How to hombrew PLO gel

[acecombact1]

Ok guys im a newbie wanabe pharmacy student , I did tons of research before the holiday on PLO gel, and I spend sometimes on library reading about transdermal gel compounding . Here is instructions to make 8 Oz of PLO gel.



Ingredients:

-Lecithin with high phosphatidylecholing concentration ( you can buy it from here: http://www.bulknutrition.com/?products_id=617 this Lecithin contains 25% phosphatidyl choline) . the higher concentration of PS in the lecithin the better it is.

-Isopropyl palimate (from www.lemelange.com)

-Surfactant (from lemelange Surfactant Oil Blend - A proprietary blend of surfactants, including PS20)

-Isopropyl alcohol ( I got mine from health store for 0.99 cents per 8 Oz 91% pure)

-D-Limonene (optional)

How to prepare:
(oil phase)
-Weigh 50g of lecithin powder.
-In a beaker measure 120ML of Isopropyl palimate.
-Add the lecithin to the Isopropyl palimate in the beaker and mix. You can either leave the mix covered for one day and the lecithin will dissolve on its own. Or you can heat the mix with hot water path, but note phosphatidylecholing is very sensitive to heat, and it may be denatured.

Liquid phase :

Original formula of plo gel uses of Pluronic F127, which is a surfactant and detergent. Pluronic F127 Is hard to find, because it’s a patent surfactant. Now the main pupose of Pluronic F127 , is to mix the oil phase ( which is very thick and take long time to dry) with the polar solvents. it also helps to adjust the consistency and make it easier to apply and dose, it also good penetration enhancer. Now I replaced Pluronic F127, with surfactant blend from lemelange contains Polysorbate 20 (PS20), which is used in cosmetic products and acts very similar to Pluronic F127 ( mixes oils with with polar solvents).
Liquid phase acts mainly as solvent for the PH or AAS you going to choose.

this is called Lecithin Micro-emulation carrier (oil phase), tons of research done on this formula as a safe drug delivery system.

Preperation:

Measure and add 70ml of isopropyl alcohol/ 30ml of water to the oil phase, and mix .

Leave the mix to settle couple of minutes. You will notice 2 layers separated (oil and polar solvent) added 20 ml of surfactant blend and mix the solution. Now you can add 2ml of D-Limonene with each 10ml of surfactant. D-Limonene adds good citrus smell, helps mix the 2 layers, and its good penetration enhancer.

Leave the solution settle again, and when you notice separation of layers add more surfactant and D-Limonene . Keep repeating the step until the solution become unified solution, and no layers appear any more.

Finally add the PH, AAS, drug your gonna use to the solution, and mix very good until it dissolves. Amount of powder you can get in the gel depends on the solubility properties of drug you want to use. Most Phs and steroids dissolve at 200mg/ml-100mg/ml range.

PS: 10% addition of DMSO to solution, will give higher absorption rate than typical gels in market that contains DMSO , or PLO gel alone. I think addition of oleic acid will be great also, but will make solution very greasy.

here you go fox ver cheap formula you can make 2 L of solution for 30$. No smell,and no irretation.

 

[doggzj]

Anyone know how well does this formula work for transporting into the body?

EDIT: Better question would be how could this be measured out?

 

[wojo]

wow great post..gonna def try this..whats the consistency? can i use a squirt bottle? or a syringe to dispense?

 

[acecombact1]

Anyone know how well does this formula work for transporting into the body?

EDIT: Better question would be how could this be measured out?

bioavilablity is about 20% according to this study below, which is similar to DMSO alone, but with androgen bases i imagine absorption rate would be much highier due to small molecule size. i think adding dmso to formule will enhance absorption rate to 30%-35% range.

1: Am J Health Syst Pharm. 2004 Dec 1;61(23):2541-4. Related Articles, Links


Relative bioavailability of ketoprofen 20% in a poloxamer-lecithin organogel.

Dowling TC, Arjomand M, Lin ET, Allen LV Jr, McPherson ML.

Pharmacokinetics and Biopharmaceutics Laboratory, Department of Pharmacy and Therapeutics, School of Pharmacy, University of Maryland, Baltimore 21201, USA.

