I want to make a couple of very minor corrections to what HairLossTalk.com said, and then I'll make a general comment or two about "RUM":
HairlossTalk said:
Drug targeting to the sebum gland and derma papillae, however, may allow topical antiandrogen treatment in men (if they can keep it localized to the follicle's structures, it may be safer). Accomplishing this may be possible by particulate carrier systems such as solid lipid nanoparticles, SLN, which are known to support dermal targeting (they've found something that can take the active ingredient and target only the local follicle structures. they're called liposomes)
It may or may not be actual "liposomes" that these researchers are talking about. There seems to be more than just one kind of these particulate carriers in existence, depending on various factors like their size and exact chemical structure. For example, I see the term "nanosome" being bandied about on some hairloss sites for what are apparently even TINIER particles than liposomes. I don't really know if the term these guys are using (solid lipid nanoparticles, or SLN) are liposomes, nanosomes, or something else entirely. Maybe someone else who is more interested in that general technology can clarify that for us. Where is Jacob when we need him?? :wink:
HairlossTalk said:
Methods:
The New Antiandrogen prodrug called RU58841-myristate was developed for topical therapy. (I believe this is a new version of RU58841 intended for topical application for hair loss sufferers). Ester cleavage was proved, receptor affinity and local tolerability were compared to RU58841. (they made sure it did all the same things as orally ingested RU).
Nobody would ever orally ingest RU. RU is _exclusively_ intended for topical use, whether it's the original version or the altered "RUM" form.
What they mean in that last sentence above is that they proved that when the altered "RUM" form of RU58841 (which has no antiandrogenic properties itself) penetrates into cells, enzymes in the cells break it back down into the standard RU58841 form, which then goes on to have the expected potent antiandrogenic effect. They're essentially saying, don't worry, it turns back into RU58841 once it enters the cell!
The additional comments I have are the following:
1) There's nothing new about the idea of using topical RU58841 in liposomes (or whatever the exact kind of carrier particle it is that they're using). In fact, that's what one of the published RU studies used a few years ago! The anonymous guy who posted his before-and-after RU pics over on HLH a while back also used liposomal RU. I'm sure he got the idea from that earlier study.
2) The truly novel and original idea these guys had was altering the standard RU molecule by linking it to a molecule of myristic acid (a fatty acid). What they're claiming is that it improves the ability of the RU molecule (along with the attached fatty acid) to penetrate through the skin by making the whole molecule a little more "fatty". They're saying that even though the combination molecule is not ITSELF an antiandrogen, enzymes within the cell eventually separate the two parts of the molecule again, and the lone RU then goes about its normal and well-known job of efficiently blocking androgen receptors.
Bryan
