New Study: Topical Cetirizine For Androgenetic Alopecia Shows Promise

HairSuit

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Finally received my topical ceti. Been using it past couple nights. Do y’all know if it’s okay to apply it to wet, towel dried hair? I was told to do this with minoxidil, and so that how I’ve done it for years. Didn’t know if that would negatively affect the results?
 

Spice_Lord

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Whilst you've said water is an inappropriate vehicle, is alcohol as used in the study fine ? I've heard some say alcohol degrades the Cetirizine, however if you're making daily batches does this remain a problem ?

I remember reading a study when I was looking into Cetirizine that did say it reacted with EtOH. I can't remember the time scale though. One thing to remember with topical skin absorption is that retention is a big factor. You want that cetirizine to be in the vehicle and in contact with your skin as long as possible. That could be a few hours, and over those hours it could react with the EtOH. I'll see if I can find the study, but I'd rather formulate it in something else.
 

jgray201

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I have some what intermediate experience working with drug formulations as a pharmacist in the U.S.

After seeing many here have some what mixed success with topical cetirizine. I would like to point out why it is most likely having no effect (assuming that it does have activity on PGD2). Cetirizine is a zwitterion, meaning it has both a acidic group, and a basic group. This is important because these groups will become charged depending on the pH relative to the pKa of the molecule.

For Cetirizine it looks like the pKa of the basic group is 7.7 and the pKa of the acidic group is 3.6. This means that at a pH of about 7 or below, which is mostly the pH in a formulation dissolved in water, BOTH the basic and acidic group is charged.

Why is being charged bad? The skin is a lipophilic substance, and like attracts like, meaning that it will not readily absorb a charged molecule. Basically, you are wasting drug applying cetirizine dissolved in water on your head.

How do we bypass this? My theory revolves around making a nanoemulsion. Essentially suspending nano-sized droplets of water containing cetirizine in olive oil. The oil will usher the cetirizine to the follicle and disrupt the surface, essentially allowing the cetirizine to sneak in past the defense of the skin.

All you need for this is cetirizine, olive oil, and a surfactant (to form the nano droplets). I will be conducting trials on myself using this preparation. I also plan on adding d-limonene to the water phase to hopefully help with additional penetration.

I am just following the directions detailed in this study, except substituting out the drug they used for cetirizine.


Crocin loaded nano-emulsions: Factors affecting emulsion properties in spontaneous emulsification

I will let you guys know how it goes, currently I am waiting on some glassware to get here from eBay, and then I will begin.

Hi mate, appreciate your expertise. what are your thoughts on this study? The vehicle used seems to suggest that Cetirizine can be used in a vehicle with ethanol in? I must admit im not aware of what the various other products are so doubt i woild be able to replicate it.

https://www.google.co.uk/url?sa=t&s...FjACegQIBBAB&usg=AOvVaw0Jna0x-Fc3olecR_MZUlvD

The hair loss study with Cetirizine used ethanol and a cyclo-silicone product in the lotion. In your opinion could this kind of vehicle work against the 'charging' process that you mention?
 

hairloss_user

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I bought cetirizine pills and distilled water. Think I would be good to go with these ingredients?
 

opti

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I bought cetirizine pills and distilled water. Think I would be good to go with these ingredients?
Maybe try to add propylene glycol or use a dermaroller for penetration...only water as vehicle isn't that good in terms of penetrating
 

sunchyme1

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ffs guys we must be able to figure out exactly what kind of vehicle is best for this stuff
 

jgray201

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ffs guys we must be able to figure out exactly what kind of vehicle is best for this stuff

Lol - do you know what a cyclo silicone pentamer is?
I'm going to try and replicate what i think the study used. I have some cet powder, ethyl alcohol and cyclomethicone which i think is the silicone bit. Its used in many other cosmetics.
 

opti

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Maybe try hydropropyl chitosan as firm agent when using the water solution so the water solution won't evaporate that quick
 

sunchyme1

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Lol - do you know what a cyclo silicone pentamer is?
I'm going to try and replicate what i think the study used. I have some cet powder, ethyl alcohol and cyclomethicone which i think is the silicone bit. Its used in many other cosmetics.

no idea mate

but surely this problem cannot be that difficult to solve

so much confusion about its vehicle

there are enough smart people here to figure this out
 

Spice_Lord

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no idea mate

but surely this problem cannot be that difficult to solve

so much confusion about its vehicle

there are enough smart people here to figure this out

The use of the lotion would not do anything to solve the pH issue which leads to the charging of the molecule. Basically nothing you could do would leave cetirizine unionized in solution (any buffer would leave at least part of the molecule charged, additionally you don't want to make the solution too acidic or basic as it could damage the flora of the scalp).

