Ep 193 – The Rogue Pharmacist: Product Penetration vs. Skin Absorption

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Lamb Probe can empower your skin practice with these new and highly in-demand services. For more information, visit lambprobe.com. That's L-A-M-P-R-O-B-E. And follow Lamb Probe on social media at Lamb Probe. Hello and welcome to ASCP and the Rogue Pharmacist with Benjamin Knight Fooks. In each episode, we'll explore how internal and external factors can impact the skin. I'm Maggie Stasick, ASCP's education program manager, and joining me is Ben Fooks, Skincare Formulator, and Pharmacist, Hey Ben. Hello Maggie. How are you doing? I'm doing great. Thank you for having me. Nice to see you. Nice to see you. It's my understanding that product absorption and product penetration they sound similar, and they're sometimes used interchangeably, but there is actually a big difference. Well, you know, I think I know what you're talking about. Penetration refers to the through the surface of, in terms of skin care, refers to the through the surface of the skin, and then absorption means into the body. I assume that's what you're thinking about, and there is a distinction, and it's a very important distinction to make. And in order to understand the relevance of that distinction, you got to understand a little bit about the structure of the skin. Most people listen to this podcast, understand the structure of the skin, but just to quick review, you get the surface of the skin, then you've got a layer under the surface of the skin, then you got a layer underneath that, and then you've got a layer underneath that, and then you've got the body. So the surface of the skin, stratum corneum, hard layer, very thin, probably about a thin is one-tenth of a piece of notebook paper. Underneath that, you have the epi-dermus, that's about as thick as one piece of notebook paper, and then underneath that, you have the dermis, and that's about as thick as nine pieces of notebook paper in between the dermis, and the epi-dermus, and the stratum corneum, you have what's called the skin. Underneath the skin, underneath the dermis, you have the subcutaneous layer, the fatty layer, and then underneath that, you have the blood, and you have the body. It's a little bit of blood probably in the subcutaneous layer, but basically the blood in the body are located underneath the subcutaneous layer. So we talk about penetration, we're talking about through the surface, through the stratum corneum, when you talk about absorption, you're talking about into the blood. Now in pharmacy school, we study a lot of something called pharmaceuticals, which is the study of how you get drugs from stratum corneum into the bloodstream. That is no mean feat. There's a lot of technical stuff that has to happen in order for that to occur. When I'm formulaing skincare products, I leverage some of those ideas not to get my skincare products or my skincare ingredients into the blood through the subcutaneous layer, but into the dermis, so we can get to the fibroblast, and into the lower level of the epidermis, so we can get into the keratinocyte. That's where you really need to be if you're going to have an effective skincare product. You got to be in the lower level of the epidermis, the basal layer, and to a certain extent, the squamous layer, where you have the basal cells, the keratinocytes, and the squamous cells, and then in the dermis to get to the fibroblast, and there's some techniques that you can use. There's some strategies that you can use in terms of formulating a skincare product that can allow your molecules to get to the keratinocyte, and to get to the fibroblast. That being said, just because you get to the keratinocyte and the fibroblast doesn't mean your molecule is going to get in to the keratinocyte and in to the fibroblast. The keratinocyte and the fibroblast are not stupid. They're not going to take in just anything. There has to be a certain relevance. The molecule has to be relevant to the functioning of that keratinocyte or the fibroblast for it to actually get into the cell to do its work. I've heard you use a term, and it's on the tip of my tongue. I want to say biomimetic, but that's not right. No, that is. That's right. That's right. You're thinking maybe biogenic. Biogenic. Okay. So biomimetic and biogenicity and biomimicry are two very, I think they're very relevant terms when it comes to leveraging the activity of molecules, taking advantage of the activity of molecules. Biogenicity is a term I made up. Biomimicry is a term that's in the vernacular. These days, other people are talking about biogenic, but I wanted to convey the idea that certain molecules are familiar to biochemistry. When I said early relevant to the keratinocyte and relevant to the fibroblast, what I mean is molecules that are already inherent into the system, they're native, they're familiar to the skin cells, and those are the molecules that are going to get into the fibroblast and into the keratinocyte. The keratinocyte is like, oh, I know who you are. Welcome home. Or even there's receptors sometimes in the keratinocyte. Retinol, for example, there's actually receptors and carriers that can bind to retinol and then transport the retinol into the cell and even into the nucleus in the case of vitamin C. There's actually receptors on the vitamin C. There's a scorebait receptors on the keratinocyte and on the fibroblast that will bind with that molecule. There are peptides, for example, there are hormones also that have an ability to react or bind to receptors on the cell. So those molecules that are inherent to the native to the