Penetration Enhancers

[Old Baldy]

Here's a list of penetration enhancers, etc., written by Dow Chemical. Just a tidbit for you homemade concoction wackos.

http://www.dowpharm.com/publications/Da ... ne1997.pdf

 

[CCS]

oldbaldy, did your oils dissolve fully in your minoxidil? bryan was asking me why i was using these oils. I think he disapproves, but then he also disapproves of me using topical 5ar inhibitors.

 

[Old Baldy]

oldbaldy, did your oils dissolve fully in your minoxidil? bryan was asking me why i was using these oils. I think he disapproves, but then he also disapproves of me using topical 5ar inhibitors.

Maybe I misspoke before. I make my own creams, lotions and liquid solutions with active male pattern baldness medications. I make those with oils, water and alcohols (glycols, etc.).

You ALWAYS have to add emulsifiers to the concoction so the oils, water and alcohol combine into a homogenous mixture.

If I were to add oils to minoxidil., I guess I'd have to add about an equal amount of an emulsifier (e.g., polysorbate 80 is a common emulsifier). I'm guessing here because I don't add oils to minoxidil.

The minoxidil. vehicle is good by itself to dissolve medications put into it. I've never had the minoxidil. precipitate out of the mix.

I understand Bryan's concerns relative to topical finasteride. From what I've read, it's almost certain that some gets into the bloodstream. At the same time, some gets into the follicle directly. The rub is - does it get metabolized when it reaches the follicle from the topical administration? I think it does, I assume Bryan thinks it does not?

I also assume (from what I've read) that the amount that makes its way into the bloodstream is minimal. I assume Bryan thinks enough might get into the bloodstream to make it equal to just taking it orally?

Most likely, Bryan feels there just isn't enough proof to make the assumptions I have made.

 

[Old Baldy]

College: Maybe you've seen this PubMed abstract but it discusses various formulations used for delivering finasteride. to the follicles.

Best was niosomes/liposomes, second was hydroalcoholic and third was gels. (Hydroalcoholic solutions absorbed quickly.) Here is the abstract:

Int J Pharm. 2006 May 26; [Epub ahead of print] Related Articles, Links


Enhancement of follicular delivery of finasteride by liposomes and niosomes 1. In vitro permeation and in vivo deposition studies using hamster flank and ear models.

Tabbakhian M, Tavakoli N, Jaafari MR, Daneshamouz S.

Department of Pharmaceutics, School of Pharmacy & Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.

Finasteride is indicated orally in the treatment of androgenetic alopecia and some other pilosebaceous unit (PSU) disorders. We wished to investigate whether topical application of finasteride-containing vesicles (liposomes and niosomes) could enhance drug concentration at the PSU, as compared to finasteride hydroalcoholic solution (HA). Liposomes consisted of phospholipid (dimyristoyl phosphatidylcholine (DMPC) or egg lecithin):cholesterol:dicetylphosphate (8:2:1, mole ratio). Niosomes were comprising non-ionic surfactant (polyoxyethylene alkyl ethers (Brij((R)) series) or sorbitan monopalmitate):cholesterol:dicetylphosphate (7:3:1, mole ratio). Vesicles were prepared by the film hydration technique and characterized with regard to the size, drug entrapment efficiency and gel-liquid transition temperature (T(c)). In vitro permeation of (3)H-finasteride through hamster flank skin was faster from hydroalcoholic solution (0.13mug/cm(2)h) compared to vesicles (0.025-0.058mug/cm(2)h). In vivo deposition of (3)H-finasteride vesicles in hamster ear showed that liquid-state vesicle, i.e. those made of DMPC or Brij97:Brij76 (1:1), were able to deposit 2.1 or 2.3% of the applied dose to the PSU, respectively. This was significantly higher than drug deposition by gel-state vesicles (0.35-0.51%) or HA (0.76%). Both in vitro permeation and in vivo deposition studies, demonstrated the potentials of liquid-state liposomes and niosomes for successful delivery of finasteride to the PSU.

PMID: 16837150 [PubMed - as supplied by publisher

I've read another patent (can't find it now) that tested octyl salicylate mixed 50-50 with 190 proof alcohol.

