HairlossTalk
Senior Member
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Hint on understanding this abstract. Read it VERY.... VERY slowly and think about each word. You'll do fine! I've put helper text in (parenthesis).
Objectives:
Acne and Androgenetic Alopecia (Androgenetic Alopecia, male pattern baldness, etc) are linked to Androgen effects and therefore should IMPROVE following a topical application of antiandrogens (topical spironolactone, topical finasteride?, revivogen, crinagen, etc).
Serious side effects due to a systemic absorption, however, exclude this treatment in men (there are very powerful antiandrogens but they can't be used because they may get into the bloodstream and be unsafe. the holy grail is to find a powerful one that stays somewhat local in the scalp). 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) Cutaneous uptake was also visualized by flourescence microscopy using dye loaded SLN (they dyed the liposomes so they could see if it did indeed keep things localized).
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). In contrast to native RU58841, the more lipophilic RU-myristate and nile red can be loaded into the lipid particles by hot homogenization (they found they could more easily dye the RU-myristate and track its activities during absorption than they could with traditional RU).
Results:
While receptor binding experiments proved the almost complete loss of binding to the androgen receptor, RU-myristate is rapidly metabolized to the potent antiandrogen RU58841 by the skin cells. Cellular viability was not impaired. (in a nutshell, the stuff effectively was delivered to the follicles and then transformed into a potent antiandrogen without any adverse effects. the trojan horse effect. deliver the ingredients inside the city walls and then spill out and lay everything to waste. it effectively did what propecia does from the bloodstream - it stopped the harmful binding to the androgen receptors, which should result in reversing hair loss). The new form of RU58841 known as RU58841-myristate (or "RUM") had negligible antiandrogen permeation through the skin, implying a more topical action of the drug (it didn't absorb past the skin to any noticeable extent - aka the holy grail?). Flourescent microscopy showed that the Lipid vehicle and the Nanoemulsion vehicle increased dye uptake into the skin as compared to the cream (they tried the stuff in apparently 3 different types of solutions and the lipid solution absorbed better than the cream)
Conclusions:
The new form of RU58841 known as RU58841-myristate (or "RUM") combined in a Solid Lipid Nanoparticle solution should be considered for topical antiandrogen therapy for both acne and Androgenetic Alopecia.
AKA ... a new treatment? Don't ask me where to get it, no idea
See guys they are researching things.
If anyone has a different interpretation of the above please feel free to chime in. One thing I don't know, is everything!
HairLossTalk.com
Objectives:
Acne and Androgenetic Alopecia (Androgenetic Alopecia, male pattern baldness, etc) are linked to Androgen effects and therefore should IMPROVE following a topical application of antiandrogens (topical spironolactone, topical finasteride?, revivogen, crinagen, etc).
Serious side effects due to a systemic absorption, however, exclude this treatment in men (there are very powerful antiandrogens but they can't be used because they may get into the bloodstream and be unsafe. the holy grail is to find a powerful one that stays somewhat local in the scalp). 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) Cutaneous uptake was also visualized by flourescence microscopy using dye loaded SLN (they dyed the liposomes so they could see if it did indeed keep things localized).
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). In contrast to native RU58841, the more lipophilic RU-myristate and nile red can be loaded into the lipid particles by hot homogenization (they found they could more easily dye the RU-myristate and track its activities during absorption than they could with traditional RU).
Results:
While receptor binding experiments proved the almost complete loss of binding to the androgen receptor, RU-myristate is rapidly metabolized to the potent antiandrogen RU58841 by the skin cells. Cellular viability was not impaired. (in a nutshell, the stuff effectively was delivered to the follicles and then transformed into a potent antiandrogen without any adverse effects. the trojan horse effect. deliver the ingredients inside the city walls and then spill out and lay everything to waste. it effectively did what propecia does from the bloodstream - it stopped the harmful binding to the androgen receptors, which should result in reversing hair loss). The new form of RU58841 known as RU58841-myristate (or "RUM") had negligible antiandrogen permeation through the skin, implying a more topical action of the drug (it didn't absorb past the skin to any noticeable extent - aka the holy grail?). Flourescent microscopy showed that the Lipid vehicle and the Nanoemulsion vehicle increased dye uptake into the skin as compared to the cream (they tried the stuff in apparently 3 different types of solutions and the lipid solution absorbed better than the cream)
Conclusions:
The new form of RU58841 known as RU58841-myristate (or "RUM") combined in a Solid Lipid Nanoparticle solution should be considered for topical antiandrogen therapy for both acne and Androgenetic Alopecia.
AKA ... a new treatment? Don't ask me where to get it, no idea
See guys they are researching things.
If anyone has a different interpretation of the above please feel free to chime in. One thing I don't know, is everything!
HairLossTalk.com
