Ketoconazole Shampoo (DIY Recipe)

[MunenMuso]

I've been compounding my own hair loss topicals for quite a few years now.

Even though I create complex formulations, ketoconazole is by far one of the most difficult compounds I've worked with. No wonder it's included in "Class II of the Biopharmaceutical Classification System".

It's extremely difficult to solubilise ketoconazole at a therapeutic concentration of 2% (or even 1%).

I'm trying to create a non-irritating, "gentle" alternative to the Nizoral shampoo. So I can use it daily.

And I simply can't find any skin-friendly, non-toxic solvents that solubilise ketoconazole at concentrations of 2% (or 1%).

I'm purposefully avoiding the sulfates used in Nizoral.

The only other Ketoconazole shampoo that doesn't use sulfates is Regenpure DR and they are barely able to get the ketoconazole concentration up to 1%.

The things that I've had slight success with are:

- Polysorbate 80
- Reducing the pH
- Ethanol (not suitable for a shampoo formulation)
- Propylene glycol (not suitable for a shampoo formulation)

Any thoughts, ideas, suggestions? All will be greatly appreciated!

Thank you

P.S. I've read virtually all the clinical literature on ketoconazole dissolution even the studies behind paywalls.

 

[johnwester130]

I've been compounding my own hair loss topicals for quite a few years now.

Even though I create complex formulations, ketoconazole is by far one of the most difficult compounds I've worked with. No wonder it's included in "Class II of the Biopharmaceutical Classification System".

It's extremely difficult to solubilise ketoconazole at a therapeutic concentration of 2% (or even 1%).

I'm trying to create a non-irritating, "gentle" alternative to the Nizoral shampoo. So I can use it daily.

And I simply can't find any skin-friendly, non-toxic solvents that solubilise ketoconazole at concentrations of 2% (or 1%).

I'm purposefully avoiding the sulfates used in Nizoral.

The only other Ketoconazole shampoo that doesn't use sulfates is Regenpure DR and they are barely able to get the ketoconazole concentration up to 1%.

The things that I've had slight success with are:

- Polysorbate 80
- Reducing the pH
- Ethanol (not suitable for a shampoo formulation)
- Propylene glycol (not suitable for a shampoo formulation)

Any thoughts, ideas, suggestions? All will be greatly appreciated!

Thank you

P.S. I've read virtually all the clinical literature on ketoconazole dissolution even the studies behind paywalls.

Piroctone olamine and ketoconazole against hair loss

Piroctone olamine or ketoconazole? Which shampoo best stimulates hair growth? We specialize in hair loss in women and men.

www.hgspecialist.com

you don't need keto

 

[ecstatichamster]

I doubt ketoconazole is safe.

 

[rei]

I doubt ketoconazole is safe.

i doubt the amounts used topically pose any systemic risk. If they have even a slight positive effect on the skin the risk is not something to worry about

 

[ecstatichamster]

i doubt the amounts used topically pose any systemic risk. If they have even a slight positive effect on the skin the risk is not something to worry about

well everyone has their opinion of what they are okay with risk-wise. But if you are trying to fight fungus there may be better ways of doing that.

 

[Birdie]

I like Sebclair which is a Piroctone shampoo. Also like one by LaRoche Posay. I think there are two by LRP and one doesn't dry the scalp as much as the other.

 

[Birdie]

Ideas here:

The Best Piroctone Olamine Shampoos for Treating Seb Derm and Dry Scalp

 

[MunenMuso]

Piroctone olamine and ketoconazole against hair loss

Piroctone olamine or ketoconazole? Which shampoo best stimulates hair growth? We specialize in hair loss in women and men.

www.hgspecialist.com

you don't need keto

Thanks for the reply!

I would be more hesitant if I were you when making definitive statements like "you don't need this" or "you don't need that". Especially when there's only one study that backs your claims. Plus, the study isn't high quality.

Not to mention that you're referencing a commercial article which speaks of the KTZ, PTO, ZPT study and not the actual study itself.

As I said in my initial post, I've read all the clinical literature on ketoconazole. And I have the exact study you're referring to (not only the abstract that's available online but the full study).

The researchers in it seem to be mixing up two very different conditions.

Quote:

"A total of 150 men aged from18 to 65 years presenting with mild-to-moderate dandruff, telogen effluvium related to androgenic alopecia (Hamilton grade III) of the vertex were enrolled."

Telogen effluvium and androgenic alopecia are two completely different conditions. And just the fact that they are somehow mixing them together makes me doubt the validity of the entire study itself.

Also, piroctone olamine isn't a proven anti-androgen, whereas ketoconazole is.

I'm not after their anti-dandruff properties, I'm after the trichogenic effect of ketoconazole mediated by its anti-androgenic properties.

