pharmaceutical grade dmso: use to rub on injectables?  

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pSimonkey
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23/03/2019 11:23 am  

Boom ! Great information thanks ersatz. Please where would i find the best recipe for a transdermal with reasons for it's effectiveness? Where would I find a consice list of chemical mw's ?What is a good site/s, besides this one, to follow up research on this topic, ie transdermal products ? How do i know if a chemical/compound has a high absorbability rate? I'm a bit of a research junky and I have the bit between my teeth on this one. I have some ideas and need to get to the bottom of them. Thanks very much againagain. :- )


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ersatz
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23/03/2019 12:06 pm  

I use chemfinder to find the molecular weight of substances. As far as absorption rate, it depends on a several factors, mw structure, lipophilicity (oil solubility) of the molecule, etc. In general, the more lipophilic the molecule, the more easily it will pass through the stratum corneum. However, extremely lipophilic molecules do not pass through well. Phs and steroids have very good lipophilic properties for percutaneous absorption.

The first and most important aspect of percutaneous delivery systems is to understand the structure of the skin which will give you better insight on the differences between topical/site specific and traditional transdermal systematic delivery systems. The stratum corneum is the outermost layer of the skin. It consists of flat, hard, shield-like cells that are constantly sloughing off and being replaced by cells moving up from lower layers. The stratum corneum impedes the evaporation of water from the skin layers below it and it also serves as the principle barrier to absorption through the skin by external penetrants. Thus substances with a mw >500 won't pass through the SC very well. The use of penetration enhancers encourage drugs to pass through this layer. Once the barrier of the stratum corneum is crossed, the substance diffuses through the lower layers of the epidermis and eventually into the dermis (the main layer of the skin). The dermis is composed of water-rich living cells (as opposed to the epidermis which consists of dead cells) with a rich blood and lymph supply. So it is here in the dermis that substances are carried away by the rich amount of fluids present into the blood and lymphatic systems. Most transdermal products are abosorbed in this layer providing for systematic delivery. To make a site specific application the delivery system needs to pass through this layer and into the tissue itself. I don't think any current formulations can overcome this rate limiting step thus I don't believe there is any viable topical/site specific products. IM injection is really the only viable method to get the drug into a specific area, and even then we see that it gets absorbed systematically and there isn't vast growth in the site of injection as opposed to the other tissues. So if you're looking for site specific growth I don't think you'll achieve it unless you resort to synthol injections.

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ersatz
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23/03/2019 1:02 pm  

As for recipies here's the most common one and most products are a variation of it:
40% ISOPROPYL ALCOHOL( ISO )
15% ISOPROPYL MYRISTRATE( IPM )
15% ISOPROPYL PALMITATE( IPP )
10% OLEIC ACID( OA )
10% PROPYLENE GLYCOL( PG )
10% DMSO

*note* most commercial products available substitute DMSO with d-limonene for issues of legality. Some also include disteilled water to reduce the alcohol content which has a tendancy to dry the skin out. An example of one such formulation would be:
IPA 25%
IPM 9%
IPP 2%
OA 8%
DMSO 10%
PG 10%
D-Lim 6%
dH2O 30%

A carbomer may be added to make it into a gel consistency but then you have to adjust the ph of the solution hence the inclusion of Triethanolamine.

Here's a breakdown of the chemicals common used and their properties.

DMSO (Dimethylsulfoxide) is a popular and effective penetration enhancer. First off it is a good solvent for organic compounds and because of this it was used as the carrier for many products.This meant that a product would contain 50-80% DMSO which often resulted in skin irritation. DMSO's action mechanism isn't exactly known but it is believed to affect lipid layers and also the structure of cells. It is amphiphillic which allows it to penetrate deep into the skin so it can build up in subcutaenous tissues. DMSO is also known for its foul smell, which is supposedly the result of an impurity bismethylthiomethane. USP grade DMSO should be free of this impurity and thus not have the foul smell. Bad breath will probably still be associated with DMSO regardless of grade and is the result of the sulhpur breakdown.

DMFA (Dimethylformamide) is an alternative to to DMSO because it is supposedly a slightly more powerful PE and doesn't have the malodorus properties of the latter. Skin irritation is also supposedly reduced in comparison. Unfortuantely short term/acute exposure to dmfa can cause abdominal pain, nausea, vomiting, jaunidice, rashes and even liver damage. Chronic exposure has also resulted in liver and digestive disturbances and even alledgedly testicular cancer(1,5). DMFA and its metabolite monomethylformamide cause testicular damage(2,3) and chromosomal aberrations(4) in labratory animals. The Occupational Safety and Health Administration(OSHA) has set the permissable exposure limit(PEL) for dimethyl formamide at 10ppm, 30mg/m3(skin). Popular transdermal products containing this PE resulted in a exposure level half that of OSHA's PEL. The potential hazardous nature of DMFA outweighs its slight benefits over DMSO, and probably accounts for its limited availability on the market.

