Comment · Fri, February 15, 2019
R-ALA cyclodextrin dosing
Original post in this thread
Hywardhayward · 1 points
Hi,
According to Ikuta et al. in "Bioavailability of an R-α-Lipoic Acid/γ-Cyclodextrin Complex in Healthy Volunteers" (https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4926482/#!po=22.0588)
6g of R-ALA Cy is equivalent to only 600mg of Na-R-ALA. The reccomended dosing of R-ALA Cy according to ND is 500mg. If you see table 2 and chart 2 you can see to get the increased bioavailability benefits of R-ALA Cy still requires a larger dose of powder, I think it means more of the total powder weight is the cyclodextrin complex vs. smaller weight of sodium content of Na-R-ALA. So while the actual R-lipoic acid is better uptaken when in cyclodextrin complex, the fraction of each mg of R-a-lipoic acid in Na-R-ALA is way higher, i think only 5% is sodium, while the cyclodextrin appears to take up 90% of each mg of powder.
If you took 500mg of R-ALA Cy, you would only need 125mg of Na-R-ALA to match the bioavailability, even taking into account the 2.5x increased bioavailability of cyclodextrin form because there is just so little actual lipoic acid and so much cyclodextrin taking up space in the powder.
This means the R-ALA Cy needs to be dosed at a prohibitively expensive amount, using 10…
What they were answering
Direct reply to the original post — see the thread post above.
u/MisterYouAreSoDumb
The R-ALA cyclodextrin complex is an expensive option. We are the only ones selling it in the United States partly because of the cost. However, I like to bring novel things to market sometimes, even if the pricing is not ideal in comparison to other options. It can be similar to taking 1,000mg curcumin with piperine instead of Longvida. One is massively cheaper than the other, but there are still arguments for the use of the more expensive one. Plasma levels are not everything. One of the reasons Longvida is better is because it can reach the brain better. Well, cyclodextrin complexes are not just able to increase systemic bioavailability, but they are also more permeable to the blood brain barrier. This is why cyclodextrin complexes are used in a lot of cancer drugs. The γ-cyclodexrin disrupts the membrane of the BBB, allowing for the delivery of the drug to the brain in much high amounts than a simple salt would.
Other advantages to a cyclodextrin, apart from increased bioavailability, is that it is much more heat-stable. It is also stable for longer periods than even Na-R-ALA. On top of that, the cyclodextrin masks the horrible taste of ALA. I think ALA is one of the worst tasting things out there, and having a powder that can mask that is nice if you are putting it into smoothies or drinks. In addition, Na-R-ALA forms polymers when put into solution. γ-cyclodextrin R-ALA is completely stable in solution. So is it an inexpensive option? No, certainly not. However, it does have advantages that some might value enough for the price. Since you can't get it anywhere else in the US, I figured it would be nice to have a source. If we can reduce the price in the future, we certainly will. It just costs us a lot to make at the moment.