I doubt ketoconazole is safe.

Thanks for your reply!

It would be best if you back up your claims with at least some rudimentary evidence, heck, even an anecdote.

There's not even 1 study in the clinical literature which shows that the topical application of ketoconazole poses systemic risks.

Quote from fda.gov:

"The topical forms of ketoconazole that are applied to the skin or nails have not been associated with liver damage, adrenal problems, or drug interactions."

Only one study done on infants shows some detectable plasma levels, but they applied 40g of 2% ketoconazole cream which equals to a whopping 800 mg of topical ketoconazole. Not to mention that it was done on babies which have more easily permeable skin and they used a leave-on formulation, i.e cream and not a rinse-off shampoo.

"Plasma concentrations of ketoconazole were not detectable after topical administration of Nizoral 2% Cream in adults on the skin. In one study in infants with seborrhoeic dermatitis (n = 19), where approximately 40 g of Nizoral 2% cream was applied daily on 40% of the body surface area, plasma levels of ketoconazole were detected in 5 infants, ranging from 32 to 133 ng/mL."

i doubt the amounts used topically pose any systemic risk. If they have even a slight positive effect on the skin the risk is not something to worry about

Thank you for the reply!

Yes, I agree.

well everyone has their opinion of what they are okay with risk-wise. But if you are trying to fight fungus there may be better ways of doing that.

Nowhere in my initial post did I mention "fighting fungus".

I'm using ketoconazole for its antiandrogenic properties in a hair loss context.

I like Sebclair which is a Piroctone shampoo. Also like one by LaRoche Posay. I think there are two by LRP and one doesn't dry the scalp as much as the other.

Ideas here:

Thanks for that!

Yes, I'm very aware of the piroctone olamine shampoos.

 

[ecstatichamster]

It’s systemically toxic. That is enough of a red flag. Anything you put on skin gets absorbed. Are we now trusting the FDA?

 

[MunenMuso]

It’s systemically toxic. That is enough of a red flag. Anything you put on skin gets absorbed. Are we now trusting the FDA?

"Anything you put on your skin gets absorbed"

That's entirely and utterly false.

When it comes to transdermal absorption of a given compound, molecular weight and molecular geometry are the determining factors (but also chemical polarity, lipophilic/lipophobic properties and more).

Why do you think you don't drown every time you take a shower? Because water is repelled by the skin...

Why do you think we need vehicles and permeation enhancers to improve the transdermal absorption of compounds?

What you're saying speaks volumes about your understanding of pharmacodynamics and pharmacokinetics, or the lack thereof.

The molecular weight of ketoconazole is ~531 daltons which makes it very difficult to pass the stratum corneum.

However, some emerging hypotheses and anecdotes claim that the mid 500s in molecular weight might be the "gold zone" for topical medications which need to have a limited systemic absorption. Because the molecular weight is small enough to allow the compound to get to the derma papilla (in the case of KTZ) but large enough to prevent it from going further than that.

Even though this is a hypothesis, the clinical data clearly shows no systemic absorption.

Not to mention that the primary reason why oral ketoconazole is hepatoxic is because due to it being "oral" in nature doesn't allow it to skip 1st pass metabolism, whereas, topical does.

So in the highly unlikely event of a small percentage of the topical ketoconazole going systemic, it will be far less toxic.

But again, the average oral dose which is deemed toxic is 400 - 800mg of ketoconazole, and here we're talking about only 20mg of topically administered KTZ which is more than enough to induce a trichogenic effect.

I quoted the FDA because they have a summarised statement on the systemic side-effects of topical ketoconazole. I didn't want to inundate my already long post with additional quotes from independent studies.

And please don't tell me you're one of these people who "doesn't trust" the FDA.

If you don't trust the FDA, then you should disregard all of the chemotherapy drugs, heart medication, etc. that they've helped develop, which by the way, are saving lives as we speak.

The FDA has brought far more good than bad to the world of science, and this is non-negotiable. Only dilettantes and flat-earth proponents will say otherwise.

 

[ecstatichamster]

"Anything you put on your skin gets absorbed"

That's entirely and utterly false.

When it comes to transdermal absorption of a given compound, molecular weight and molecular geometry are the determining factors (but also chemical polarity, lipophilic/lipophobic properties and more).

Why do you think you don't drown every time you take a shower? Because water is repelled by the skin...

Why do you think we need vehicles and permeation enhancers to improve the transdermal absorption of compounds?

What you're saying speaks volumes about your understanding of pharmacodynamics and pharmacokinetics, or the lack thereof.

The molecular weight of ketoconazole is ~531 daltons which makes it very difficult to pass the stratum corneum.

