Climbazole leave on lotion (moisturiser) - Cosmetic Science Talk

Climbazole leave on lotion (moisturiser)

I am trying to make a climbazole leave on lotion. I need to make my own because the ones on the market are no good - they either have food grade oils for malassezia (the thing I am trying to target as it is the cause of seborrehic dematitis) or chemicals that give me a bad skin reaction. I am first dissolving climbazole in MCT oil (MCT oil can't be metabolised by malassezia). Climbazole dissolves in MCT oil at 96.8C but it reduces its half life to 90 days so I am making 3 months supply at a time max. I then need to incorporate the climbazole/mct oil into a leave on lotion. I have adapted 2 recipes trying to eliminate any chemicals my skin has reactions to

Phase 1:
  1. Heat 10ml MCT oil to 96.8C

  2. Add 0.3g climbazole

  3. Cool to 75C

  4. Add 2.5g BioGreen Emulsifier

Phase 2:
  1. Heat 80.95ml distilled water to 70C

  2. Add 2ml vegetable glycerin 

  3. Add 0.25g citric acid

  4. Cool to 40C

Phase 3:
  1. Dump oil phase into water phase

  2. Cool to 40C

  3. Add 4ml Leucidal Liquid SF 

My question with this recipe is 1) whether a self emulsifier, such as BioGreen, will enable the climbazole to target the malassezia or will the lamellar layers prevent this? and 2) whether there will be an interaction effect between the lactobacillus ferment (Leucidal Liquid SF) and the climbazole?

Or whether I need to use a different emulsifier recipe such as:

Phase 1. 

MCT Oil – heat phase 1 to 70C


15.0%

Climbazole dissolved in MCT oil

0.3%

Ceteareth 20 (emulsifier) (HLB = 15.2 = 4.3% of 2.5% total)

0.1%

Cetyl Alcohol (thickener)

2.0%

Glyceryl Stearate SE (emulsifier) (HLB = 5.8 = 95.7% of 2.5% total)

2.4%

Phase 2. 

Distilled Water – heat phase 2 to 70C


71.45%

Vegetable Glycerin (VG, surfactant)  

2.0%

Citric Acid (reduce pH to 3.5)

0.25%

DL Panthenol

2%

Allantoin

0.5%

Phase 3. 

Leucidal Liquid SF (preservative) add below 40C


4%

 
I've added the DL Panthenol and Allantoin in here as anti irritants and I will also add in calendula extract in glycerine when it arrives! With this recipe do you think there is sufficient emulsifier (2.5%) or should I be using more (4%)?

Any advice or thoughts on these would be really helpful.

Matthew

Comments

  • It would be helpful if you would use the proper chemical names. From some research with Google I deduce that by "MCT oil" you mean capric/caprylic triglycerides, eg Myritol 318. (to help other forum members)
    Sorry but your question is way outside my areas of interest. I can't help.
    Design of anti-aging creams, gels, and serums; shampoos; and therapeutic cosmetics. In-house label and box design capability.
  • Yes, sorry, by MCT oil I mean capric/caprylic triglycerides

    BioGreen Emulsifier is Hydroxystearyl Alcohol & Hydroxystearyl Glucoside

    Leucidal Liquid SF is Lactobacillus Ferment
  • You may want to contact Tom Busby at https://rosaceagroup.org/The_Rosacea_Forum/forum.php

    He seems to specialise in this.

  • Thanks - I've spoken to Tom - I can't keep bothering him though! I just wondered if there were others who had knowledge in this area?
  • edited December 2016
    Climbazole is not a common cosmetic ingredient and its properties will be little known to most cosmetic chemists.

    I do work in the area of topical pharmaceuticals but climbazole doesn't come within my remit - this is why I suggested Tom.

    One thing that comes to mind - and this is only a notion - triethyl citrate has some interesting solvent properties and might be worth a try. Other than that, have you Gooooooogled climbazole solubility?
  • Let me put another concept out for you to think about.

    Essentially, we make emulsified lotions for only two (maybe three) reasons. First, to give our consumers an elegant/pleasant feel while applying the product. Second, to give our consumers the ability to quickly and easily apply a thin uniform layer of our oil phase (which is what does all the work), and the possible third reason is because water is much, much cheaper than any oil.

