how a chemist helped bring the Holy Grail of cosmetics—stable, effective vitamin C—to the public.

Forum devoted to the topical use of Vitamin C for the improvement of the skin, production of collagen, and general antiaging.

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how a chemist helped bring the Holy Grail of cosmetics—stable, effective vitamin C—to the public.

Post Number:#1  Post by ofonorow » Wed Oct 02, 2019 6:31 am

https://www.happi.com/issues/2019-10-01 ... the-quest/

A first-person account of how a chemist helped bring the Holy Grail of cosmetics—stable, effective vitamin C—to the public.
Owen R. Fonorow
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Re: how a chemist helped bring the Holy Grail of cosmetics—stable, effective vitamin C—to the public.

Post Number:#2  Post by ILoveParis » Wed Oct 02, 2019 3:14 pm

noun
plural noun: elastomers

a natural or synthetic polymer having elastic properties, e.g. rubber.

https://www.happi.com/issues/2019-10-01 ... the-quest/

This is all a quote from the article below:

"We added pure l-ascorbyl acid to a combination of silicone elastomer gels, under intense mixing, adding plasticizer as the viscosity increased with more vitamin C. Simply put, it is wrapped in an elegant system of elastomers that has no gritty feel, but an elegant cloud-like, lightweight feel. Encasing the vitamin C in this anhydrous structure stabilizes and delivers a desirable texture—so desirable that consumers swear it’s water-based.

The US Patent Office agreed with the novelty of our compositions and granting a broad utility patent:
9,132,080. Delivery system having stabilized ascorbic acid and other actives.
Another patent focused on anti-aging:
9,901,532 Anti-aging formulation with stabilized ascorbic acid and other actives.

How stable is it? Six months at 50°C shows no sign of yellowing or degradation. Three years at room temperature and counting shows no signs of degradation. There is no special packaging, just a jar with a screw-on cap that was opened and closed many times throughout the testing.
Does It Work?
My quest has ended with the recent introduction of Beautystat’s Universal Vitamin C Skin Refiner, which delivers stable, 20% pure vitamin C in a beautiful, silky smooth delivery. It is another game changer. Does it deliver? A clinical test proves it. Tests by a third-party, industry-leading testing center proves it. After only four weeks of use, test subjects reported a 91% reduction of lines and wrinkles, a 97% improvement in skin firmness and a 97% improvement in skin smoothness. Instrumental measurements also recorded significant improvements, including evening of skin tone.

Clearly, the formula delivers all of the promises of potent vitamin C in an aesthetically beautiful skin care system."

I feel like Indiana Jones after the final crusade. It is particularly gratifying delivering the product we all wanted for the past 40 years. We can’t wait to see how the market responds. We at Beautystat promise that we will not rest on our laurels; this breakthrough inspires us to conquer new categories and meet new consumer needs."


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Re: how a chemist helped bring the Holy Grail of cosmetics—stable, effective vitamin C—to the public.

Post Number:#3  Post by ILoveParis » Wed Oct 02, 2019 7:53 pm

Silicone Elastomer Gels

Many types of silicone are rated a 1 on the Skin Deep Environmental Working Group Page.
Skin deep gives chemicals a toxicity rating from 1-10 with 10 being the worst.
Here is an example:

Dimethicone (a silicone) has a rating of 1-3 depending on how much you use.

Other MODERATE concerns: Organ system toxicity (non-reproductive); Other LOW concerns: Data gaps, Ecotoxicology

About DIMETHICONE: Dimethicone (also called polymethylsiloxane) is a silicon-based polymer used as a lubricant and conditioning agent.

Function(s): Antifoaming Agent; Skin-Conditioning Agent - Occlusive; Skin Protectant; EMOLLIENT; SKIN CONDITIONING; SKIN PROTECTING

Synonym(s): DIMETHICONE COPOLYOL; DIMETHYL SILICONE; HIGHLY POLYMERIZED METHYL POLYSILOXANE; METHYL POLYSILOXANE; SILICONE L-45; DC 1664; DIMETHICONE 350; DIMETICONE; DOW CORNING 1664; MIRASIL DM 20; VISCASIL 5M

https://www.ewg.org/skindeep/search.php ... imethicone

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Re: how a chemist helped bring the Holy Grail of cosmetics—stable, effective vitamin C—to the public.

