Reads this article, sounds very interesting, anybody got any thoughts on it, is this form of administration common place?
Just trying to learn a little....
Cyclodextrins are a form of linked carbohydrates. They're formed by an enzymatic synthesis that begins with starch. The enzymes, called transglycosidases, are derived from bacteria. What these enzymes do is couple the starch molecules together to form a truncated, conical, molecular structure with a hollow cavity inside.
The inside of this cyclodextrin "cone" is just about the perfect shape and volume to accommodate a steroid molecule. It's also a non-polar molecule, which means that it has some of the same properties as a fat or oil. The steroid molecule doesn't just sit inside the cone, it actually attaches to the inside of it. Also, it won't dissolve in water. However, while the inside of the cyclodextrin cone is non-polar, the outside is polar, which means that it will dissolve in water. What's the significance of all of this? When a steroid molecule and a cyclodextrin molecule hook up, they form a 1:1 complex. So, while the steroids themselves won't dissolve in water, a cyclodextrin/steroid complex will. The upshot is that steroid complexes become more absorbable through the oral mucosa.
A lot of clinical research has been published on the use of sublingual cyclodextrin complexes (SCCs) in humans. At the forefront of much of this research has been Josef Pitha of the US Department of Health and Human Services. Pitha has several patents on sublingual cyclodextrin complexes. He's also authored a journal article where he details the results of an SCC of testosterone on men. In a nutshell, Pitha found that an SCC containing 10mg of testosterone per tablet raised testosterone levels astronomically high (900% over baseline at one hour) and at two hours the levels were still elevated 485%. Compare that with another study that used regular testosterone at 20 times the dosage used in Pitha's study. Regular testosterone - not complexed with cyclodextrin - only raised testosterone around 500% at the peak.
Another study performed by Stuenkel et.al. showed that testosterone SCCs of 2.5 and 5.0mg raised testosterone levels in hypogonadal men 2341% and 4270% (absolute increases of 1765 ng/dL and 2406 ng/dL) respectively! It took an average of 20 to 30 minutes to achieve maximum blood testosterone levels, but even after eight hours post-dose, the testosterone levels were still elevated 126% for the 2.5mg dose and 195% for the 5.0mg dose. Interestingly enough, the peak levels for estradiol only increased 300% and 340% over baseline, respectively. Remarkable, considering that one usually sees estradiol levels increase proportionally with testosterone levels when other forms of administration are used (i.e. injectable esters and TU orals).