The patent application indicated the finasteride. dissolved well and penetrated very well. It dried to a cosmetically acceptable level. (It was tested with good result on animal skin - can't remember which animal! )

IIRC, it was a very recent patent application, (i.e., in 2006)?

You can get octyl salicylate from LeMange.com and 190 proof from The Chemistry Store.com (it's called Perfumer's Blend).

I ordered some octyl salicylate the other day. Haven't received it yet. It's used in sunscreens because it is a UV protector. It's cheap btw.

 

[Felk]

Perfumer's blend is recommended to use with the RU antiandrogen by the chemical makers, I believe.

OldBaldy, despite those "assumptions" you believe you're making, do you still believe topical finasteride to be effective? Are there some studies on it's effectiveness?

I ask because i had previously completely discounted it as an option, mainly due to Bryan's attitude towards it (only effective through systematic absorption anyway) I'd know if it was being absorbed systematically however, as i got a particular weird side effect from it (burping, chest tightness, heart pain, discomfort)

If you have a recipe you're using, i'd like to hear about it

 

[Old Baldy]

Perfumer's blend is recommended to use with the RU antiandrogen by the chemical makers, I believe.

OldBaldy, despite those "assumptions" you believe you're making, do you still believe topical finasteride to be effective? Are there some studies on it's effectiveness?

I ask because i had previously completely discounted it as an option, mainly due to Bryan's attitude towards it (only effective through systematic absorption anyway) I'd know if it was being absorbed systematically however, as i got a particular weird side effect from it (burping, chest tightness, heart pain, discomfort)

If you have a recipe you're using, i'd like to hear about it

Bryan's explained it very well. Studies are "all over the place". Some say it works without systemic effects, some say it is useless, some say it works by systemic effects only.

Just read College's posts on recipes, he has a good handle on what to do. I agree with his recipes from all I've read.

The 50-50 octyl salicylate/190 proof alcohol is probably a very good one. Both are safe products. It dissolves and delivers finasteride. adequately according to the patent. (Btw, it makes sense that that vehicle would work from all I've read.)

Same for just crushing a few tablets and mixing with minoxidil. The minoxidil. vehicle is a very good solution for mixing stuff.

Creams use anywhere from 0.025 percent to 0.050 percent from what various studies have used. (Edit: I think some studies used 0.25 percent also. So you can see, topical finasteride. studies are "all over the place" not just in conclusions but in RECIPIES also! :-x )

I say just use College's advice. It's good advice IMHO.

 

[Felk]

Cheers, sounds good, i'll try that one you mentioned.

Even though I dislike having to apply too many topicals, without finasteride it's so much harder to fight DHT so I have to use a lot of stuff.

I wonder if it'd be possible to make a topical finasteride/spironolactone combination? Or perhaps a finasteride/spironolactone/bayberry one?

 

[Aplunk1]

I was hoping this thread was going to be about something different.

 

[hairhaircomeagain]

I was hoping this thread was going to be about something different.

HEHE

 

[Old Baldy]

I was hoping this thread was going to be about something different.

Well it isn't if you don't gravitate towards creativity. Some of us like to "tinker". (And I like the results so far.)

I'm very satisfied with how things are going. It's kind of fun to tinker. I guess you don't have the mindset to get excited by tinkering. I do.

Is that good or bad? No. :wink:

You see, guys like Felk and I like the fact that someone filed a patent using a 50-50 mix of 190 proof alcohol and octyl salicylate combined with finasteride. and/or dutasteride. Since the author concluded it had good penetrating qualities and was cosmetically acceptable that gets some of us interested.

It gives us something else to tinker with. If it doesn't work - well at least we tried. And it's fun to boot. I mean, the ingredients are good IMHO.

The vehicle is so very important Aplunk. Never discount that. A good vehicle is as important as the medication. Maybe even MORE. Think about it.

IMHO, the topical use of dutasteride. and/or finasteride. will minimize the side effects and likely "deliver the goods" at the same time. I can't prove this but it is a gut level feeling I've developed from alot of reading. I could be wrong however.

But I'm never going to know unless I try. That's what tinkerers do!!