Post Number:#4  Post by ILoveParis » Fri Oct 04, 2019 3:03 pm

Should we use elastomers or Liposomes?
Elastomers give creams a silky feel but they have long chemical names like Dimethicone.

Studies show liposomes cross skin barrier.

Phosphatidylcholine liposomes as carriers to improve topical ascorbic acid treatment of skin disorders
Liposomes have been intensively investigated as carriers for different applications in dermatology and cosmetics. Ascorbic acid has potent antioxidant and anti-inflammatory properties preventing photodamage of keratinocytes; however, due to its instability and low skin penetration, an appropriate carrier is mandatory to obtain desirable efficacy. The present work investigates the ability of a specific ascorbate phosphatidylcholine (PC) liposome to overcome the barrier of the stratum corneum and deliver the active agent into the dermis to prevent photodamage.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4687614/

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Re: how a chemist helped bring the Holy Grail of cosmetics—stable, effective vitamin C—to the public.

Post Number:#5  Post by ILoveParis » Fri Oct 04, 2019 3:07 pm

16 different types of Lipsomes used in cosmetics:

Liposome Cosmetics Types Of Liposomes Applications
Copyright © 2016, Journal of Skin and Stem Cell. This is an open-access article distributed under the terms of the Creative Commons Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/) which permits copy and redistribute the material just in noncommercial usages, provided the original work is properly cited
1. Context
1.1. Composition
Although in the manufacture of liposomes a wide variety of amphiphilic molecules are employed, which may have uncharged positively, negatively or 2 oppositely charged polar heads, the membrane of liposomes is essentially formed by natural or synthetic phospholipids in which adding cholesterol will increase their stability. The properties of liposomes depend on the characteristics of the used structural phospholipids. Phospholipids often used in liposomes are lecithins, which are mostly extracted from natural sources such as egg, soya bean, or synthesized. Lecithins are mixtures of glycerophospholipids, which phosphatidylcholine is the most common. Another commonly compound that is used in liposomal membranes is cholesterol. Cholesterol itself does not cause a double-layered structure, though when added to the compound, enable liposome to keep the entrapped substance inside for a longer time. Based on sophistication, other stabilizers may play a role as well (1-3).
2. Evidence Acquisition
2.1. History
The possibility of forming vesicular structures from amphiphilic molecules in aquatic systems was initially speculated by Bernard (1947) during microscopic observations of myelin bodies formed with ammonium oleate in water. Bangham and Horne (1992), via electron microscopy, observed the disparity of phosphatidylcholine (lecithin) or its combination with cholesterol in water by performing negative staining using 2% sodium phosphotungstate and ammonium molybdates. Conclusions showed that a decent number of vesicles of diverse sizes were formed after shaking or sonication. Later, Wizeman dubbed these vesicles, Liposomes, which consists of Lipos (fat) + soma (body) (4).
Until early 1980s liposomes were just used as a synthetic model of bio membranes and then as a vehicle for delivery of drug molecules. Mezei and Gulasekharam reported the efficacy of liposomes for exploitation in delivery of drugs with topical approach (5).
The first liposomal cosmetic product introduced into the commercial market was the Capture anti-aging cream by firm Christian Dior in 1986, which has been followed by many other products.
In field of skin care also Laboratories RoC launched 2 products in 1987 and 1990 that were Myosphere, the first emulsion with inclusion of liposomes and the first liposomal facial cream for men. For body care, the first liposomal formulation was introduced in 1987 and many other products, which the majority of them that claimed to be effective for slimming were manufactured after that. In 1988 and later, other skin protectives such as sunscreens or self-tanning products were also turned out.
Liposomal products in cosmetics are not limited to skin care and for hair care, in 1989 a liposomal formulation was prepared. However, not many other liposomal products applicable for hair came to the market since then.
The first product containing liposomes for make-up was a powder produced in 1988 followed by mascara and different foundations (6).
2.2. Definition
Liposomes are spherical vesicles in which their central aqueous section is surrounded by one or more of a bilayer membrane (Lamella) that is frequently enclosed by aquatic environments. These vesicles are formed when amphiphilic lipids confront with aqueous milieu. They can vary in size from 15 nm to several microns. In the last 30 years, the application of liposome has been expanded from drug delivery to the cosmetic field and it is the most widely known cosmetic delivery system nowadays. Owing to their unique structure, liposomes can be utilized as a delivery system, carrying hydrophilic agents through their enclosed aqueous section, and lipophilic substances via the nonpolar tails of the bilayer section (7-9).
3. Results
3.1. Types of Cosmetic Liposomes
Based on composition and indications, cosmetic liposomes divide to different types. Depending on the features we want our cosmetic product possess, we can use one of these types.

