® PGMC"},"content":{"rendered":"","protected":false},"excerpt":{"rendered":"","protected":false},"author":9,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"_yoast_wpseo_title":"Capryol® PGMC -Propylene glycol monocaprylate type I - Surfactant","_yoast_wpseo_metadesc":"Capryol® PGMC is a nonionic water-insoluble surfactant used as cosurfactant in oral lipid-based formulation SEDDS and SMEDDS."},"categories":[7],"tags":[],"acf":{"component":"PageProductPharma","":false,"product_codes":[{"code":"3241"}],"product_image":{"id":13616,"alt":"","title":"liquid","caption":"","description":"","mime_type":"image/jpeg","url":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/liquid-1.jpg","width":1716,"height":600,"sizes":{"thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/liquid-1-150x150.jpg","thumbnail-width":150,"thumbnail-height":150,"medium":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/liquid-1-300x105.jpg","medium-width":300,"medium-height":105,"medium_large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/liquid-1-768x269.jpg","medium_large-width":474,"medium_large-height":166,"large":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/liquid-1-1024x358.jpg","large-width":474,"large-height":166,"post-thumbnail":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/liquid-1-672x372.jpg","post-thumbnail-width":672,"post-thumbnail-height":372,"twentyfourteen-full-width":"https://www.gattefosse.com/wordpress/wp-content/uploads/2017/04/liquid-1-1038x576.jpg","twentyfourteen-full-width-width":1038,"twentyfourteen-full-width-height":576}},"product_title":"Capryol® PGMC","introduction":"
A nonionic water-insoluble surfactant used as cosurfactant in oral lipid-based formulation SEDDS and SMEDDS. Cosurfactant and solubilizer in topical dosage forms.
\n","names_kv":[{"keys":"USP NF Name","value":"
Propylene Glycol Mono and Dicaprylate NF \n[May also be labeled as Propylene Glycol Monocaprylate (type I) NF until December 1, 2026]
\n"},{"keys":"EP Name","value":"
/
\n"},{"keys":"UNII Code (FDA)","value":"
RT9P9S09QI
\n"},{"keys":"Preferred Substance Name (FDA)","value":"
PROPYLENE GLYCOL CAPRYLATE
\n"},{"keys":"Handbook of Pharmaceutical Excipients","value":"
Propylene glycol monocaprylate
\n"},{"keys":"Chemical description","value":"
Consists of propylene glycol esters of caprylic acid (C8), composed of mono- and diesters.
Solubilizer for poorly-soluble APIs and bioavailability enhancer. Cosurfactant in LFCS Type II (SEDDS) and Type III (SMEDDS) formulations. Solubilizer and cosurfactant for microemulsion in topical formulation. Safety of use is inferred by precedence of use in approved pharmaceutical products.
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\n
Every woman faces a gynecological disorder at some point in her life, during puberty, maternity, menopause or post menopause. These age periods structure the women’s health market with treatments for menopause related disorders, postmenopausal osteoporosis, infertility, endometriosis, gynecological cancer and birth control.
\n"},{"wysiwyg":"
For a healthy vaginal flora
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Equilibrium of the vaginal flora is fragile and is easily altered by external factors such as:
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Hormonal changes with menopause, oestro-progestative birth control pills, diabetes
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Excessive hygiene
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Medicines such as antibiotics
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Stress
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Tobacco
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Probiotics are known to restore the vaginal flora, either by local treatment or oral administration, the latter being the most efficient. They can also be administered preventively during pregnancy for women with recurrent fungal infections or in combination with antibiotic treatments. Probiotics to restore vaginal flora are available as:
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Oral tablets with precedence of use of Precirol® ATO 5 (glyceryl distearate) and Compritol® 888 ATO (glyceryl dibehenate) as lubricants
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Vaginal suppositories with Suppocire® and Ovucire® (hard fats) as pessary base
At menopause many changes occur with the drop in hormones inducing vaginal dryness, among other symptoms. Hyaluronic acid is frequently used for mucosa hydration in creams using Tefose® 63 (mixture of PEG-6 stearate and ethylene glycol palmitostearate and PEG-32 stearate) and Labrafil® M 2130 CS (lauroyl polyoxyl-6 glycerides) or in pessaries using hard fats. In the Application Laboratory in Saint Priest a pessary formulation was developed with 0.25% of hyaluronic acid 99.75% Ovucire® WL 3264. Product characteristics are as follows:
\n
Homogeneous beige pessary\r\nMelting point 34.9°C +/- 0.1°C\r\nMecanical stress > 5.400 Kg\r\nLiquefaction time 8 min 18 s +/- 25 s
Antifungal agents such as clotrimazole, metronidazole or miconazole nitrate are listed on the WHO Essential Medicines List. They are frequently formulated in pessaries and/or creams to treat vaginal infections.