    NONE of these reasons apply to you. If you are making a treatment product for your own use, why are you making an emulsion? The water isn't helping you, and neither is the emulsifier, or the glycerin. Just apply the climbazole/CCT solution directly to your skin. There's no need to worry about preservation if you're careful with your container/closure system.
    Robert Zonis, Sr. Formulation Chemist, Beaumont Products "All opinions and comments expressed are my own, have no relation to Beaumont Products, are fully copyrighted, and may not be used without written permission."
  • Thanks johnb and Bobzchemist. 

    That is a very good point and it is one I started with. If I was starting from scratch I am sure this would work great for me. The problem I have is that I have followed dermatologists advice over the last couple of years and applied steriod creams and other things - I now have hypersentsitive skin in that area - it goes red and inflamed very easily when in contact with many ingredients. 

    So I applied the MCT oil/Climbazole mix to the areas that I need to apply it to and it is fine for an hour or so but then my skin gets irritated (not inflamed but it itches like I haven't moisturised). It then gives me hell for the next 12 hours or so until it calms down again - by that I mean it is painful/itching. My thinking was that I could make a lotion that was more soothing (like cetaphil eczema lotion helps) but without the food grade oils and with climbazole - this is what Tom Busby does. It is a hope and it may not work but it is worth a shot. What do you think? I could try some soothing oils along with the MCT oil to help? 

  • Here's the thing - the water in an emulsion doesn't do anything much. It might feel soothing while it goes on, but it's completely gone in under an hour. So, making a lotion isn't going to help you much, if at all. Don't fall into the trap of believing marketing hype.

    I think you have the right idea with adding other oils. The thing to do is to get a bunch of oils/butters to try and see which ones work best for you. Also check using pure CCT to make sure it's the oil and not the climbazole you're reacting to. 

    Allantoin is one of the few "active" ingredients that work, adding it certainly can't hurt.

    If you absolutely want to try an emulsion product, try the shealoe from lotioncrafter, and mix your CCT/climbazole into it cold, rather than try to make something yourself. http://www.lotioncrafter.com/shealoe.html ;

    Make sure you're keeping your climbazole level constant each time you evaluate an ingredient, or you won't have a basis for comparison.
    Robert Zonis, Sr. Formulation Chemist, Beaumont Products "All opinions and comments expressed are my own, have no relation to Beaumont Products, are fully copyrighted, and may not be used without written permission."
  • That is helpful, thank you.

    I have a diagnosis of seborrheic dermatitis, which is caused by malassezia - according to research this fungus metabolises fatty acids of chain length C:12-C:24. I can buy an MCT oil (C:6, C:8, C:10) easily and it won't make the condition worse. Shea Butter has C:16, C:18, and C:20 in and so theoretically would make it worse (Cetaphil has it in and soothes it for a short while but doesn't help in the long run - it becomes redder and itchier). So the only reason I am using MCT oil is because of its composition but clearly it isn't the answer for me - at least not on its own. Oils and butters which are considered to soothe irritated skin have fatty acids of child lengths greater than C:11, which is why I have excluded them. If you know of any that this isn't the case for then that would really help me.

    I did make a lotion with aloe vera but I had a bad skin reaction - I think it was the potassium sorbate? It was Tom Busby who suggested I get rid of the aloe vera and try water. 

    Things which research shows kills malassezia are: Lime Oil, Tea Tree Oil, and Sandalwood Oil. I haven't experimented with these because I have read a lot about irritating the skin with essential oils. So it leaves me at a loss of which oils to combine. I will do some more research on it. Or I could try things which soothe that dissolve in oil - but I haven't done much research on that as I have been focused on making a lotion! The only reason I thought making a lotion would help is so that I could use it in the day and not look like I have a really oily face at work! 

    johnb suggested triethyl citrate to dissolve climbazole. Would this be safe for the face? And I see it is slightly soluble in water. If I could dissolve climbazole in it then maybe it could be combined with other water soluble ingredients? Such as aloe vera (without potassium sorbate!)? Or is this barking up the wrong tree?
  • Triethyl citrate (TEC) is generally considered to be safe on the skin but, there is no guarantee that a sensitive skin like yours will be OK. Test it first.

    TEC, as well as being a good solvent, is also a recognised treatment for acne vulgaris so, possibly this action may be useful in treating seb. derm.

    Be very careful in applying essential oils to your skin. The alacrity in which some people suggest treating the skin with pretty much neat essential oil (whichever one it may be) leaves me very concerned.

