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@Sibech The absorption of products across the skin are complicated processes for which we use specialized calculus-based Pharmacokinetic mathematics models to understand and quantify the factors.  When discussing the modeling, we consider the scenario as a “two vessel” simplified system.

Imagine a vessel with some limited permeability characteristics (the skin in this simplified model) suspended into another tank (vessel, here the actual blood/plasma). The first vessel contains a high level of the active and the main vessel (the blood/plasma) contains zero active ingredients.

Through the broad actions of homeostasis, the two vessels will “want” to reach a state where the concentration is the same in both vessels.

Now we must consider the factors. The concentration gradient (the relative difference in the active between the secondary suspended vessel and the blood/plasma vessel), the size of the active, the properties of the semi-permeable membrane and other factors apply. Since we are dealing with a delta (change) equation, the math is Calculus-based. Even in my Junior Year when Calculus was fresh and I had just aced Pharmacokinetics/Biopharmaceutics in College, the math was involved and in fact, for a whole summer internship, I sat in a windowless room doing this math on the Ciba Geigy QC line. It is not for the light-hearted.

My overall point is that facilitating and designing the transport of an Active be it Pharmaceutical or Cosmetic is not an easy process and easily out of the skill set of most if not all the participants in this blog. In fact, I would probably need to review Calculus myself and I have actually done it in the past. It is also a bit puzzling since many of the people seeking to do it in an unqualified manner usually start in Cosmetics asserting “60%/70%/95% (heard them all) of what you put on your skin gets absorbed into the body.” Then they pivot and say, “Let me add this penetration enhancer and get this complicated botanical consisting of hundreds of compounds into the body” since it is natural. THIS IS A PROCESS THAT SHOULD NOT BE ATTEMPTED WITHOUT HIGH-LEVEL UNIVERSITY TRAINING AS WELL AS INDUSTRIAL SUPPORT.

“However, that does not (necessarily) exclude dermal absorption into the epidermis where some marketing additives could arguably have an effect on stratum basale for instance (assuming they are druglike in structure).

And some compounds if formulated well can also gain systemic access (although unlikely to be significant).”

Yes, but you shouldn’t. We are making Cosmetics and it is a much more involved process than any allow. Likely, I could do the research and make a small crude nuclear reactor next door to you. The documents are declassified and I could use a Medical isotope in some crude manner.: SHOULD I TRY?

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@Bill_Toge “literal-minded donkey-work..” I now have a better job description for my resume.

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PEGs is that they are penetration enhancers and can have impurities

Kind of for the second part. I don’t believe that PEG’s are penetration enhancers, especially since you are describing a large group of products not a single compound.

In the simplest of terms, when you ethoxylate a compound, you can create a PEG. This compound which previously was hydrophobic is now hydrophilic (water soluble). You are doing this with the water-soluble Shea Butter. This allows you to get some of the benefits in an aqueous base.

As @DAS points out, one of the by-products of the ethoxylation process is 1,4 dioxane. Since identifying the concerns with these compounds, the suppliers have greatly reduced the percentage of 1,4 dioxane. It is in the very low PPM.

Now, even though the Science is sketchy, the market doesn’t care. One of the common misconceptions in the “natural” market is that the presence of a material, regardless of how infinitesimal the concentration is, it is bad. They do not recognize the fact that it is often dose-dependent.

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First, we are going to keep batting Niacinamide around. 10% is far too high. Look at these two resources and then let us never speak of Niacinamide again. You will see 10% is a waste.

https://knowledge.ulprospector.com/294/pcc-benefits-niacinamide/

https://knowledge.ulprospector.com/1587/pcc-benefits-of-niacinamide/

The DMI is being used with the Niacinamide, but again they are not making any drug claims and “maybe” it helps.  Again, I submit that a great Formulation uses multiple actives and modalities to deliver the claims. Shotgunning one ingredient can be one-dimensional in regards to performance.

With the Salicylic acid products, they are again not making any drug claims when used as an exfoliant, at least any that make it fall under an OTC monograph. It can assist the product, but not cross the line.

