- Reaction score
- 57
It’s speculation in that no data have been released for the use of the lotion or really any of the lotion’s components for the treatment of androgenetic alopecia. All we have is the good professor’s word that he did in fact try it on balding men and that it worked.
The lotion makes a fair amount of sense based on what we know.
Brief history from [Male Alopecia: Guide to successful management; Ralph M. Trüeb, Won-Soo Lee]
~400 B.C.: Hippocrates noted that Eunuchs do not go bald.
~350 B.C.: Aristotle noted that male sexual maturation was a prerequisite for male pattern baldness.
It was suspected that whatever makes a man “male” is implicated in hairloss.
1942: Dr. James B. Hamilton shoes that Androgenetic Alopecia can be triggered in men castrated prior to puberty if they were injected with testosterone.
Androgens were implicated in hairloss.
1974: Imperato-McGinley et. Al. observed intersex children in the Carribean who appeared sexually ambiguous at birth, but then grew external male genitalia and other masculine characteristics after the onset of puberty. These patients had a genetic mutation that made them deficient in 5-α reductase, which is responsible for the conversion of testosterone to dihydrotestosterone. As adults, these patients had underdeveloped prostates and also no incidence of male pattern baldness.
DHT was implicated in hairloss.
1990: Merck develops finasteride, a potent, competitive suicide inhibitor of 5-α reductase isoenzymes type II and III.
1998: 1mg finasteride tablets became the second FDA-approved prescription drug for the treatment of male pattern baldness.
· The inhibition of DHT’s actions on the hair follicle, or perhaps that of a step further downstream of this hormonal process, is a necessary step to halt hairloss.
2003: Propecia Help was formed. Many men reported transient, temporary (while on the drug) as well as permanent side effects from finasteride. Side effects included loss of libido, inability to concentrate, anxiety, suicidal thoughts/depression, poor sperm quality, erectile dysfunction, etc.
Large scale studies do not report a significant incidence of sexual side effects in finasteride users, both for hairloss as well as for BPH.
[Risk of erectile dysfunction associated with use of 5-α reductase inhibitors for benign prostatic hyperplasia or alopecia: population based studies using the Clinical Practice Research Datalink; Katrina Wilcox Hagberg,1 Hozefa A Divan,2 Rebecca Persson,1 J Curtis Nickel,3 Susan S Jick ]
It is also speculated that erection difficulty and depression could stem from the accidental inhibition of neurosteroids also synthesized via 5-α reductase, the most often cited of which is allo-pregnanolone.
[Finasteride, a 5a-Reductase Inhibitor, Blocks the Anticonvulsant Activity of Progesterone in Mice; TUSHAR G. KOKATE, MELISSA K. BANKS, TAMIKA MAGEE, SHUN-ICHI YAMAGUCHI and MICHAEL A. ROGAWSKI]
~2007: There is growing interest in being able to deliver finasteride topically in order to avoid possible systemic side effects due to prolonged androgen/5-αR deprivation.
[Development of Liposomal Systems of Finasteride for Topical Applications: Design, Characterization, and In Vitro EvaluationDevelopment of Liposomal Systems of Finasteride for Topical Applications; Rajiv Kumar, Bhupinder Singh, Gautam Bakshi, and Om Prakash Katare]
[A novel finasteride 0.25% topical solution for androgenetic alopecia: pharmacokinetics and effects on plasma androgen levels in healthy male volunteers; Maurizio Caserini1, Milko Radicioni2, Chiara Leuratti2, Ottavia Annoni2, and Renata Palmieri]
[Effects of a novel finasteride 0.25% topical solution on scalp and serum dihydrotestosterone in healthy men with androgenetic alopecia; Maurizio Caserini1, Milko Radicioni2, Chiara Leuratti2, Emanuela Terragni2, Matilde Iorizzo3, and Renata Palmieri]
[Topical Formulations Containing Finasteride. Part I:In VitroPermeation/Penetration Study and In Vivo Pharmacokinetics in Hairless Rats; DANIELA MONTI,1SILVIA TAMPUCCI,1SUSI BURGALASSI,1PATRIZIA CHETONI,1CARLA LENZI,2ANDREA PIRONE,2FEDERICO MAILLAND]
[Topical Formulations Containing Finasteride. Part II: Determination of Finasteride Penetration into Hair Follicles using the Differential Stripping Technique; SILVIA TAMPUCCI,1SUSI BURGALASSI,1PATRIZIA CHETONI,1CARLA LENZI,2ANDREA PIRONE,2FEDERICO MAILLAND,3MAURIZIO CASERINI,3DANIELA MONTI]
To date, nobody has demonstrated a liposomal topical finasteride solution that maintains efficacy while allowing serum DHT to remain high. Some low-dose liposomal formulations resulted in an amount of finasteride in serum below the detection limit, but nevertheless, serum DHT inhibition was still ~70%. Finasteride is known to have a very steep dose-response and a tendency to accumulate in tissues.