  • If the climbazole works in killing the fungus, why does it matter whether or not the carrier oil feeds the fungus?

    Personally, if you're concerned about this, I think you need to stay far away from any "natural" materials. Use silicones and/or organo-silicones along with the TEC.
    Robert Zonis, Sr. Formulation Chemist, Beaumont Products "All opinions and comments expressed are my own, have no relation to Beaumont Products, are fully copyrighted, and may not be used without written permission."
  • Sorry for the long time in replying.

    Can I just ask about TEC, is it safe to put on the skin neat? or only as part of a lotion? if so what concentration do you recommend?  

    In terms of killing malassezia and feeding it at the same time, my conversations with Tom Busby have taught me that the malassezia creates a biofilm making it difficult to treat as it is protected within it. The climbazole will treat it but slowly - it can take months, even up to a year to treat properly - but feeding it can help it immediately and so the less food for it the more effective the treatment will be. I suspect the reason why so many of the products available OTC today don't work is precisely because of this, but that is my guess!



  • the malassezia creates a biofilm making it difficult to treat as it is protected within it. 
    Then why not use a system that disrupts the biofilm?
    Design of anti-aging creams, gels, and serums; shampoos; and therapeutic cosmetics. In-house label and box design capability.
  • People have been putting Xylitol in their creams to do just that. This is on some evidence that it disrupts candida biofilms but I don't think there is any research specifically on malassezia? I could be wrong but I haven't come across it. I've put some in the one I made but my problem is that I'm struggling to make a cream that soothes my skin for longer than an hour. Cetaphil restoraderm works but that the feeds the malassezia and it gets worse after a few days. I have been putting mct oil/climbazole mix on each day for a few hours before it then itches too much and I have to wash it off. That's why I was interested in the TEC, maybe it would be a better oil for me?
  • Have you seen a dermatologist about your problem?
    EDTA was mentioned as a biofilm disruptor that can remove plaque from teeth. Here's a possibly useful link.
    Design of anti-aging creams, gels, and serums; shampoos; and therapeutic cosmetics. In-house label and box design capability.
  • Thank you, I'll have a look. I've seen a few dermatologists, as have a number of people suffering with the same condition, they prescribe steroid creams, which don't help in the long run. one told me to use nizoral shampoo on my face and another daktarin, a foot cream, both of which are too harsh for my face and give me a reaction. so I'm researching making my own lotion. I came across this today https://www.google.co.uk/url?sa=t&source=web&rct=j&url=http://www.lucasmeyercosmetics.com/mailing/pdf/DermosoftDecalactLiquid-ProductInformation.pdf&ved=0ahUKEwjq88KDtYvRAhXIO1AKHVtDCnUQFggnMAQ&usg=AFQjCNFBfCUuMxU-jgmKrGJoW3i2YV_C7g&sig2=3KLG4CqHc197C6tOOYOKXw which looks promising!  it shows TEC has antifungal properties. I just don't know much about how to use tec in lotions
  • You need to let go of this idea of making a lotion as something that will be good for your hypersensitive skin. The truth is, there are no effective emulsifiers that you can access that will not be at least somewhat irritating, with the possible exception of lanolin.

    I am not at all sure that you will ever be able to get small quantities of the Decalact Liquid - and you are in any case entirely wrong about the TEC. If you read the document carefully, you will see that is being used only as a carrier/solvent to dissolve the active ingredient.

    I looked into this further, and I see that Climbazole is soluble in Benzyl Alcohol, and further, that Benzyl Alcohol is FDA approved at 5% as a lice treatment, so higher than usual doses of it should be OK. Of course, patch test everything.

    My suggestion is to make a soluble mixture of the Climbazole in Benzyl Alcohol and then mix that solution into silicone gel. This, for example:
    http://www.makingcosmetics.com/Silicone-Gel_p_1108.html

    Robert Zonis, Sr. Formulation Chemist, Beaumont Products "All opinions and comments expressed are my own, have no relation to Beaumont Products, are fully copyrighted, and may not be used without written permission."
  • No need for Decalact or Decalact liquid.

    You can buy small quantities of triethyl citrate from Amazon.com

    https://www.amazon.com/Triethyl-Citrate-Flavor-Fragrance-Compound/dp/B014PQ0BYE

    There are several sizes available.