If you do not want to go through the trouble of making a nanoemulsion (essentially is a liposome-esk formulation), as I am doing (or you just don't like putting oil on the head).

I would try 1% solution of Transcutol P (this is quite cheap and used frequently), try varying amounts of propylene glycol, and add d-limonene if you wish (terpenes aide in penetration as well). There really is no "perfect vehicle", all you can do is experiment, but I would bet on liposomes or a nanoemulsion being the best bet at sneaking cetirizine in.

The article below is pretty interesting, and I am considering trying to see how feasible it would be to produce these liposomes in my garage.

Genç R, Ortiz M, O'sullivan CK. Curvature-tuned preparation of nanoliposomes. Langmuir. 2009;25(21):12604-13.

It requires no sonicator or anything else, just spontaneous production of liposomes through alteration of the pH.

***My end goal is to try liposomal IGF-1. I believe the hairloss ultimately boils down to TGFB2 overexpression, and IGF-1 underexpression in the scalp.
 

Spice_Lord

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Hello everyone,

I have been absolutely consumed with this for the past month. Over the past 2 weeks, I have been able to formulate and do some brief testing on a formulation, thanks to a huge favor by a friend of mine who has access to a lab.

The result that was formulated is a niosomal gel. Here is some information from our testing:

Size of niosomes: 34 microns
Encapsulation efficiency of cetirizine: >90%
Ex vivo drug permeation: 1% (over 24 hours)
Drug deposition into stratum corneum: 88% (indicating that this will slowly release through out day AND maintain drug levels within the dermal-epidermal layers)
Amount of cetirizine per gram: ~20 mg

Stability of gel: 3 months refrigerated (estimate based on the stability of similar niosomal gels)
Cost per gram: ~$1-2

1 gram should cover the entire scalp. The way this was formulated was to contain the drug to the skin layers, and avoid release into systemic circulation.
 

itsjustsimon

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Hello everyone,

I have been absolutely consumed with this for the past month. Over the past 2 weeks, I have been able to formulate and do some brief testing on a formulation, thanks to a huge favor by a friend of mine who has access to a lab.

The result that was formulated is a niosomal gel. Here is some information from our testing:

Size of niosomes: 34 microns
Encapsulation efficiency of cetirizine: >90%
Ex vivo drug permeation: 1% (over 24 hours)
Drug deposition into stratum corneum: 88% (indicating that this will slowly release through out day AND maintain drug levels within the dermal-epidermal layers)
Amount of cetirizine per gram: ~20 mg

Stability of gel: 3 months refrigerated (estimate based on the stability of similar niosomal gels)
Cost per gram: ~$1-2

1 gram should cover the entire scalp. The way this was formulated was to contain the drug to the skin layers, and avoid release into systemic circulation.

Please post back your results
 

Ollie

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Hello everyone,

I have been absolutely consumed with this for the past month. Over the past 2 weeks, I have been able to formulate and do some brief testing on a formulation, thanks to a huge favor by a friend of mine who has access to a lab.

The result that was formulated is a niosomal gel. Here is some information from our testing:

Size of niosomes: 34 microns
Encapsulation efficiency of cetirizine: >90%
Ex vivo drug permeation: 1% (over 24 hours)
Drug deposition into stratum corneum: 88% (indicating that this will slowly release through out day AND maintain drug levels within the dermal-epidermal layers)
Amount of cetirizine per gram: ~20 mg

Stability of gel: 3 months refrigerated (estimate based on the stability of similar niosomal gels)
Cost per gram: ~$1-2

1 gram should cover the entire scalp. The way this was formulated was to contain the drug to the skin layers, and avoid release into systemic circulation.

Is this something that us normal individuals at home could produce - or something similar for the best results ?

We have a lot of people on this forum who are sort of spotlighted as 'clever' and when referring to topical drugs (Like Ru58841) say because the dalton weight is x and it dissolves in alcohol and Pg then it 'should' have no problem being the ideal vehicle. However, you've clearly demonstrated given your background that it is far more complicated when forming the correct vehicle.