However, some emerging hypotheses and anecdotes claim that the mid 500s in molecular weight might be the "gold zone" for topical medications which need to have a limited systemic absorption. Because the molecular weight is small enough to allow the compound to get to the derma papilla (in the case of KTZ) but large enough to prevent it from going further than that.

Even though this is a hypothesis, the clinical data clearly shows no systemic absorption.

Not to mention that the primary reason why oral ketoconazole is hepatoxic is because due to it being "oral" in nature doesn't allow it to skip 1st pass metabolism, whereas, topical does.

So in the highly unlikely event of a small percentage of the topical ketoconazole going systemic, it will be far less toxic.

But again, the average oral dose which is deemed toxic is 400 - 800mg of ketoconazole, and here we're talking about only 20mg of topically administered KTZ which is more than enough to induce a trichogenic effect.

I quoted the FDA because they have a summarised statement on the systemic side-effects of topical ketoconazole. I didn't want to inundate my already long post with additional quotes from independent studies.

And please don't tell me you're one of these people who "doesn't trust" the FDA.

If you don't trust the FDA, then you should disregard all of the chemotherapy drugs, heart medication, etc. that they've helped develop, which by the way, are saving lives as we speak.

The FDA has brought far more good than bad to the world of science, and this is non-negotiable. Only dilettantes and flat-earth proponents will say otherwise.

Completely disagree. Of course it’s absorbed. Ridiculous. The skin isn’t an impervious barrier. And no I don’t trust the FDA. They are a terrible promoter of horrific Pharma. i can’t think of anything good they have done.

 

[MunenMuso]

Completely disagree. Of course it’s absorbed. Ridiculous. The skin isn’t an impervious barrier. And no I don’t trust the FDA. They are a terrible promoter of horrific Pharma. i can’t think of anything good they have done.

You didn't address one single line of my argument.

You have no facts, no empirical evidence, no anecdotes even.

You don't understand pharmacodynamics & pharmacokinetics.

You don't understand basic chemistry.

You're an "FDA denier" and you're saying that they haven't done anything good, when I already stated clearly how they've done more good than bad and how they've positively impacted the world of science.

Without willingly making ad hominem attacks, it feels like I'm talking to a 5-year old.

Please, refrain from posting here in this thread again if you don't have anything of value to say.

Thank you.

 

[ecstatichamster]

You didn't address one single line of my argument.

You have no facts, no empirical evidence, no anecdotes even.

You don't understand pharmacodynamics & pharmacokinetics.

You don't understand basic chemistry.

You're an "FDA denier" and you're saying that they haven't done anything good, when I already stated clearly how they've done more good than bad and how they've positively impacted the world of science.

Without willingly making ad hominem attacks, it feels like I'm talking to a 5-year old.

Please, refrain from posting here in this thread again if you don't have anything of value to say.

Thank you.

do not tell me where I can post. That is not up to you.

 

[rei]

"Anything you put on your skin gets absorbed"

That's entirely and utterly false.

When it comes to transdermal absorption of a given compound, molecular weight and molecular geometry are the determining factors (but also chemical polarity, lipophilic/lipophobic properties and more).

Why do you think you don't drown every time you take a shower? Because water is repelled by the skin...

Why do you think we need vehicles and permeation enhancers to improve the transdermal absorption of compounds?

What you're saying speaks volumes about your understanding of pharmacodynamics and pharmacokinetics, or the lack thereof.

The molecular weight of ketoconazole is ~531 daltons which makes it very difficult to pass the stratum corneum.

However, some emerging hypotheses and anecdotes claim that the mid 500s in molecular weight might be the "gold zone" for topical medications which need to have a limited systemic absorption. Because the molecular weight is small enough to allow the compound to get to the derma papilla (in the case of KTZ) but large enough to prevent it from going further than that.

Even though this is a hypothesis, the clinical data clearly shows no systemic absorption.

Not to mention that the primary reason why oral ketoconazole is hepatoxic is because due to it being "oral" in nature doesn't allow it to skip 1st pass metabolism, whereas, topical does.

So in the highly unlikely event of a small percentage of the topical ketoconazole going systemic, it will be far less toxic.

But again, the average oral dose which is deemed toxic is 400 - 800mg of ketoconazole, and here we're talking about only 20mg of topically administered KTZ which is more than enough to induce a trichogenic effect.

I quoted the FDA because they have a summarised statement on the systemic side-effects of topical ketoconazole. I didn't want to inundate my already long post with additional quotes from independent studies.

And please don't tell me you're one of these people who "doesn't trust" the FDA.

If you don't trust the FDA, then you should disregard all of the chemotherapy drugs, heart medication, etc. that they've helped develop, which by the way, are saving lives as we speak.

