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  1. #1
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    Default More evidence for topical finasteride(July-August)

    Int J Clin Pharmacol Ther. 2014 Jul 30. [Epub ahead of print]
    A novel finasteride 0.25% topical solution for androgenetic alopecia: pharmacokinetics and effects on plasma androgen levels in healthy male volunteers.
    Caserini M, Radicioni M, Leuratti C, Annoni O, Palmieri R.
    Abstract
    Objective: Finasteride, a selective inhibitor of type 2 5-alpha reductase isoenzyme, inhibits the conversion of testosterone to dihydrotestosterone (DHT) and is indicated in the treatment of male androgenetic alopecia. The study objective was to evaluate a newly developed finasteride 0.25% topical solution in comparison to the marketed finasteride 1 mg tablet, with respect to finasteride pharmacokinetics and suppressive effects on plasma DHT. Methods: 24 healthy men with androgenetic alopecia were randomized in a single center, open-label, parallel-group, exploratory study, and received either multiple scalp applications of the topical solution b.i.d. or oral doses of the reference tablet o.d. for 7 days. Plasma finasteride, testosterone and DHT concentrations were determined. Results: After multiple doses, mean (± SD) finasteride Cmax and AUC00-t corresponded to 0.46 ± 0.28 ng/mL and 6.64 ± 7.50 ng/mL x h for the topical solution and to 6.86 ± 1.78 ng/mL and 57.93 ± 29.38 ng/mL x h for the tablet. Plasma DHT was reduced by ~ 68 - 75% with the topical solution and by ~ 62 - 72% with the tablet. No relevant changes occurred for plasma testosterone with either treatment. No clinically significant adverse events occurred. Conclusions: A strong and similar inhibition of plasma DHT was found after 1 week of treatment with the topical and tablet finasteride ormulations, albeit finasteride plasma exposure was significantly lower with the topical than with the oral product (p < 0.0001).


    Arch Pharm Res. 2014 Aug 2. [Epub ahead of print]
    Enhanced skin permeation of 5α-reductase inhibitors entrapped into surface-modified liquid crystalline nanoparticles.
    Madheswaran T1, Baskaran R, Sundaramoorthy P, Yoo BK.
    Author information
    1College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsan, 712-749, South Korea.
    Abstract
    The objective of this study is to enhance skin permeation of finasteride and dutasteride for the treatment of androgenetic alopecia using surface-modified liquid crystalline nanoparticle (sm-LCN) dispersion. LCN entrapped with the drugs was prepared by using monoolein as a liquid crystal former, and surface modification was performed by treatment of the LCN dispersion with same volume of 1 % v/v acetic acid solution containing chitosan. Physicochemical properties of the LCN's were studied with regard to particle size, polydispersity index, zeta potential, and release of the drugs. Skin permeation of drugs entrapped into the LCN and sm-LCN was investigated with porcine abdominal skin using Franz diffusion cell. Cytotoxicity of the LCN's was also studied using human skin keratinocytes. The particle size and zeta potential of the LCN were 197.9 ± 2.5 nm and -20.2 ± 1.9 mV, respectively, and sm-LCN showed slightly bigger size and positive zeta potential due to the presence of thin coating on the surface of the nanoparticles. Compared to LCN, sm-LCN resulted in significantly enhanced skin permeation of the drugs whereas in vitro release was significantly reduced. Cell viability as a measure of cytotoxicity was above 80 % up to 20 μg/ml concentration of both LCN and sm-LCN. In conclusion, sm-LCN may provide a strategy to maximize therapeutic efficacy minimizing unwanted systemic side effects associated with the use of the drugs for the treatment of androgenetic alopecia.


    J Pharm Sci. 2014 Aug;103(8):2323-9. doi: 10.1002/jps.24045. Epub 2014 Jun 10.
    Topical Formulations Containing Finasteride. Part II: Determination of Finasteride Penetration into Hair Follicles using the Differential Stripping Technique.
    Tampucci S1, Burgalassi S, Chetoni P, Lenzi C, Pirone A, Mailland F, Caserini M, Monti D.
    Author information
    Abstract
    The differential stripping technique consists of a tape-stripping phase followed by a cyanoacrylate biopsy. This technique not only allows the quantification of drug retained in the stratum corneum (SC) and in the hair follicles but also differentiates transepidermal from transfollicular penetration. Our study aimed at both validating the differential stripping procedure on hairless rat skin and assessing the role of the hair follicle in the cutaneous penetration of finasteride (FNS) after application of two experimental formulations for 6 or 24 h: P-08-016, a hydroxypropyl chitosan (HPCH)-based formulation and P-10-008, an anhydrous formulation devoid of HPCH. Microscopic and histological evaluation showed that after 15 tape strips both the SC and the viable epidermis were completely removed. A subsequent cyanoacrylate skin surface biopsy led to the removal of the infundibula content. The largest amounts of FNS were found in the epidermis and in the appendages after application of P-08-016, regardless of the time from application. In contrast, smaller and statistically significant amounts of FNS were recovered with P-10-008 6 h after application, compared with that at 24 h. In conclusion, the differential stripping technique allowed determination of the amount of FNS localized in different skin districts, focusing particularly on the follicular contribution. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:2323-2329, 2014.