skin that are recognized by the cell, biogenic molecules. Genic, meaning genesis, has its beginnings in biology. Biogenic, born, or has its beginnings in the biological system. Biomimicry is a molecule that mimics or imitates, and they're very similar, that imitates something that's already in the body or already in the biological system. So they're similar, but they're not exactly the same. Biomimicry is a more accepted term than biogenetic or biogenicity. So when we're talking about, first of all, ingredients, even having the ability to enter into a cell. That's enormous. Yeah, that is enormous because my understanding or perception is that the size of these molecules is so large, they're actually not even penetrating sometimes past the corneum. Well, the vast majority of skin care ingredients are too big to get into. They're even too big to get through the stratum corneum, which is a good thing because you don't want emulsifying wax to get into the epidermis and into the dermis and into the fibroblast. You don't want a seal alcohol, a sterile alcohol, but there are some molecules. In fact, there's quite a few molecules that do have an ability to get through the stratum corneum. Luckily, they're not necessarily going to go into a cell. Remember, the cell has to have a certain familiarity. That being said, there are some molecules that will get into the cell and can create problems. But you have two, two steps here. You got to get through the stratum corneum. That's number one. Then you got to get it through the epidermis. That's got to migrate your molecules to migrate through the layers of the epidermis and then has to go into the cell. So there's three places where three levels of penetration that have to occur before you're going to get a cellular effect. There's not a lot of molecules that can necessarily do that. There's some factors that are important in order to permit that molecule to get through the stratum corneum through the epidermis and eventually into a cell. Size is one and you know about the 500 Dalton rule. Most active materials, certainly most drugs and most cosmetic active materials like retinol and vitamin C and caffeine and forscalant and active molecules will pass the 500 Dalton rule. That doesn't necessarily mean you're going to get a cellular effect though. Remember, the cell has to recognize the molecule and the molecule has to somehow be able to interact with the cell so that the cell will say, hey, come on in, do your work. There's not a lot of molecules that will do that. Vitamin C does it and that's what makes vitamin C such an important ingredient and retinol does it and that's what makes retinol such an important ingredient and interestingly alpha hydroxy acids won't do it themselves but they will release parts of them, parts of themselves called protons which are electronic components that are released by acids. What makes something an acid is its ability to release protons but protons are released from acids and protons can get into the cell. So while glycolic acid isn't going to really get into the cell, the protons from glycolic acid can get into the cell and those protons can activate the cell and that's where you get all your good benefits for or as partially where you get a lot of your benefits from alpha hydroxy acids like glycolic acid. So whether or not glycolic acid can get into the cell and it's possible that glycolic acid is small enough to get into the cell, the protons themselves are what are doing the work, the little pieces of electrical energy from the glycolic acid and in fact they're actually drugs that you can take that will inhibit protons of the entrance to protons into the cell to dumb down cells. So have you heard of these things called proton pump inhibitors, PPI's? So proton pump inhibitors will actually keep protons from getting into cells so that they don't make acid. That's how they work to suppress acid production if you have heartburn or if you gird the thinking is by blocking the entrance of protons into the cells that make acid they won't make acid anymore and you won't have heartburn and those are the so the PPI. So the point being it's not always the ingredient that has to get into the cell in order to exhibit the effect. Sometimes the electrical energy from the ingredient is enough to activate the cell and give you some skin health benefits. Interesting. All right. So for clarity here we're saying that absorption means we have something that is entering the skin and into the blood. Into the blood. Which is something that's not really happening in cosmetics. Cosmetics. Right. Penetration we're saying is penetrating. Through the surface. Okay. Through the skin surface. And there are a few ingredients that do that and then even enter the cell. Yes. Retinol vitamins and retinol vitamin C are the ones that stand out in importance or the little pieces of electrical energy from alpha-hydroxy acids. You can also enhance penetration. Things like galvanic and ion tofaresis and exfoliation will enhance penetration. Using retinol before or an exfoliating ingredient like a colic acid before you put another ingredient on the skin will enhance the penetration of the active ingredients shaking up the stratum corneum a little bit to exfoliation or microdermabration or laser. You can also use chemicals or absorption enhancing chemicals. There's also little tricks that cosmetic chemists will do by creating they can create little bubbles that active ingredients can sit inside. And while the active ingredient may not be may not effectively penetrate the bubble will. Remember we said how familiarity is important. Well, the stratum corneum has