You also keep mentioning the PEG-8 Dimethicone. I am unsure of your knowledge level, but let me ask you a leading question that may either stump you, cause you to do some credible reading on the topic or be elementary to you. Why do we create PEG’s and what benefit do we gain? As a hint, I also ask why you might see an ingredient such as PEG-75 Lanolin? What do we gain? What is the outdated market bias against PEG’s and what is the concern with PEG’s under some natural standards?

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@Belassi I couldn’t agree more. I am forced by the client’s rigid marketing standard to use EO’s. In the US Market, there is a big marketing bias against “fragrance” partially due to the concern of Phthalates and the demand for “No synthetic fragrance.” The fragrance houses have come up with safer products, but still, many lines insist on EO’s. It is the nature of the beast.

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@Belassi Excellent anecdote! I only spent hours in Jeddah back in 1991, but I found that in much of the Muslim World they had workarounds to drinking. It is a generalization since many are observant of the restrictions but it was there. In Karachi Pakistan, I sampled a home-brewed alcohol concoction that could have stripped paint.

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Too many variables to cite regarding safety. We are really beginning to segue into toxicology and safety.

I do know that in my experience I have seen some adverse incidents with Essential oils. What sticks most to mind is the fact that many are a respiratory irritant. If you read some of the credible research, there has been an increase in this adverse effect due to some feel the increase of Essential oils in the home due to MLM programs (DoTerra, YL). You will hear people say that “Lavender makes it hard for me to breathe.”

In the end, this is all academic. When seeking guidance refer to the IFRA guidelines. Pragmatically I see the real benefit of Essential oils as alternatives to fragrance in my client’s products. You gain a “natural” market advantage but you lose a great deal of flexibility in the scent options. Unless you can afford to outsource to a Perfumist, it is rudimentary. In this case, your biggest concern should be staying within the IFRA recommended ranges.

I know many people will make claims towards the Essential oils, especially in Aromatherapy. I have consulted on many of these products. In that case, I opt out of any claims and only concentrate on getting THEIR Essential oils into a stable product. The limits to claims in Aromatherapy are loose and that whole regulatory issue could take up its own thread.

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@ngarayeva001 Let me challenge you with a few other questions that may direct you to your own answer. I am sorry if it becomes pedantic.

Dimethicone 500cst is beginning to approach the more viscous grades and is in general used in skin protectants to create a barrier. I have used it in scar treatment products etc. Why would you create a product with a known barrier and add an active?  Of course, theoretically it would increase the absorption, but why?

Let’s say that you proposed a different active and designed a product with a Dimethicone barrier to increase absorption. Is this something that you should be doing?  You could increase irritation and the increase of absorption minimally. We could go back and forth, but I will say categorically that this is not an area we should explore, that being seeking a substantial skin penetration, without a great deal more technical support and I would wager a lot more letters after our names.

So, playing devil’s advocate. I submit that the dimethicone would likely increase the absorption due to the barrier it produces (much like the technical grade membranes we used in trans dermal patches but in a very crude form) and the increase in contact time due to the persistence of the dimethicone on the skin. Lets say that you decide to capitalize on this effect to increase absorption of an active. Propose to me a Cosmetic product and active where you feel that the increase in absorption is warranted or where it would be safe and responsible. Remember that you pretty quickly will tip to an OTC product if there is any significant absorption and we have ruled this out due to lack of technical support and monitored study protocols.

It is not impossible, but the effect is finite. I will propose one, sunless tanners and the use of DMI to increase the penetration of Dihydroxyacetone (DHA) into the upper levels of the skin. It is the very upper layers of the skin and finite. It is more in order to get a more consistent effect.

Don’t cite Salicylic acid in Acne care, we ruled out OTC.

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Also, I see a lot of questions about the safety of Essential Oils. One of your best resources would be the International Fragrance Association (http://www.ifraorg.org/).

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@Biochemist I have read about Essential Oils perhaps increasing penetration and there are actually some good studies out there. Now, since I make Cosmetics, I am resolute that there are few Formulations where I could or should use this effect responsibly. In my opinion, when you start looking at aiding absorption of actives, you really are starting to get into the realm of Pharmaceuticals and/or OTC products.

