I would like to try to formulate a cream with vitamin B12 as topical active (eczema).
Vitamin B12 is an effective scavenger of nitric oxide. NO has been found to be implicated in the pathogenesis of (atopic) eczema and psoriasis.
I've found a research showing that the experimental application of a NO synthase inhibitor (N omega-nitro-L-arginine), led to a clear decrease in pruritus and erythema in atopic dermatitis, so one would expect a comparable effect from vitamin B12.
Point is which form?
Some researches (the excerpts) don't mention the form of B12 used.
Some use cyanocobalamine. I also found a simple W/O emulsion formula with it:
· 0.07 g vitamin B12 (cyanocobalamin)
· 0.25 g citric acid
The form I can get hold of is hydroxocobalamine. Cyanocobalamine as well as OH-cobalamine are two biologically inactive forms of B12 and need to be converted via a methylation cycle to be fully functional systemically.
Apparently the conversion doesn't seem to be necessary to inhibit nitric oxide though, as OH-cobalamine binds and scavenges NO (
source).
My questions:
Since information on topical B12 emulsions (especially with OH-cobalamine) is very scarce, I really hope people here can help me:
·
Does anyone know how stable OH-cobalamine is in an emulsion?
·
What pH range is necessary for it to remain stable?
·
Is a buffer recommended?
·
Important interactions (e.g. preservatives)?
·
Recommended concentration?
·
W/O rather than O/W?I know what I'm planning to formulate would be OTC rather than cosmetic, since I hope it will relieve eczemic laesions. I'm not planning to sell, I will be making it for a family member.
Hopefully it can be succesfully used next to indifferent creams and topical corticosteroids.
Edit: adjusted lay-out
Comments
Thanks for your reply.
I didn't know that brand, thanks for mentioning.
Hopefully I can get some answers to my questions.
Hopefully not the last.
I didn't find any pH range information in this study which is the full paper of the study you are probably reading about. https://www.dropbox.com/s/waf7hg5c4br2rid/vitaminb12-study.pdf?dl=0
But you should clarify some of your questions.
1. ·Does anyone know how stable OH-cobalamine is in an emulsion?
2. ·What pH range is necessary for it to remain stable?
I didn't see your replies yesterday, didn't get a notification.
I will read both of your replies thoroughly and respond later, thanks very, very much!!
https://jpharmsci.org/article/S0022-3549(15)34243-X/pdf
Incompatibilities may include ascorbic acid. http://europepmc.org/articles/pmc4179674
Regarding the colour you will get from cyanocobalamin, it actually depends on the oxidation state of the cobalt atom. Pink is the natural state Co(III) & Yellow-ish is Co(II). Where Co(III) is the natural state in B12.
Thank you all so much for your answers!
(@Sibech you're right, I typed this answer + scheme when I only got answers from Perry and Pharma)
I'll first try to make it without a buffer at a pH of about 6.
(Thanks Sibech and chemicalmatt for your help!!)
Regarding red colorants: I've tried Gromwell root (CO2) extract a while ago. I needed only the tiniest speck to turn almost half a kilogram of emulsion from white into pink. (It should turn into a blue hue when the product is alkaline instead of neutral or acidic.)
Edit: adjusted lay-out
I also want to thank Pharma and amitvedekar for info about buffers and pH (I see I only mentioned Sibech and chemicalmatt). I've been too hasty, it's terribly late (or actually very early) here and I'm in dire need of sleep.
And thank ALL of you who have replied, I really value your input very, very much!
I'll keep you informed about how things went!
Maybe it's the form that matters (hydroxo or cyano), regarding incompatability with lidocaine? I read the warning not to use hydroxocobalamine together with i.a. lidocaine in the same IV line (and thus couldn't be mixed in the same syringe either) due to 'chemical incompatability' in the Cyanokit booklet (page 23)
The i.m. injection isn't painful at all though?
The Cyanokit is exactly the same.
So? I have never seen two incompatible substances being put together in one syringe, nor for immediate i.m. use or otherwise.
@Belassi
You mentioned availability of the B12.
For me it's the cheapest way to use the solution for injection in hydroxocobalamine form (in the research they used cyanocobalamine, but the powder is quite expensive here). If you can't find the pure powders, maybe you can get hold of the injection solution too? Just a tip.