 

[Cassin]

http://www.bellonoche.com/a***%20Lube.gif

 

[Old Baldy]

Cassin: You ain't right! :lol: :lol: :shock:

Here's another patent showing octyl salicylate can help with penetratoin of anti-androgens and 5AR inhibitors.

http://216.109.125.130/search/cache?p=o ... 1&.intl=us

 

[CCS]

Oldbaldy,
You've done some excellent work! that pubmed paper and the patent you found are exactly the kind of information I wanted but could not find. i wonder if you even realize how good a find that was, judging from that fact that you say you are making assumptions.

The abstract did not say the vesicles were better than a hydroalcohol. it said they have about a 2.2% absorption rate, which his much greater than that of the gel. It also said that the finasteride in the hydroalcohol was absorbed about 3 times as fast as the finasteride in the vesicles. Did you read the whole paper and find that actually said the vescicles are better than the finasteride? This is a good find because we know the finasteride is absorbed at least 2.2% in the minoxidil vehicle, and likely as much as 6%.

Felk,

Ask Bryan questions when you want facts. He knows as many facts as 200 encyclopedias. But I don't recognise him as an engineer. As such, as long as at least one study got some finasteride absorption, you should not let Bryan discourage you from designing new vehicles.

Felk and OldBaldy,

Topical finasteride is good for avoiding side effects, which is my selling point to get more people to use my ideas. But the reason I want topical dutasteride or finasteride for myself is not to avoid side effects, but because I think I can get a mega dose to my follicles, without upping my serum levels. My goal is to knock out 99.9% of follicle DHT, and inhibit serum DHT maybe 50 or at most 60%. That abstract you found takes a lot of the guess work out of my percentages. I really think this can be done.

 

[Felk]

Sounds good big guy, could you tell me (or direct me to) the recipe of topical finasteride, which you believe will be most effective?

 

[Old Baldy]

College: I think the abstract said (if I'm reading it correctly) the hydroalcohol solution absorbed at 0.76 percent. Isn't that a lower absorption rate?

Another thing you have to realize is I'm a layman. I have to read, re-read, re-read..... in order for the technical medical terms and chemical names to make "sense".

I have to cut and paste unknown terms and do a search on them ALOT so I can understand what the author is saying. It takes me hours to understand things when, someone like you, probably understands it the first time you read it. Oh well, I never had medical classes in school. (And the few chemistry classes I had are completely out of my old memory.)

Glad the abstract and patent helped. I wish I had kept the link to the 50-50 mix of octyl salicylate and 190 proof alcohol patent. :-x

Btw College, I've read alot of Bryan's old posts at various sites. He is one of the biggest tinkerers that I've come across. He's mixed up all sorts of concoctions in his home.

He's just wary of using topical finasteride. and dutasteride. because they can penetrate into the bloodstream. He doesn't want that to happen IMHO.

I'm looking forward to more of your suggested recipes College!!!

 

[powersam]

'd be interested in the makeup of the cream which they used in that successful topical finasteride study. the one which decreased arm hair on the women where the cream was applied but nowhere else. that was a very interesting study but i cant find it now.

 

[Old Baldy]

I think this is what you are after Power Sam:

The instructions from that study were as follows:


"Fifteen tablets of finasteride (5 mg each) were triturated
(ground into a fine powder) and then wetted with 2 mL of
propylene glycol. The mixture was incorporated into Dermabase
(Paddock Laboratories, Inc.) by levigation (that is, mixed evenly
by high-speed mixer and gradually incorporated). The final
cream contained 0.25% finasteride."


And here's the abstract:


Endocr Pract 2001 Jan-Feb;7(1):5-10
Finasteride cream in hirsutism.
Lucas KJ.


