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Penetration enhancer?
I am working on a protein/vitamin/mineral topical solution.What would be the best penetration enhancer to make sure that the entire solution penetrates deep into the dermis??Propylene glycol doesnt work, its not strong enough.Any help would be appreciated -
25 Replies
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The answer is more or less nothing.
There is a reason most things which need systemic access are formulated to be injected or ingested.First of all different chemicals can function as a penetration enhancer, but they may not increase the penetration for the same molecule.
minerals (ie metals we need) are inherently ionic and you will not get any of them absorbed through the skin no matter what you try.
Some vitamins can be formulated for dermal absorbance retinol, tocopheryl acetate for instance, but you do not mention which.
proteins are as an even broader class than vitamins and sure some proteins may absorb, but that is highly dependent on the structural features of the given protein.
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First question is how did you determine that propylene glycol doesn’t work?
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Dimethylsulfoxide/DMSO is the only penetration enhancer that I know of, we use it as extravasation antidote.
Liposomal skin actives are said to penetrate deeper into the dermis. I just read an article about the quality of liposomes, those of a less quality not penetrating at all. I’ve bought Rovisome CE Plus a while ago, with vitamins C and E in liposomes. Haven’t used it yet and I don’t expect much from it, but I like to experiment.
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DMSO is not generally used in Cosmetics. It is also not as innocuous as many believe.Dimethyl Isosorbide (DMI) is more common.
Or Ethoxydiglycol;
In the end, these are NOT raw materials for a novice. If in fact any real absorption was accomplished to any area other than the uper layers of the skin, it quickly becomes a drug NOT a Cosmetic.In the end, it is highly doubtful that you will get any real absorption of the actives NOR should you. -
@Microformulation
In the end, these are NOT raw materials for a novice. If in fact any real absorption was accomplished to any area other than the uper layers of the skin, it quickly becomes a drug NOT a Cosmetic.In the end, it is highly doubtful that you will get any real absorption of the actives NOR should you.I totally agree!
(I didn’t mention the DMSO as a tip to put in cosmetic formulations, I just mentioned it as the only penetration enhancer that I personally know of.) -
DMSO would definitely be an irresponsible option. I remember reading an article about DMSO accidentally increasing the absorption of incidental heavy metals found in whatever raw material they were using. Unfortunately I can’t find it because every result I see is people claiming to “detox” with DMSO. Ironic, huh?
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The Ordinary use DMI in many of their products. But in many cases you don’t really need the product to penetrate deep. It really depends on your actives and the formula in general. “Propylene glycol doesnt work, its not strong enough” is a blanket statement.
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DMSO is widely used as a penetration agent in lots of creams that contain other substances (eg. Aloe Vera, Hyaluronic acid, Vitamin E, B17……..etc…….etc).
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@dynamin Notice how they all write: Intended for use as a solvent only (or something to that effect), that is likely there in the hope it will keep them out of legal issues when using DMSO.While standing with what I previously wrote, another option for a penetration enhancer Tetrahydropiperine, which will likely increase the bioavailability of your vitamins.Fair warning, keep an eye out for regulations. As @m@Microformulation mentioned you get close to a Drug in the US. You may also Borderline Drug/Medical Device in the EU.
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ngarayeva001 said:The Ordinary use DMI in many of their products. But in many cases you don’t really need the product to penetrate deep. It really depends on your actives and the formula in general. “Propylene glycol doesnt work, its not strong enough” is a blanket statement.Actually, my solution has to penetrate into the papilla of the hair follicle
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Sibech said:@dynamin Notice how they all write: Intended for use as a solvent only (or something to that effect), that is likely there in the hope it will keep them out of legal issues when using DMSO.While standing with what I previously wrote, another option for a penetration enhancer Tetrahydropiperine, which will likely increase the bioavailability of your vitamins.Fair warning, keep an eye out for regulations. As @m@Microformulation mentioned you get close to a Drug in the US. You may also Borderline Drug/Medical Device in the EU.
Fair point Sibech, but if people had gotten sick from their DMSO products they wouldve been sued into oblivion by now already
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@Dynamin What would they have been sued for? You cannot sue a properly labelled solvent, which the end-user abused, can you? (I don’t know, I am not an attorney nor am I based in the US).
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Dynamin said:Actually, my solution has to penetrate into the papilla of the hair follicle
What for? As far as I know, follicles feed on blood from the inside, and not something from the outside. Ingredients long fall into the dermis. In addition, the issue of convenience: propylene glycol, for example, gives oily scalp.
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Microformulation said:DMSO is not generally used in Cosmetics. It is also not as innocuous as many believe.and that’s why it’s been banned in European cosmetics since 1979
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Sibech said:@Dynamin What would they have been sued for? You cannot sue a properly labelled solvent, which the end-user abused, can you? (I don’t know, I am not an attorney nor am I based in the US).