As Ru is a topical that is heavily utilised on the forum do you think you could shed any light onto it, and recommend a suitable vehicle to get the best out of the drug ?
 

abcdefg

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Hello everyone,

I have been absolutely consumed with this for the past month. Over the past 2 weeks, I have been able to formulate and do some brief testing on a formulation, thanks to a huge favor by a friend of mine who has access to a lab.

The result that was formulated is a niosomal gel. Here is some information from our testing:

Size of niosomes: 34 microns
Encapsulation efficiency of cetirizine: >90%
Ex vivo drug permeation: 1% (over 24 hours)
Drug deposition into stratum corneum: 88% (indicating that this will slowly release through out day AND maintain drug levels within the dermal-epidermal layers)
Amount of cetirizine per gram: ~20 mg

Stability of gel: 3 months refrigerated (estimate based on the stability of similar niosomal gels)
Cost per gram: ~$1-2

1 gram should cover the entire scalp. The way this was formulated was to contain the drug to the skin layers, and avoid release into systemic circulation.

IMO there should be a sticky with all this crap in it for RU for anyone that wants to experiment with it. Why does everyone need to research and invent all this over and over again? Some new guy wants to try RU he can just read this if finasteride didnt work.
 

Ollie

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IMO there should be a sticky with all this crap in it for RU for anyone that wants to experiment with it. Why does everyone need to research and invent all this over and over again? Some new guy wants to try RU he can just read this if finasteride didnt work.

This is Cetirizine.
 

sunchyme1

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Hello everyone,

I have been absolutely consumed with this for the past month. Over the past 2 weeks, I have been able to formulate and do some brief testing on a formulation, thanks to a huge favor by a friend of mine who has access to a lab.

The result that was formulated is a niosomal gel. Here is some information from our testing:

Size of niosomes: 34 microns
Encapsulation efficiency of cetirizine: >90%
Ex vivo drug permeation: 1% (over 24 hours)
Drug deposition into stratum corneum: 88% (indicating that this will slowly release through out day AND maintain drug levels within the dermal-epidermal layers)
Amount of cetirizine per gram: ~20 mg

Stability of gel: 3 months refrigerated (estimate based on the stability of similar niosomal gels)
Cost per gram: ~$1-2

1 gram should cover the entire scalp. The way this was formulated was to contain the drug to the skin layers, and avoid release into systemic circulation.

so let me get this straight

cet in alcohol, as used in the studies, isnt optimal because it degrades it. even if you make fresh batches, your not getting the maximum benefit. once its been applied to the scalp, it starts degrading throughout the day

ceti in water is useless because it doesnt penetrate the scalp

what your doing here is making sure it penetrates the scalp and stays useful throughout the whole day

so your method should product far superior results than those in the studies?
 

Spice_Lord

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also @Spice_Lord what else are your using at the moment for your hair

and whats your age/norwood level

so we get some perspective

I am 27 years old, intact hairline, but probably Norwood III vertex. I used finasteride from 22 to 25 before stopping because I felt like it was negatively impacting my mood, etc.

I believe that yes this could be better than the what was used in the study. The formulation in the study didn't do any skin permeation tests or anything so I cannot say for sure though. It also depends on if Cetirizine needs to directly reach the hair follicle, or if just targeting eosinophils and other cells in the epidermis and dermis is enough. I don't know how the niosomal formulation directly targets/effects the hair follicle. But, I would bet on it being better because it forms a depot in stratum corneum and continuously releases from it.

As for topical formulation and what is best. It really depends on the drug and what you want to do. Transdermal penetration is MUCH different than local topical penetration. Transdermal assumes that it reaches systemic circulation.

In general what impacts absorption into the skin for transdermal delivery is:

- size of drug (< 400 Da)
- skin hydration of the site (basically want an occlusive barrier, through ointment etc)
- drug vehicle (drug should be more attracted to skin than the vehicle)
- retention (how long the drug is in contact with the skin)
- concentration of the drug in vehicle
- micro needling and other disruptive processes of the skin can impact absorption
- heat can also increase absorption

This is all for successful transdermal delivery however, in terms of hairloss, we do not necessarily want transdermal absorption, we do not want these drugs to go systemic. We want them to stay and work locally, which is what the niosomal formulation I detailed above will do.

**EDIT**

I forgot to mention that, yes, niosomes are quite easy to make, it may not be perfect in terms of size (like nanometers bc you need a sonicator or you could perhaps use extrusion for a cheaper alternative), but I made the above niosomes with no sonicator just fine. Many formulations may require a rotovap but you can build one yourself for fairly cheap.
 
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