    TEC is relatively harmless. It is used in foods as a flavour carrier and as a stabiliser for egg whites used in meringue. It is used as a nontoxic plasticiser in childrens toys.

  • Thanks John.

    And Bob, thanks too. That's a good suggestion, I'll give it a go. benzyl alcohol is only licenced upto 1% here in Europe so I'm hoping I can dissolve 0.03g climbazole in 1ml benzyl alcohol and add that to 9ml silicone gel. 

    I can see I read the Dermosoft Decalact liquid info wrong! Oops. Still looks interesting in terms of targeting malassezia. I can order 10ml of it from Germany so might get some and see how it is
  • Note that 1ml in 9ml is 10%, not 1%.
  • Yes, sorry, it would have to be in 90ml! And 0.3g climbazole in 1ml benzyl alcohol 
  • Hi,

    After the Christmas post has finally arrived I have had a go at making a silicone gel / climbazole mix. 

    I found climbazole to dissolve in benzyl alcohol very easily - I used 1:2 and heated (under 40C) and it dissolved

    I found it difficult to mix it with the silicone gel though. I heated it to 70C (as it would have been if added to the oil phase) and then mixed the benzyl alcohol/climbazole solution and then stirred it. I couldn't mix it with a blender as it was too sticky so I just used a hand mixer but I am not confident it is mixed through. Should I be blending it? Should I heat the silicone gel to higher temperatures? Any advice would be much appreciated
  • You don't need to heat the gel at all. You should be able to just stir the benzyl alcohol/climbazole solution into the gel with a spatula at room temperature.
    Robert Zonis, Sr. Formulation Chemist, Beaumont Products "All opinions and comments expressed are my own, have no relation to Beaumont Products, are fully copyrighted, and may not be used without written permission."
  • Thanks, I did do that but I wasn't sure if I had missed something - it is not easy to stir such small amounts into such a sticky substance - I was worried it wouldn't be uniform throughout. Has heating the gel and/or the benzyl alcohol/climbazole solution ruined them do you think? 
  • No, not at all. 
    Robert Zonis, Sr. Formulation Chemist, Beaumont Products "All opinions and comments expressed are my own, have no relation to Beaumont Products, are fully copyrighted, and may not be used without written permission."
  • Thank you for all your help with this. 

    The end result seems to be good for most of my face but it is not good for my eyebrow areas (which are the sensitive bits - I don't think it is an allergy to the silicone, just it doesn't soothe the irritated skin enough so it is too uncomfortable to leave on for any length of time). I see the benzyl alcohol is soluble in water 1g to 25ml water https://pubchem.ncbi.nlm.nih.gov/compound/benzyl_alcohol#section=Solubility so I wondered if it could be added to aloe vera? 
  • edited January 23
    According to the data sheet for Crinipan AD (climbazole), it is soluble in alcohol and glycols.

    Try dissolving your climbazole in a glycol (propylene glycol, propane 1,3 diol, butylene glycol, isopentyl diol etc.) and slowly diluting with water until precipitition occurs. This will give you an idea of the concentration of glycol necessary.

    You don't need anything more that this - a simple solution of climbazole in glycol/water. Provided there is sufficient glycol present (20% or so) you don't need a preservative or stabilizer.

    Climbazole is now available in the UK from http://www.naturallythinking.com/ priced at 10g for £5. Larger pack sizes are available.

    The product is of European origin and is a repack of Crinipan AD (Symrise).

  • Hi Jon, I know I have replied on the other forum but thanks for the link - that is very helpful indeed. 
  • Price rules that out for a commercial shampoo. Think I will talk to Symrise directly. They have a branch in Mexico.
    Design of anti-aging creams, gels, and serums; shampoos; and therapeutic cosmetics. In-house label and box design capability.
  • Price rules that out for a commercial shampoo. Think I will talk to Symrise directly. They have a branch in Mexico.
    That is a small user price. I'm sure the commercial rate is much lower than that.
  • Hi Donmattus, I haven't been following this discussion until just now, but a quick look on the internet mentioned a relatively recent and successful clinical trial using oral itraconazole (DOI: 10.1007/s40257-015-0133-9) which is used where patients show extensive SD resistance to topical therapies. Maybe it is mentioned somewhere in your above discussion and I have missed it, but thought it worth adding in case it helps.

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