PURPOSE: The bioavailability of a single, topically applied, 200-mg dose of ketoprofen (delivered in a ketoprofen 20% gel) relative to a single 50-mg oral dose in healthy volunteers was studied. METHODS: This was an open-label crossover study. The subjects were randomized to receive an oral 50-mg ketoprofen capsule or a single topical dose of ketoprofen 20% in a poloxamer-lecithin organogel (PLO). Treatment was followed by a one-week washout period. Blood samples were collected at intervals up to 10 hours after administration, and plasma ketoprofen concentrations were determined by high-performance liquid chromatography with ultraviolet or mass spectrometry detection. Noncompartmental pharmacokinetic values were obtained after each dose, and relative bioavailability was calculated. RESULTS: Eight healthy volunteers enrolled in and completed the study. Topical absorption of ketoprofen was highly variable among the subjects over the 10-hour sampling period. The median oral maximum plasma concentration (Cmax) exceeded the topical Cmax by nearly 200-fold (4.15 versus 0.021 microg/mL) (p = 0.001). The median relative bioavailability of topical ketoprofen was 0.48%, with individual subjects' values ranging from 0.18% to 2.1%. CONCLUSION: The relative bioavailability of ketoprofen was low and highly variable when the drug was administered as a single dose in a PLO-based ketoprofen 20% gel

 

[acecombact1]

wow great post..gonna def try this..whats the consistency? can i use a squirt bottle? or a syringe to dispense?

yes you can use a squirt bottle, in fact im doing that right now, consisiency is similar to T-gel, a little bit thicker.

 

[Alpha Dog]

acecombact1, thanks for all the work! I agree, Its definately worth a try.

 

[Simon Keller]

Very interesting, nice work Ace...

 

[Strateg0s]

Octyl salicylate should be added as well. Check out Par Deus' article on the science of transdermals. After reading that, it seems to me that this ingredient is not optional.

 

[judge-mental]

Indeed great post, Im gonna wait for feedback from fellow homebrewers, I got enough homebrew for the next months anyway...

 

[acecombact1]

Octyl salicylate should be added as well. Check out Par Deus' article on the science of transdermals. After reading that, it seems to me that this ingredient is not optional.

i looked into Octyl salicylate, there is only one study that shows it has some effect as penetration enhancer.

only reason many people use it is that its a good solvent, you can get more powder when you add it. otherwise it dosnt have much of a benefit.

 

[wojo]

anyone try this?

 

[Alpha Dog]

Just mixed up a batch for my next transdermal cycle. For the most part, I followed the recommendations above. I did change the ratio of the surfactant blend to d-limonene to about 1:1. I did this to improve the odor, especially considering I also added about 9% DMSO. I wasn’t sure if 1:1 ratio would effect the mixing of the oil and liquid phases, but it seems to have worked. Picture taken below was about 45 minutes after mixing the two phases. Still no stratification, which leads me to believe it will work at that ratio. The only other PE I added was octyl salicylate at about 4%. Solvent mix was as follows:

60 ml Isopropyl palimate (43%)
14 ml iso alchohol (10%)
6 ml distilled water (4%)
12 ml dmso (9%)
6 ml octyl salicylate (4%)
12 ml d-limonene (9%)
10 ml surfactant blend (7%)
25 grams lecithin (14% by volume)

Total Volume 140 ml

If the actual percentages seem odd, it’s because the lecithin occupies about 20 ml’s of volume. I wasn’t sure initially how much volume the lecithin would occupy, so I wasn’t able to initially calculate (only estimate) the volume of each solvent.

I’ll be running this in about a week with 1-test and 4-ad and will report the results. I just applied 5 ml’s of the solvent alone to test for irritability.

Thanks to acecombact1 for doing all the legwork.

 

[acecombact1]

my skin feels realy tight after using this.......um

 

[pepo72]

Nice work acecombat

 

[bodyfort]

Nice work. Im about to buy everything though I can find surfactant?Where to get it or can I substitute with PS20?

thank you in advance

 

[BEEFY]

Anyone know how say 1-test cypionate would work in a transdermal regarding half life?
Would it still have a long half life or would it have to be applied daily still?

 

[fatsuperman]

Although testosterone with esters will work transdermally (at debate effectiveness), research apparently shows that the hormone will basically enter the blood steam desterfied.

Meaning no mater what test powder you use you should still apply it every 12 hours, because the half life of the ester won't make a difference.