Hard fat suppository base with emulsifier to improve dispersion of hydrophilic APIs, recommended for formulation of glycerin suppositories.
\n","names_kv":[{"keys":"USP NF Name","value":"
Hard fat EP/NF/JPE with Glycerol Monostearate EP/NF and PEG-75 Stearate (type I) NF
\n"},{"keys":"EP Name","value":"
Hard fat EP/NF/JPE with Glycerol monostearate EP/NF and PEG-75 Stearate (type I) NF
\n"},{"keys":"UNII Code (FDA)","value":"
8334LX7S21 230OU9XXE4 OT38R0N74H
\n"},{"keys":"Preferred Substance Name (FDA)","value":"
FAT, HARD GLYCERYL MONOSTEARATE PEG-75 STEARATE
\n"},{"keys":"Handbook of Pharmaceutical Excipients","value":"
Suppository bases, hard fat
\n"},{"keys":"Chemical description","value":"
Consists of mono-, di- and triglyceride esters of fatty acids (C10 to C18), the triester fraction being predominant and containing glycerol monostearate (C18) and PEG-75 (MW 3500) stearate (C18)
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Did you know that age spots are the first sign of aging in Asian skin, and the third major aging concern of European and American women, after wrinkles and sagging? Though we often think of wrinkles as the primary issue, 70% of all people over 55 have at least a few age spots.1 Age spots, or dark spots, are permanent hyperpigmented marks that appear on UV-exposed areas of the skin. Although it was previously believed that these spots form primarily in the epidermis, recent research suggests that the health of the dermis also plays a role in their formation. Gatuline® Spot-Light is the first ingredient to diminish these spots while brightening complexion—through targeted preventive and curative action at the epidermal and dermal levels.
Gatuline® Spot-Light is obtained by extracting active molecules from Asian Sophora flavescens and handpicked Italian kiwi. Our strict sourcing standards ensure continuous supply and appropriate concentrations of key molecules, while preserving the natural growth and health of the plants.
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Modified- or sustained-release matrices are designed to release a drug slowly over an extended period of time. Formulations must be robust to ensure drug release over time and avoid dose-dumping. Lipid-based matrices are water-insoluble and do not swell or erode when in contact with aqueous media. When used as sustained-release agents, they form an inert matrix from which the drug diffuses slowly.
\n
Advantages of Gattefossé’s modified-release agents:
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• Drug release is a function of diffusion, which enables simple product design and offers both straightforward modulation of drug release and high reproducibility. • Tablets are biopharmaceutically robust as the lipid matrix is not sensitive to physiological variations (e.g., pH, digestive processes, alcohol level). • Agents are suitable for a wide range of processing techniques, including direct compression, granulation, melt coating, hot melt extrusion, and capsule molding.
finely atomized lipid excipient powder of well-defined, reproducible composition and particle size
\n
used at proportion of 10%–40%, depending on drug solubility and diluent properties
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suitable for direct compression, granulation, and hot processes (i.e., hot melt coating, granulation, and extrusion)
\n
crystalline material with narrow melting range (∼70 °C) and rapid recrystallization, ideal for hot melt processes
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GRAS status and precedence of use with many APIs (FDA IID)
\n
\n
We can provide technical guidelines that offer useful tips on SR formulation development and numerous case studies with model drug molecules, e.g., bupropion HCl, levodopa, metformin HCl, metoprolol succinate, niacin, and theophylline.
finely atomized lipid excipient powder of well-defined, reproducible composition and particle size
\n
crystalline material with narrow melting range (∼55 °C) and rapid recrystallization, suitable for use in hot processes (i.e., hot melt coating, extrusion, and capsule molding)
\n
GRAS status and precedence of use with many APIs (FDA IID)
crystalline material with narrow melting range (∼60 °C) and rapid recrystallization, suitable for use in hot processes (i.e., hot melt coating, extrusion, and capsule molding)
\n
GRAS status and precedence of use with many APIs (FDA IID)
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\n
Gattefossé opened a cell biology laboratory, including clean rooms, at its headquarters in 2013. Laboratory staff culture skin cells and tissues and carry out research in skin biology aimed at developing cosmetic substantiation tests and innovative investigative models.
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Cell culture models to substantiate cosmetic active ingredients
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Our active ingredients are substantiated through a battery of efficacy tests adapted to molecular screening:
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Simple models of monolayer cell culture (fibroblasts, keratinocytes, melanocytes, adipocytes, and sebocytes) are used to investigate the efficacy of active ingredients on cell metabolism (cell proliferation and protein synthesis),
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Pluristratified models, such as spheroid cultures, are developed to reach matrix targets and complete the screening process.
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\n
\n
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3D models of artificial skin
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We also work with advanced 3D artificial skin models and reconstructed epidermis, dermis, and skin. Human skin biopsies are used to mimic skin physiology and isolate innovative biological mechanisms and targets. These cultures effectively elucidate the mechanisms of action and biological properties of our active ingredients.