OBJECTIVE: To determine, in a preliminary study, whether women
with hirsutism attributable to various causes would benefit from
treatment with finasteride cream. METHODS: Finasteride cream
(0.25%) and placebo cream were administered to eight women
with various degrees of facial hirsutism. The two creams were
used on opposite sides of the face in an area of excessive hair
growth. The side chosen for the finasteride cream versus placebo
was randomized and blinded. In a 1 cm2 area on each side of
the face, hair counts were done every 2 months throughout the
6-month study period. Hair thickness was also measured.
RESULTS: Hair follicles respond to testosterone by the conversion
of this androgen to dihydrotestosterone through the action of
5a-reductase. Finasteride partially blocks this enzyme. Because
of the easy solubility of this medication through the skin, a cream
applied to the area of hair growth would be expected to decrease
hirsutism locally. After a 6-month period, mean hair counts
decreased significantly from 27.5 to 15.5 (P<0.05) in the
finasteride-treated sites but showed no significant change
from baseline in the placebo-applied sites. Moreover, the mean
thickness of the measured hairs (in hundredths of millimeters)
was significantly different between the placebo and finasteride-
treated sites (4.33 versus 3.11, respectively; P<0.001).
CONCLUSION: In this study of women with facial hirsutism,
topically applied finasteride significantly decreased hair growth
and thickness, and no adverse effects were noted.


Mike

You could use Dermovan, Cetaphil, Neutrogena Neutral Cream, etc. Nothng very special about Dermabase IMHO.

If my math is correct, 0.25 percent with 15, 5 mg pills would make a 30ml mixture. About one ounce. For the classic 60ml mixture, you would need 30 pills if you wanted to duplicate that study. (Check my math though.)

Also, that seems to be a VERY strong percentage of finasteride. IMHO. (At 60, 1ml applications, that would be 2.5mg of finasteride. for each dosage! That's ALOT of finasteride.!!)

If you put 3, 5mg pills into a 60ml solution that would equate to 0.25mg per 1ml application. If you put 6, 5mg pills into a 60ml solution that would equate to 0.5mg per 1ml application. You have to decide what's best. Like Bryan says, the studies are "all over the place"! :hairy:

Most of the veterans' posts I've read have suggested 0.025 percent to 0.050 percent for an effective "dose". They arrived at that percentage much the same way College does (i.e., area of application and milligram percentages applied to that small area in relation to our entire body, and/or the mg's per 1ml dose).

 

[CCS]

yeah, it was wrong for me to comment on bryan like that. What he may or may not do was irrelavent to the discussion at hand. I've only read is more recent posts, and a few older ones i subbled accross while doing some searches. that is great that he tinkers. so far all I've heard him talk about was what is in a study or that he uses dr proctors products.

 

[CCS]

HA - hydro alcohol. I missed that. I thought they omitted the hydroalcohol absorption rate, gave the other two, and said the alcohol was absorbed much faster than with the vesicles. The absorption speed was the invitro data, and the absorption percentage was the in vivo data. Interesting how they seem to vary so much.

0.76% still is not that bad. I can't do a mega dose with that, without upping costs, but people who get side effects from finasteride should be able to get enough to get therapudic effects and not systemic effects.

at least bryan posted some more studies. thats a good thing. If 25% of the amount that penetrates makes it into the follicles (which are near the pores where most of the stuff enters), and the volume of the scalp is 1/400th the volume of the body, and oral finasteride is absorbed 60%, then applying 1mg/day to the scalp would give the scalp the effect of a 5mg oral dose. I believe the cells will eventually let go of the finasteride into the blood stream, and at steady state the body will still get 0.0076*1mg per day, which is less than 0.01mg/day, which lowers systemic DHT only 5%. I doubt anyone will get side effects on that. This would benifit me to because right now I'm only taking 1.25 mg per day. So I could get a higher dose. But I suspect that serum DHT does affect follicle DHT levels by maybe 5 or 10%, so I don't know if I'd see the 1mg/5mg 20% difference when my body DHT levels climb. Also, Bryan says that systemic DHT reduction almost prevents prostate cancer. The main reason I'd go topical is to use dutasteride, since it causes90% systemic reduction which I don't want, but we don't have data on that and I suspect it is absorbed less than finasteride.

 

[Old Baldy]

College wrote:

0.76% still is not that bad. I can't do a mega dose with that, without upping costs, but people who get side effects from finasteride should be able to get enough to get therapudic effects and not systemic effects.

I wonder how much finasteride. gets to the PU when taken orally?