There is an interesting side note on this discussion though. The CBD Industry is beginning to look at terpenes, a component of essential oils as an aid to increase absorption in pain relief topical products. The research is promising,

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Technically once you add any additives and change the Formula from the base, the testing on the altered base is invalid. PET/Stability is Formula dependent.

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Yes, but first you are missing a minor point. Salicylic acid, when used on the pores, is that a Cosmetic Product? No, when used at effective levels is an OTC DRUG.

There are several Cosmetic actives that have some activity that would be purported drug claims such as Niacinamide and Retinol.

The vast and overwhelming majority of actives and products do not absorb significantly. That is the Science. The concern, the chemophobia and all the memes “80% of what you put on your skin is absorbed” is marketing driven pseudoscience.

If you truly want to increase penetration of products, you would need to transition to OTC or Pharmaceutical products. It is irresponsible, dangerous and often not technically feasible in Cosmetics. 

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@ngarayeva001 I do want to stress not to get discouraged or feel as if you are being attacked. It is very common for novices to enter into Formulation while still believing a great deal of the crap out there. Be skeptical. Use the Scientific method. Set standards for sources of information. In the end, you will learn.

Much of what you are bringing to the table is that misinformation. Generally, it is marketing crap. I may be naive, but I still believe that I can make a quality Cosmetic product that promises credible Cosmetic claims, this product can be ethically marketed and be successful.

Keep learning.

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We would need to see the entire Formulation to provide any useful info. In my opinion, this is not likely a simple post-Formulation substitution. You would need to prototype it again, redo stability and any other performed testing, especially if you have already done the sunscreen testing.

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Repeat after me….”Cosmetics do not significantly penetrate the skin.” As such, this is really not even fairly a secondary issue and one I would not get concerned with. There are so many other overall issues to a successful Formulation.

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They need to improve the emulsification system. Until then any existing drag is theoretical, can drive a revision BUT is not really relevant for the most part.

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We can postulate on what pH is self-preserving. It is very much Formula dependent. How can you know? By sending it off to be tested. Preservation is an educated guess proven by testing.

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I would not heat Retinol. It is a fairly unstable compound. I can’t share due to an NDA, but one of the most experienced manufacturers with this product takes special care to limit the stress on the compound through special process controls. The better raw materials are encapsulated in some way but costly with higher minimums.

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@ngarayeva001 You are not wrong on the polymers. While 85% of my clients work under a natural standard or define a standard (if they don’t I pass, an advantage of existing accounts), 15% of the time I get to do mainstream projects. Recently I did a silicone moisturizer that would outsell any “natural” product on performance alone. The polymers have great sensorials. To match them with naturally derived materials, you really have to become knowledgeable of the emulsifiers and emollients. You can get close but even so, you will always have that tiny gap.

Essential oils can be phototoxic and have other issues. That alone is worthy of its own thread. It does show an area where novices will compromise safety inadvertently because “Essential oils are natural and safer.”

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@ngarayeva001 It is an evolution and one that needs to be made to really produce effective products. You will see me repeatedly weigh-in when someone naively uses the term “natural” as if it means something. It is a marketing term and in fact, encourages one to rely upon less than impartial sources. As a Formulator, leaving it undefined makes it a barrier to R&D and can cause you to compromise some performance. (Someone will disagree, but many natural products do compromise performance for the “crunchy” feel).

I will either have my clients follow a “natural standard” (Perry has done some great summary posts on these) OR define it prominently in their marketing. “XYZ Cosmetics avoids the use of parabens, formaldehyde donors, {insert maligned raw materials with too much marketing bias to overcome} AND uses plant-based materials minimally processed to produce safe and effective products.” (If you do mineral make-ups or sunscreens you will need to add “naturally occurring minerals minimally processed). Why minimally processed? Throw some raw Aloe plant in your lotion today and you tell me why! If you want more info on the appropriate processes, COSMOS has outstanding guidance.