If I’m injured by someones product, it doesnt matter how many warning labels they put on it, they can still be held liable. Especially if the injuries are serious enough
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Bill_Toge said:Microformulation said:DMSO is not generally used in Cosmetics. It is also not as innocuous as many believe.
and that’s why it’s been banned in European cosmetics since 1979
If it has been banned, there sure are a lot of UK outlets selling it:https://www.google.ca/search?q=dmso+site:.co.uk&lr=&source=lnms&tbm=isch&sa=X&ved=0ahUKEwiwvbeNncbgAhXDyoMKHXM2BAUQ_AUIDigB&biw=1280&bih=551And this was before BREXIT of course
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SauerLaura said:Dynamin said:Actually, my solution has to penetrate into the papilla of the hair follicle
What for? As far as I know, follicles feed on blood from the inside, and not something from the outside. Ingredients long fall into the dermis. In addition, the issue of convenience: propylene glycol, for example, gives oily scalp.
Laura, the product I’m working on is a minoxidil supplement, and only needs to go down to the dermis as far as the papilla resides
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@Dynamin
Coincidentally I’ve just arrived at this chapter in a cosmetic handbook that I’m reading. I can try to copy the chapter if you like? (It also mentions vitamins and Minoxidil btw) -
Dynamin said:Bill_Toge said:Microformulation said:DMSO is not generally used in Cosmetics. It is also not as innocuous as many believe.
and that’s why it’s been banned in European cosmetics since 1979
If it has been banned, there sure are a lot of UK outlets selling it:https://www.google.ca/search?q=dmso+site:.co.uk&lr=&source=lnms&tbm=isch&sa=X&ved=0ahUKEwiwvbeNncbgAhXDyoMKHXM2BAUQ_AUIDigB&biw=1280&bih=551And this was before BREXIT of course@Dynamin Strictly speaking they are not selling it as cosmetics, and since it’s written as a chemical it does not fall under the cosmetic regulation but REACH and CLP (possibly others too) in the EU.As for the “But others are doing it, that does not mean it is legal nor that you should. -
Sibech said:@Dynamin Strictly speaking they are not selling it as cosmetics, and since it’s written as a chemical it does not fall under the cosmetic regulation but REACH and CLP (possibly others too) in the EU.if anything, many of these products are unlicensed medicines, which would put their distributors even further up that infamous creek without a paddle if they were to get caught
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Dynamin said:ngarayeva001 said:The Ordinary use DMI in many of their products. But in many cases you don’t really need the product to penetrate deep. It really depends on your actives and the formula in general. “Propylene glycol doesnt work, its not strong enough” is a blanket statement.Actually, my solution has to penetrate into the papilla of the hair follicle
Then you can look into Minoxidil formulations.
Most comprise ethyl alcohol and propylene glycol. -
@Bill_Toge I completely agree, of course, it is impossible to say for certain as it is evaluated on a case-by-case basis. Having a solvent in a cream base makes no sense however and if someone were to report them their local competent authority I am certain we would see it on Rapex/”Safety Gate”.@Dynamin have you considered if you should just have the drug produced as a tablet/solution for drinking instead, seems easier. (I am disregarding possible patents).
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DMSO is used in high concentrations for arthritis creams, and have been vets applying it topically at 70-100% strength for decades. I believe the issue is more what is being used with it and purity. Water a formulation with DMSO causes DMSO to heat up on skin contact which can cause discomfort or irritation to some.But I saw a product paper where DMSO was used as a negative control for a hair active. A 10% DMSO solution significantly suppressed viability/metabolism ofHFDPc and ORSc proliferation. So should DMSO be avoided then at all costs for topical hair products?Propylene glycol also causes irritation commonly in the large amounts as a solvent in hair products which can also speed hairloss.So the question is what are the best/safest solvents for specifically hair topicals that aren’t likely to cause irritation/promote further hairloss?
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So frequently I have turned to this website for reliable and useful information that I’ve come to recognize the screen names of many of the helpful experts here, who often send me off with more things to research to find my answer, but because of them, I DO find it. I’m glad to see none of those screen names I usually recognize, in this thread.
If someone asks a question about or proposes a practical application of DMSO, information on its regulation is helpful, but ancillary. I’d expect replies with scientific instruction on how best to formulate with it, including safety concerns and risks, as well as critical scientific analysis of the proposal. I’m not an expert or advocate on or for DMSO, but I know BS when I smell it, and that I have, in much of what I’ve read, all over the place, for and against it. It’s controversial, I get THAT, and it’s fine to address that. But it’s not Anthrax, it’s not illegal, and not all of us are here to formulate something that’s intended for a shelf in a store. In this case, the OP didn’t even bring it up - DMSO was merely offered as an option for the answer requested. The inrush or finger wagging, clucking and moralizing wasn’t scientific, wasn’t helpful, and though it was meant to discourage, I can only see how it would make a scientific mind hunger for more.
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If something is or not a penetration enhancer is relative and depends on the whole formulation and the ingredient whose penetration is supposed to be enhanced. For example, the same penetration enhancer dimethyl isosorbide might increase penetration of dihydroxyacetone while impede penetration of salicylic acid. However, this depends on the whole formula, concentration of each ingredient etc. Therefore how successful something is at penetrating skin needs to be tested experimentally for every new formulation (if this a goal).
Furthermore, something that increases penetration to dermis might not necessarily increase penetration to pilosebaceous unit, while the latter might be more beneficial in the case of some acne medication.
While there is this idea, that ingredients need to penetrate to living layers to “work”, cosmetics are perfectly capable to perform as intended even if their action is located in the uppermost layers of stratum corneum.
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