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Innovation through research in skin biology
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Our skin biology research, conducted in partnership with Academic Research Institutes, equips up us with technologies at the cutting edge of innovation. Our 3D artificial skin cultures not only serve to demonstrate efficacy, but also function as investigative models to acquire a better understanding of skin pathophysiology (aging, UV, pollution, and stress) and discover new cosmetic targets for the development of active ingredients.
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Gattefossé expertise in cell culture and tissue engineering is matched by biochemical, enzymological and immunological methods as well as microscopy and image analysis.
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Follow the guide
\n\n
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Gattefossé invites you behind the scene to discover its skinbiology laboratory from the inside. A virtual tour at 360° to dive into the fascinating universe of cell culture.
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Agent de texture naturel et durable, Lipocire™ A SG donne du corps aux formules cosmétiques et leur confère un toucher plus onctueux, ultra fondant.
\n
Une expérience sensorielle unique dans de nombreuses applications soin et maquillage.
Beurre végétal texturant, Lipocire™ A SG est issu de l’hydrogénation et de l’inter-estérification d’huiles de palme et de palmiste, extraites des fruits et des graines du palmier à huile. Relipidants et nourrissants, ces lipides filmogènes présentent une excellente affinité avec la peau et permettent de reconstituer le film protecteur hydrolipidique. Ils apportent douceur et confort à la peau et aux formulations.
\n
Gattefossé n’utilise que des huiles de palme et de palmiste certifiées RSPO Segregated (SG) (Roundtable on Sustainable Palm Oil). Cette certification garantit que les huiles proviennent exclusivement de plantations gérées durablement.
\n
\n
Le fruit du palmier a la peau rouge foncé et la chair jaune-orange, il est particulièrement riche en éléments nutritifs. La pulpe du fruit et l’amande dans son noyau ont tous deux une teneur élevée en triglycérides (> 50%).
\n
Autres grades disponibles :
\n
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Lipocire ™ CM SG a un point de fusion légèrement supérieur et est préconisé pour les formulations de plus grande rigidité : par exemple, sticks ou poudres pressées.
\n
Lipocire ™ DM SG a un point de fusion supérieur aux deux autres grades. Il est conseillé de l’utiliser pour les formulations avec une solidité encore plus grande, comme les crayons de maquillage.
Maquillage : mascaras, rouges à lèvres, brillant à lèvres, bâtons, eye-liner, ombres à paupières, rougeurs, poudres en vrac
\n
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\n
Artificial visible light is everywhere in our modern life. Our mode of social communication confronts us with screens of all kinds and their use is on the rise. Curious to discover the potential consequences of such an environment on skin health, Gattefossé initiated a two-year investigation with CYTOO, to determine the direct effects of screen exposure on the skin.
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Created in 2008, CYTOO is a biotechnology company specialized in the development of physiologically-relevant cellular models and assays for High Content Screening (HCS).
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Unique equipment was designed by Gattefossé to accurately recreate the characteristic light emitted by screens of electronic devices (smartphones, tablets, PC). By using micropatterning technology, a method to guide cell shape and monitor cell fate, CYTOO has developed a High Content Screening assay combining precise control of human dermal fibroblast spreading and sensitive analysis of mitochondrial fusion/fission dynamics by non-invasive live-cell imaging.
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Gattefossé and CYTOO have united technology, expertise and know-how to explore mitochondrial modulation and protection upon artificial visible light exposure.
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Mitochondria, also termed the powerhouse of cells, produce the energy essential to proper biological function of cells. Mitochondrial quality is finely adjusted by constant reshaping of its structure via a process involving fusion and fission.
\n
CYTOO and Gattefossé have discovered that exposure to screens significantly weakens mitochondrial function and dynamics. Fragmentation of the mitochondrial network is observed alongside loss of quality control and diminished capacity to produce ATP*.
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“Mitochondrial fission and fusion play critical roles when cells experience metabolic or environmental stresses. We were delighted to start a long-term collaboration with Gattefossé, and to adapt our platform to dermo-cosmetic applications. Both companies have brought cutting-edge technologies to address a brand-new vision of biological processes implied in skin homeostasis. This collaboration with Gattefossé validates once more the ability of CYTOO to generate innovative and predictive solutions to our partners” said Luc Selig, CEO of CYTOO.
\n
“Using the CYTOO model, we have been able to demonstrate that screen-emitted light has a tremendous detrimental effect on the mitochondrial network of skin fibroblasts. This research highlights the need for a strategy to protect the skin from everyday artificial light”, said the Skin Biology Research Manager at Gattefossé, Nicolas Bechetoille.
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*ATP: Adenosine TriPhosphate
\n
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