Pragmatically I know that in some markets you must follow the marketing to a limited extent and as such some great raw materials are not “marketable.” In these cases, I always challenge Formulators to still look into the Science. You touched on one such case, silicones. You will hear “Silicones build-up on the hair and suffocate the hair shaft.” Wow, that sounds dangerous! Keep those silicones from me! As Scientists, we know this is not true. As Formulators we know it isn’t true, but when needed we will use an alternative material.

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I have moved away from Olivem1000. It was great 10 years ago. The issues with soaping were a problem, especially if you didn’t use it correctly. An issue that some Formulators never see is that it is very process dependent, especially in scale-up. The mixing process can have a great deal of effect on the final viscosity.

I have moved onto Olivoil Glutamate Emulsifier by Kalichem. (More-Teccin the US). It fixes the soaping issues and is much less process dependent. My intern last summer even started calling it jokingly “Olivem 1000, 2.0”

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Now, I don’t use alcohol a great deal. It has very specific uses. For example, it is often the most affordable solvents for certain actives, especially in OTC products. I submit that you will be much less reticent to alcohol in products if you make one of these products.

Your extreme caution with raw materials that you are experiencing is normal. Many people start in Formulating after learning “some” information (often filled with errors and emotional, not factual statements) and initially get into Cosmetics because “natural is the best!” As you learn and get exposed you will evolve from such a narrow perception and balance your formulations under a natural standard without losing too much performance. 

I will give you one piece of advice when reading “research” or look at sources online. When looking at online sources ask;

• Are they referencing credible sources? Avoid sources that make sweeping statements without supporting them with evidence. I personally ask “is this a source I would cite myself in a Master’s dissertation?”
• What are the authors credentials? This is important with online sources. I remember a frustrating instance where I had to deal with this. I had knocked a sunscreen out of the park. I was happy to see that the client approved the first sample and it passed testing with flying colors. We found a manufacturer, retained his services, raw materials were ordered and labels were printed. The job was scheduled to be done on a Tuesday. The Friday night before I get a dramatic email; “WE HAVE TO REFORMULATE!!!” I reached out and my client had found a sunscreen sold on Esty. The Etsy seller was crowing that her products were “silica free.” Our pre-milled ZnO had silica. I looked at the source and in the authors, bio was “Ms. X. has a Bachelors in Communications and enjoys ballroom dancing on the weekends.” The author failed under the credentials test.
• Lastly, is the person posting the information selling products? If so, this calls their impartiality into question. It is an obvious conflict of interest.

As you evolve and learn in this field, you will find yourself moving away from these online compromised posts and move to better sources.

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I didn’t have a specific Formulation in mind. In the thread, a statement was made that alcohol is “one of the worst things that you can put on your skin.” I was dispelling that myth.

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I have used Dimethyl Isosorbide (DMI for short) in a few limited cases, most notably in sunless tanners. It does help to some limited extent, but you will still be having the effect in the upper layers of the skin. This is appropriate since we should NOT be trying to effect a physiological effect. When in doubt, return to the FDA definition of a Cosmetic.

Were we able to actually get a measurable concentration in the blood, it would be a drug regardless and outside of the scope of Cosmetics.

As for Paula Begoun, she did not always have such an informed opinion on “alcohols.” About 10 years ago she was saying “All alcohols dry out the skin” without acknowledging that the fatty alcohols did not have this effect. I weighed in on her blog, she disagreed, I posted an article, someone posted another article agreeing with me. At that point, she deleted the whole conversation, booted us and then rewrote it to what she has now.

Lastly, here is the FDA Article on volatile alcohols; https://www.fda.gov/cosmetics/labeling/claims/ucm2005201.htm

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Alcohol is not as harmful as many believe. That is partly chemophobia. It is used in NUMEROUS products and in fact, is used at 20-25% for preservation. This is, unfortunately, misinformation that many get online from unvetted sources.

This is from a Beauty Blogger with a skincare line who is also a Harvard Educated Dermatologist; https://www.futurederm.com/why-alcohol-in-skin-care-is-safe-despite-what-paula-begoun-says/