Transferosomes: Transfrosomes are highly deformable, reactive, and efficient liposomes applied until now for direct transdermal drug delivery. In regards to their small dimension (300 - 200 nm), they can easily penetrate the skin and pass across the skin’s stratum corneum by using intracellular or transcellular route with the help of 2 elongated elastic layers on their surface. These species of liposomes are made of phospholipids, cholesterol with addition of some surfactants like sodium cholate (cholic acid salt) (8, 9).

Niosomes: Niosomes are small vesicles composed of non-ionic surfactants from alkyl or dialkyl polyglycerol ether class. In cosmetics and skin care, the use of niosomes is very useful due to the fact that it can improve the product effectiveness and increases its penetration, increases bioavailability of poorly absorbed ingredients, and enhances the stability of drugs (3, 8, 9).

Novasomes: Novasomes are non-phospholipid oligolamellar lipid vesicles of 0.1 - 1.0 microns that are a variety of liposomes or modified niosomes synthesized by combining polyoxyethylene fatty acids’ monoester, cholesterol, and free fatty acids with a ratio of 74/22/4. They offer further superiority for being used in cosmetic preparations by providing the ability to cleave to skin or hair shafts. This also enables sustained release and enhances the effectiveness and texture of these cosmetics (10).

Marinosomes: These types are made from marine lipid extracts that contain a high rate of Eicosapentaenoic acid and Docosahexaenoic acid that are omega-3 polyunsaturated fatty acids. Metabolized by the skin’s epidermal enzymes, they change to their anti-inflammatory and anti-proliferative metabolites, which helps in healing many of the skin’s inflammatory problems. The toxicity studies shows that this category of liposomes is safe for skin and eye contact (3, 9).

Ultrasomes: Ultrasomes are a unique category of liposomes that are formed by entrapment of the endonuclease extracted from Micrococcus luteus. They help detect ultraviolet radiation harm to the skin and increase the speed of treatment by up to 4 times. Ultrasomes also act as immunity system protectives by eliminating the destructive effect of ultraviolet radiation to the DNA and inhibiting the expression of some cytokines including the tumor necrosis factor alpha and interleukin 1, 6, and 8 as well as diminish the risk of skin cancer (9).

Photosomes: photosomes act by releasing photolysis enzymes extracted from the marine plant Anacystinidulans. They are extensively used in sunscreens, which prevents light from damaging the cell's DNA, therefore preventing the suppression of the immune system and reducing the risk of cancer induction (9).

Ethosomes: These varieties of liposomes are soft and flexible multilayer vesicles composed of phospholipid phosphatidylcholine, water, and 20% - 50% ethanol. Ethosomes are non-invasive carriers that enable the component penetrate deeply into the skin layers or enter systemic circulation. High concentrations of ethanol make ethosomes unique. Since ethanol is known to cause an imbalance in the arrangement of the skin’s two-lipid layer, it can penetrate the horny layer when mixed with a vesicle. Compared with conventional liposomes, they offer better features for efficient delivery of cosmetics to the skin in terms of both quantity and depth (9).
Asymmetric oxygen carrier system (AOCS) liposomes: this system is designed for skin oxygenation. The oxygen carrier vesicles have a perfluorocarbon nucleus and a phospholipid layer enfolded by a dual-layer membrane.
Perfluorocarbons are able to dissolve great amounts of different gases including oxygen, however, they have a hydrophobic structure making them immiscible with water. Hence, by placement of them in the center of a liposomal vesicle, we can design suitable systems for transporting oxygen to the skin (3, 9).
Yeast based liposomes: These are derived from yeast cells and provide vitamin C for skin that help in repairing, soothing, and oxygenating the skin. They stimulate skin fibroblasts in their liposomal form, which makes the skin feel healthier. When the liposome is used as a carrier, cellular vitamin C intake increases significantly (3, 9).

Phytosome: they are advanced herbal preparation of liposomes developed by mixing phospholipids and botanical extracts such as flavonoids, glycosides, and terpenoids. Phytosomes improve skin absorption of phytoconstituents and are broadly used in cosmetics for their high lipid profile and enhanced skin penetration (11).