The FDA has brought far more good than bad to the world of science, and this is non-negotiable. Only dilettantes and flat-earth proponents will say otherwise.

take a long bath and see how water is absorbed by the skin to such degree it becomes wrinkly.

 

[MunenMuso]

"Anything you put on your skin gets absorbed"

take a long bath and see how water is absorbed by the skin to such degree it becomes wrinkly.

I hope that you're joking and/or being sarcastic.

I always wonder, how do people not even "google" before they speak. It can save you a ton of embarrassment.

You could've just googled "does water absorb through the skin".

And this is the answer you get in the featured snippet:



You don't even have to go and look at empirical data for a question as rudimentary as this one.

We are talking about 'transdermal absorption' here.

Again, one of your best friends is the website www.justgoogleit.com

Use it and save face.

 

[rei]

I hope that you're joking and/or being sarcastic.

I always wonder, how do people not even "google" before they speak. It can save you a ton of embarrassment.

You could've just googled "does water absorb through the skin".

And this is the answer you get in the featured snippet:

View attachment 22931

You don't even have to go and look at empirical data for a question as rudimentary as this one.

We are talking about 'transdermal absorption' here.

Again, one of your best friends is the website www.justgoogleit.com

Use it and save face.

Maybe you should use common sense instead of listening to propaganda. If it is in your skin is it not absorbed? I guess your skin is not part of your body so donate it to me and see how you feel. If it goes into the skin, it changes how your body as a whole functions. You are delusional if you think significantly increasing the water content of the skin has no systemic effects.

 

[ecstatichamster]

A family member close to me thinks use of this type of shampoo is causing hypogonadalism. He is in his early thirties. He stopped using it. About 3 years of use. Hopefully he will recover if this indeed is the cause.

 

[Birdie]

Thanks for the reply!

I would be more hesitant if I were you when making definitive statements like "you don't need this" or "you don't need that". Especially when there's only one study that backs your claims. Plus, the study isn't high quality.

Not to mention that you're referencing a commercial article which speaks of the KTZ, PTO, ZPT study and not the actual study itself.

As I said in my initial post, I've read all the clinical literature on ketoconazole. And I have the exact study you're referring to (not only the abstract that's available online but the full study).

The researchers in it seem to be mixing up two very different conditions.

Quote:

"A total of 150 men aged from18 to 65 years presenting with mild-to-moderate dandruff, telogen effluvium related to androgenic alopecia (Hamilton grade III) of the vertex were enrolled."

Telogen effluvium and androgenic alopecia are two completely different conditions. And just the fact that they are somehow mixing them together makes me doubt the validity of the entire study itself.

Also, piroctone olamine isn't a proven anti-androgen, whereas ketoconazole is.

I'm not after their anti-dandruff properties, I'm after the trichogenic effect of ketoconazole mediated by its anti-androgenic properties.




Thanks for your reply!

It would be best if you back up your claims with at least some rudimentary evidence, heck, even an anecdote.

There's not even 1 study in the clinical literature which shows that the topical application of ketoconazole poses systemic risks.

Quote from fda.gov:

"The topical forms of ketoconazole that are applied to the skin or nails have not been associated with liver damage, adrenal problems, or drug interactions."

Only one study done on infants shows some detectable plasma levels, but they applied 40g of 2% ketoconazole cream which equals to a whopping 800 mg of topical ketoconazole. Not to mention that it was done on babies which have more easily permeable skin and they used a leave-on formulation, i.e cream and not a rinse-off shampoo.

"Plasma concentrations of ketoconazole were not detectable after topical administration of Nizoral 2% Cream in adults on the skin. In one study in infants with seborrhoeic dermatitis (n = 19), where approximately 40 g of Nizoral 2% cream was applied daily on 40% of the body surface area, plasma levels of ketoconazole were detected in 5 infants, ranging from 32 to 133 ng/mL."




Thank you for the reply!

Yes, I agree.



Nowhere in my initial post did I mention "fighting fungus".

I'm using ketoconazole for its antiandrogenic properties in a hair loss context.





Thanks for that!

Yes, I'm very aware of the piroctone olamine shampoos.

I lost track of your initial question. Whenever @ecstatichamster joins in, I bend my thought!

 

[ecstatichamster]

I lost track of your initial question. Whenever @ecstatichamster joins in, I bend my thought!

thanks @Birdie you are very kind.

 

[OccamzRazer]

You're an "FDA denier" and you're saying that they haven't done anything good, when I already stated clearly how they've done more good than bad and how they've positively impacted the world of science.

The FDA may have done some good...

...but more good would've been done if they didn't exist. lol.

The FDA has a proven track record of obfuscating scientific breakthroughs that aren't compatible with their financial interests.