· Nominally, DHT should be reduced locally in order to avoid interfering with the function of other organs, such as the prostate.
1988: Originally developed for hypertension, 2% Minoxidil is FDA approved for treating hairloss. Minoxidil is now thought to function as a potassium-channel opener. This is believe to result in opening of the blood vessels, improving circulation to the follicles and prolonging the duration of anagen.
· Improvement of microcirculation to the hair follicle can result in a significant increase in hair size and growth.
So we know that any good next-generation preventative regimen must address all three of the bullet points. Brotzu’s lotion appears to have a fantastic shot at doing all three.
· s-equol is known to selectively bind to 5-αDHT
but NOT to testosterone, dehydroepiandrosterone or estrogen with high affinity. S-equol also does not bind to the androgen receptor or 5-α reductase. Dr. Brotzu claims that adding s-equol to his formula improved its effectiveness by 80% (Don’t take that as a real number, it’s probably just a casual estimate).
[Equol: Pharmacokinetics and Biological Actions; 1,2KennethD.R.Setchell3*andCarloClerici4]
[Equol Is a Novel Anti-Androgen that Inhibits Prostate Growth and Hormone Feedback1; Trent D. Lund,2,3 Daniel J. Munson,3 Megan E. Haldy,3 Kenneth D.R. Setchell,4 Edwin D. Lephart,5 and Robert J. Handa3]
[Use of equol for treating androgen mediated diseases; Edwin Lephart Trent Lund Kenneth David Setchell Robert Handa US20060122262A1]
· Prostaglandin E1 is a very potent vasodilator.
but it has not been thoroughly investigated for the improvement of alopecia. Dr. Brotzu claims that a topical he made containing it grew hair as a side effect. Additionally, he claims that the precursor to PGE1, dihomo-γ-linoleic acid, works just as well.
[Prostaglandin-Induced Hair Growth; Murray A. Johnstone, MD,1and Daniel M. Albert, MD, MS]
[Prostaglandin E2: igniting the fire; Carlo Chizzolini and Nicolo`C Brembilla]
Sucks that the formulation is a bit of a leap of faith on several fronts. On the other hand, it is the culmination of several things that others are investigating also for the effects we desire in treatment and the idea behind the formulation is still consistent with what would be required for halting hairloss. Even if the lotion goes systemic despite the liposomes, it might be alright. Finasteride destroys the enzyme that catalyzes the conversion of testosterone to DHT. So once the catalyst is gone, no action can occur. This might be why the dose response is so unweildy. S-equol binds directly to DHT so at least one could expect the dose response to be more linear with regard to DHT inhibition. Additionally, s-equol is present in people already due to the presence of certain gut bacteria. Point is, if equol from the topical leeches into the body, it might be just fine. That alone is exciting to me. Brotzu claims DGLA/PGE1 is a better vasodialator than minoxidil in the oral presentations he gives, but I don't know much about that.
Thanks for the info man. Seems pretty legit. Won't get my hopes up too high but a little bit of it goes a long way