Sphingosome: Sphingosomes are liposomes constituted of ceramides for the aim of normalizing the damaged or dehydrated skin with respect to the fact that ceramides or other analogous molecules can compensate the water deficiency and rehabilitate the skin’s barrier function (1).

Nanosome: Nanosomes are very small liposomes formed from highly pure phosphatidylcholine in a low nanometer size range. They are applied as anti-aging serum for enhanced performance designed to upgrade skin to a healthy and youthful looking stage (12).

Glycerosome: glycerosomes are modified liposomes containing glycerol in addition to phospholipids. Their special features include the ability to deliver cosmeceutical active ingredients to the skin with high performance, healing, beautification properties. Lately, unilamellar glycerosomes containing quercetin were designed with the size of 80 - 110 nm, which showed to improve skin defensive activity. The future prospect is using them for manufacture of antioxidant skin creams (13).

Oleosome: oleosomes are natural liposomes and a reservoir of oils, vitamins, and pigments. They are found in a variety of oil bearing plant seeds or fruits and proven to be efficacious delivery systems in personal care.

Oleosomes made up of seabuckthorn fruit flesh demonstrated high stability and antioxidant properties (14).

Catezome: catezomes are novel non-phospholipid vesicles with a cationic surface charge prepared from fatty acid salts of quaternary amines that are amphipathic molecules. These liposomes with hydrophilic or hydrophobic cosmeceutical payloads have the ability to be preserved by both hair and skin and are ideal delivery systems, especially when penetration is not of acceptance or when we expect manageable penetration (15).

Invasome: Invasomes are the liposomal vesicles comprising small amounts of ethanol plus terpenes or terpene mixtures, which act as potent carriers with elevated skin penetration properties. Invasomes are soft liposomal vesicles with great membrane fluidity. The attendance of ethanol and terpenes gives the invasome specific features, which cause to get the simultaneous benefit of liposomes as potential carriers and trepenes, which promote the skin permeability and cutaneous delivery by altering the order of stratum corneum packing (16).
http://journalssc.com/en/articles/65815.html
Last edited by ILoveParis on Fri Oct 04, 2019 3:13 pm, edited 1 time in total.

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Re: how a chemist helped bring the Holy Grail of cosmetics—stable, effective vitamin C—to the public.

Post Number:#6  Post by ILoveParis » Fri Oct 04, 2019 3:12 pm

Mixing ingredients and PH:

https://knowledge.ulprospector.com/6481 ... ves-video/

TRANSCRIPT:
Cosmetics today are able to give consumers better results than ever before and a lot of that has to do with cosmeceutical active ingredients. But as a formulator how do you know what's out there and how do you know the best ones to pick for your application? This video will go through some of the selection criteria you should be using when selecting actives for your next cosmeceutical developments.
1. The first and most important principle is that active ingredients should be used in finished products the way they were to obtain the test results. What this means is if the ingredient was used at 2% in a cream applied twice daily to obtain the results in the in vivo efficacy data, you would need to use it at 2% in a cream also, with the directions to apply twice daily.
2. You could not use the evidence from a twice-a-day leave-on product for a once-a-day wash-off or once-a-week leave-on product, for example.
3. In vitro and ex vivo data won't necessarily give you a formulation input to use.
4. So look for in vivo use and efficacy data to ensure you're using the active ingredient in an amount that will get proven results. You can find multiple product and technical data sheet on Prospector, giving efficacy results for in vivo tests by conducting searches of their extensive database.
What to consider when comparing cosmeceutical actives
When comparing actives, you need to consider:
• Product, form, and compatibility: We're going to take a good look at this in the next section.
• Amount to be used: This can impact your formula but also cost. A more expensive material used in small quantities may work out cheaper than using a cheaper material in larger quantities.
• Company philosophy: How green and natural does the formula need to be and how does that then limit your active ingredient selection?
• Look for strong marketing claims from in vivo results and compare these between actives. This may give you very clear indications of which material will give you the best performance results. If you have a few materials that compare on cost, philosophy and in vivo performance, comparing in vitro and ex vivo data may then help you determine which active will work best for your application.
• Request samples of the actives and trial them in your formula. What sounds good in theory may have an unexpected and undesirable effect in the finished formula, and that may make your decision for you. Use the Prospector database extensively to get active ingredient information and then contact your supplier for samples.
Ensuring efficacy
When ensuring efficacy of a finished product, there are two key things to remember.
• The first is to ensure that you are formulating a compatible base with the active so that your active remains available in the formulation.
• And two, you need to make sure you get that active to the target delivery site. Where will it be effective? So you need to create your formula to ensure delivery of your active ingredient to where it needs to be to get the desired result.
Compatibility issues
Active ingredients may have specific pH and temperature compatibilities. They may also be affected by charge. They may also be oil- or water-soluble and you'll need to make sure you disperse them into the right medium to ensure stability in the formula over a long shelf life. Some other considerations may include:
• pH: Make sure the active is used in a formula with a suitable pH, otherwise it may be inactivated or degraded. Look specifically for this information on supplier data sheets.
• Temperature of addition: Again, adding an active to a hot product may inactive it. Most actives need to be added below 40 degrees. But refer to supplier data sheets to be sure you're adding your active at the right temperature.
• Shear may impact some actives. Another important piece of information to check for on supplier information sheets, especially if the active is provided in a liposome or encapsulated form.
• Some actives may be inactivated when too much water is present. So check this feature carefully too and adjust the product form or water input, if required.
• Your formula will need to be stable when the active is added and the active may have very specific pH, temperature or other compatibility requirements. Make sure you check for this information carefully, which can be obtained through the Prospector database.
Delivering cosmeceutical actives to the target site
The skin is a relatively thick and complex organ designed, amongst other features, to protect tissues and organs within the body from externally applied substances. To be their most effective, cosmetic ingredients need to penetrate the epidermal layers sufficiently to perform their specific function, and this will vary depending on the type of product you're creating.
For example, a moisture protective product only needs to penetrate and preferably provide some sort of film forming at the stratum corneum level. While a product designed to boost hydration over a prolonged period will need its ingredients to penetrate to the mid-layers of the epidermis, whilst also preferably providing some moisture protective properties at the stratum corneum level.
Cosmeceutical ingredients, particularly advanced cosmeceutical ingredients that activate dermal-epidermal communications, need to penetrate to the stratum basale level. The key thing to remember when formulating is where do you need the ingredients to go and how are you going to get them there?
Stratum cornea hydrophilic pathways require water soluble substances to be less than 0.4 nanometers in diameter to penetrate past this layer. While the stratum corneum lipid by-layer will allow passage of much larger lipophilic substances on a nano scale of less than 13 nanometers. The stratum corneum inter-corneocyte space will allow passage of lipophilic substances with a diameter of 20 to 75 nanometers, but then you face the challenge of the substance being able to pass through the protective intercellular lipids, which have a stratum corneum thickness of 10 to 40,000 nanometers.
To help actives penetrate to the mid-layers of the epidermis or stratum granulosum, use osmolytic substances such as:
• humectants
• glycerin
• propylene glycol
• pentylene
• butylene glycol
Many actives will come combined with these substances to protect them and enhance delivery. Substances used to reduce the polarity index of the skin such as dimethyl isosorbide can also enhance delivery of actives, particularly water soluble actives, to mid-layers of the epidermis.
To help actives penetrate into the deeper layers of the epidermis or stratum basale, and this is where you want most peptides and actives with an action on melanocytes, dermal-epidermal junction, elastin, and collagen synthesis to reach, use emulsions with very fine droplet size or small liposomal delivery. Be careful, though, because emulsions with very small droplet size may appear translucent, blue-gray or cloudy compared to a pretty white. While that very small droplet size may be ideal for delivery, it may not be aesthetically pleasing for your consumer.
You may also use micro or nano-encapsulated substances to help enhance delivery. But be careful of how you introduce and stabilize these in your formulas.
High shear, for example, can break the capsules during mixing and yet if they aren't mixed into formulas homogeneously or stabilized effectively, actives may settle to the bottom or top, over the shelf life, and not be delivered in their required doses. So you may need to use a couple of these delivery systems to ensure your active ingredients get to their target site. Remember it's not just about delivery, but also ensuring compatibility of your base formulation.
So you may need to check and double check those product information sheets from your suppliers to ensure you're not only getting the material to their active site, but also formulating a compatible base.
Finally, here's an active checklist to help you make sure you're selecting the right active for your next development and using it appropriately.


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