Diethylene glycol monoethyl ether is a PE used in some newer pharmaceutical products. It is claimed to be a potent PE but I could not find any info just how effective it is. It is a safe compound, is not a skin irritant and is not malodorus.

IPM (isopropyl myristate) has several properties that make it ideal in a cutaneous delivery formula. As a PE it is thought to remove lipids from the stratum corneum thus creating miniscule holes through which substances can be shuttled. IPM is also an emolient sealing the skin and retaining moisture. This prevents the skin from drying out by the alcohol portion of cutaneous delivery product, thus increasing skin permeability.

IPP(ISOPROPYL PALMITATE) acts in the same manner as IPM but leaves the skin feeling more oily.

Oleic Acid has been found to increase the epidermal permeability through a mechanism involving the stratum corneum lipid membrane. It is incorporated into skin lipid, disrupts molecular packing and alters the level of hydration and allows drug penetrates faster.

Isopropyl alcohol is used as a solvent. It will help disolve the ph into the solution. It also has some penetration properties but tends to dry out the skin.

PROPYLENE GLYCOL- keeps the moisture from leaving the skin but is very oily. It also dissolves the ph into solution.

d-Limonene is used because it gives a nice citrus fragrance to cover up the smell from DMSO. It also acts as a mild penetration enhancer and as an emulsifier.

A search on google for transdermal products should turn up all the info you need. The inclusion of the term prohormone or bodybuilding should make the results more specific to your needs.


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pSimonkey
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23/03/2019 1:35 pm  

I'm off to see the wizard, the wonderful wizard of transdermal application recipes.
I am now thinking of a "hot" tub of solution. ;- )
Thanks muchmuch for all that great information clearly delivered. I am very grateful.


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jboldman
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23/03/2019 2:22 pm  

ersatz, are you saying that with DMSO there is only a 30% absorbtion rate?

jb


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JGUNS
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23/03/2019 2:57 pm  

There really is no competition between USP DMSO and other transdermal carriers. USP DMSO is the only carrier that is backed by US and Canadien drug Master files and meet the rigorous USP standards specically for the purposes of transdermal pharmaceutical delivery. It is known as a super solvent, because many drugs that are not soluable in other solutions are soluable to a high degree in USP DMSO. The soluability also enhances the action of the drug. The high soluability also means that it doesn't take much, and it also works well with water. Not only that but it has a better safety profile than alcohol or other carriers, with the lowest incidence of cell toxicity in studies. DMSO penetrates the skin very rapidly, and at a measurable rate, the difference is that it penetrates reversably, which allows for a lower incidence of toxicity.

The idea that it only carries 30% it patently false. First off, much of the idea of permeability has to do with the compound and the solubility, but other factors like temperature and amount. DMSO is prescribed by doctors for transdermal preps. It penetrates as readily, if not moreso than anything else on the market. It is a better choice because of its safety, solubility,water miscible, high polarity, aproticity, and other physical properties.

 

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ersatz
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23/03/2019 3:47 pm  

Sorry for the confusion, I meant that the bioavailability(fraction/percent that reaches systematic circulation) of a transdermal is realistically 30%. I see claims of 40% and as high as 76% for some type of fina trans but have seen nothing to support those claims. USP grade DMSO would be an ideal penetration enhancer(PE) for the reasons jguns mentioned, the foremost being it's relative safety. I think BigCat had an article on why DMSO should not be used as a carrier but rather a PE in part because it penetrates the skin very rapidly. I personally use it in a pre and post application of the trans soln as well as in the trans itself. I believe DMSO is a necessity when using a transdermal product regardless of how you choose to use it.


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jboldman
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23/03/2019 4:25 pm  

well said by both guns and ersatz. I have used DMSO for years.

jb


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heavyweight
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23/03/2019 5:11 pm  

I have just started to use dsmo with transdermal Testosterone from the doctors. Seems to work rather well. I lace the dsmo with roughly 60% water and apply, then I wait a few minutes and apply the transdermal test. I love dsmo.


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pSimonkey
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23/03/2019 5:50 pm  

High heavyweight, could you please give the listed ingredients of the transdermal?


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heavyweight
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23/03/2019 6:48 pm  

Test 50mg
carbomer 940
ethyl alcohol 68.9%
isopropol myristate
sodium hydroxide
water


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pSimonkey
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23/03/2019 7:20 pm  

Thanks heavyweight. Anyone know the purpose of sodium hydroxide?


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heavyweight
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23/03/2019 7:56 pm  

probably just something to make it different..


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JGUNS
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23/03/2019 8:47 pm  
Posted by: pSimonkey
Thanks heavyweight. Anyone know the purpose of sodium hydroxide?

What was your concentration of DMSO? Also, do you use glycerin for skin drying out?

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heavyweight
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23/03/2019 9:22 pm  

I use a small container and fill it about 1/8 way, then I add 2x the amount of water.
I myslef don't use anything to keep from drying out. I am naturally dry.........
Ever get those smal containers mike sends out with his powders, like yohimbe and such? I use one of those small ocntainers.


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