a molecule in it that is extremely not only familiar if you use it in a cosmetic product but has a chemical structure that lends itself to penetration. These molecules are called phospholipids, lessethin being the classic example of a phospholipid. It's actually a complex of phospholipids and scientists can take lessethin and phospholipids and create a little bubble with them and then stick a molecule inside that bubble and then the bubble will enter into the will penetrate through the surface of the skin being familiar to the stratum corneum and having a chemical structure that lends itself to penetration. And that's called liposomal penetration and there are a lot of active ingredients that are said to be liposomes. There's also other sown means bubble and there's also other forms other sowns other bubbles that are made up of other molecules. There are things called niosomes and exosomes and ethosomes and these are all basically bubbles made of different chemicals that are designed to penetrate through the stratum corneum and help an active material get into the lower levels of the skin. Again, that doesn't mean it's going to get into the cell. There's only a few ingredients that will get into the cell or the the cell will respond to and those are basically limited to vitamins like retinol and vitamin C. A certain peptides will not. Peptides tend to be a little bit a bigger molecule but there's some tricks you can do for peptides by attaching them to a fat and that's another strategy for getting through the stratum corneum lipophilicity or faddiness. A stratum corneum as you know is a barrier to water but fatty molecules penetrate through the stratum corneum a little bit better and by taking a peptide which is water soluble and attaching it to a fat that will enhance the penetration of the peptide. Again, that doesn't necessarily mean you're going to get an effect at the cellular level but some peptides will give you a cell effect and there are some peptides that are naturally small enough. The most famous peptide probably the first cosmetic peptide. I think it was the first cosmetic peptide something called matrixel and matrixel is a small enough peptide that can get through the stratum corneum on its own and then can have cellular effects. So vitamins, peptides, hormones those will all have some cellular effects and if depending on their faddiness or the tricks that you use to enhance penetration you can get some cellular effects using these ingredients. So outside of being recognized by the skin or the cell the other reason for something to penetrate is going to be molecule size and that's where 500 gallon rule comes. Molecular size is a major parameter for penetration through the stratum corneum but there's other things that you can do to enhance penetration. Patches will work, alcohol will work, propylene glycol and other glycalls will enhance penetration. DMSO is a classic penetrating age you probably heard of DMSO. There's another penetrating ather. Sometimes you'll find in cosmetic products called a foxy dichlycall which is a glycall. So something is a larger molecule size you can still force that penetration. Yes, you can enhance, still enhance penetration by using these techniques, using other chemicals or exfoliation or myotrophoresis or galvanic. There's other ways you can do it. Molecular size is not the only parameter but it's an important one. I see. So once this ingredient enters the cell, like let's take vitamin C for instance, once that enters the cell what's happening? Well, depending on the ingredient in the case of vitamin C, vitamin C has some really interesting epigenetic effects. It can upregulate collagen production at the level of the fibroblast by turning on the genes or by supporting the genes that the production of collagen at the genetic level. Retinol is a classic epigenetic. You know what I mean by epigenetics? That means turns on the genes or activates the genes. Retinol and retinolic acid are classic epigenetic factors, hormones like DHEA that has some epigenetic effects or actually those are genetic effects. And then peptides, of course, peptides have genetic effects, things like matrixyl. So once things get into the cell, their effects are going to be at the level of the genetics. It doesn't have to get into the cell though. Like vitamin C has some antioxidant properties for the outside of the cell. There are molecules that are found in vegetables, phytosterols and phytonutrients and adaptogens. Those can have protective effects. They don't get into the cell necessarily, but they can have protective effects on the outside of the cell. And then the hydroxy acids, of course, the protons get into the cellular machinery to activate things like collagen production and cell division or cell growth, various cellular functions. Cosmetic science is really kind of fascinating. Oh, by the way, unmulsifying agents can also enhance penetration and surfactants can also enhance penetration. Sodium laurel sulfate, for example, is used sometimes in laboratory studies to test for the penetration of ingredients. Anything lipophilic is going to have a penetration enhancing effect, anything fatty. A terpenes, or another example of a penetrating aid, squalane is a classic. That's kind of like a terpenes and that's a classic penetrating aid. That concludes our show for today. And we thank you for listening. But if you just can't get enough of Ben Fuchs, the ASCP's rogue pharmacist, you can listen to a syndicated radio program at BrightsideBen.com. For more information on this episode or for ways to connect with Ben Fuchs or to learn more about ASCP, check out the show notes.