    J Pharm Sci. 2014 Aug;103(8):2307-14. doi: 10.1002/jps.24028. Epub 2014 Jun 18.
    Topical formulations containing finasteride. Part I: in vitro permeation/penetration study and in vivo pharmacokinetics in hairless rat.
    Monti D1, Tampucci S, Burgalassi S, Chetoni P, Lenzi C, Pirone A, Mailland F.
    Author information
    Abstract
    In hair follicle (Hf) cells, the type-2 5-α-reductase enzyme, implicated in androgenetic alopecia, is selectively inhibited by finasteride (FNS). Because an effective topical formulation to deliver FNS to Hf is currently unavailable, this investigation aimed at evaluating in vitro FNS skin permeation and retention through and into hairless rat and human abdominal skin. Four hydroxypropyl chitosan (HPCH)-based formulations (P-08-012, P-08-016, P-08-063, and P-08-064) and one anhydrous formulation without HPCH (P-10-008) were tested. The pharmacokinetics in plasma and skin after application of P-08-016 or P-10-008 on dorsal rat skin with single and repeated doses was investigated. P-08-016 performed the best in driving FNS to the reticular dermis without producing a high transdermal flux. Neither the in vivo single nor the repeated dose experiments produced plasma levels of FNS and no differences were found between formulations concerning skin retention. No increase in the amount of drug retained in the skin was obtained with the repeated dose experiment. In conclusion, the HPCH-based formulation P-08-016 might represent an alternative to systemic therapy for its ability to promote a cutaneous depot of FNS in the region of hair bulbs, minimizing systemic absorption even after repeated treatments. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:2307-2314, 2014.

  2. #2
    Senior Member Desmond84's Avatar
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    Good study but heres an important excerpt:

    "A strong and similar inhibition of plasma DHT was found after 1 week of treatment with the topical and tablet finasteride ormulations, albeit finasteride plasma exposure was significantly lower with the topical than with the oral product"

    And that is exactly the problem with finasteride. The sides associated with fin is due to reduction of DHT not how much fin makes it to the bloodstream. And unfortunately both reduce the dht plasma levels by the same amount meaning you can expect the same side effect profile from the topical version.

    Our only solution is CB unfortunately. Till then we're stuck with fin sadly

  3. #3
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    [QUOTE=Desmond84;181029]Good study but heres an important excerpt:

    "A strong and similar inhibition of plasma DHT was found after 1 week of treatment with the topical and tablet finasteride ormulations, albeit finasteride plasma exposure was significantly lower with the topical than with the oral product"

    And that is exactly the problem with finasteride. The sides associated with fin is due to reduction of DHT not how much fin makes it to the bloodstream. And unfortunately both reduce the dht plasma levels by the same amount meaning you can expect the same side effect profile from the topical version.

    Our only solution is CB unfortunately. Till then we're stuck with

    Yeah that was a little disappointing find from that study. However, they weren't clear in that abstract about the method of delivery and a few others point to lipid nanoparticles as the optimal choice of delivery since they would stay deposited in the hair follicle. I was initially under tge impression that finasteride works to the extent that it is absorbed into the blood stream but apparently these researchers think the opposite.

  4. #4
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    Quote Originally Posted by Desmond84 View Post
    Good study but heres an important excerpt:

    "A strong and similar inhibition of plasma DHT was found after 1 week of treatment with the topical and tablet finasteride ormulations, albeit finasteride plasma exposure was significantly lower with the topical than with the oral product"

    And that is exactly the problem with finasteride. The sides associated with fin is due to reduction of DHT not how much fin makes it to the bloodstream. And unfortunately both reduce the dht plasma levels by the same amount meaning you can expect the same side effect profile from the topical version.

    Our only solution is CB unfortunately. Till then we're stuck with fin sadly
    What they really need to study is the difference in DHT levels in the scalp between topical and oral fin. If the topical inhibits more scalp DHT for the same plasma concentration, then we might be able to use a weaker topical, which would mean lower plasma concentration for the same effect on the hair follicles. That could only be a good thing.

  5. #5
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    Quote Originally Posted by Pate View Post
    What they really need to study is the difference in DHT levels in the scalp between topical and oral fin.
    What they REALLY need to do is come up with something better (anything) than Finasteride. We're closing in on 2015 here folks. I think it's time we up our standards a little.

  6. #6
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    Quote Originally Posted by Pate View Post
    What they really need to study is the difference in DHT levels in the scalp between topical and oral fin. If the topical inhibits more scalp DHT for the same plasma concentration, then we might be able to use a weaker topical, which would mean lower plasma concentration for the same effect on the hair follicles. That could only be a good thing.
    I'm curious about this. It might be that side effects have less to do with plasma DHT and more to do with the amount of DHT suppressed in places like the gonads and brain. Maybe when it is ingested orally it is able to affect these places more broadly than topically, where it possibly seeps into the blood more slowly, and ends up in a similar plasma DHT reduction but maybe not an equally widespread DHT reduction. Side effects depend on 5ar inhibition and localized lack of DHT, so maybe there's more to the story than plasma concentration. There's gotta be a reason why hasson and wongs patients dont get sides with the topical and they do with the pill. when my ish starts getting bad enough and if CB isnt out yet i'm def trying it.

  7. #7
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    Well, oral fin goes systemic first and from there goes to the hair follicles. Topical fin goes through the scalp skin to get into the bloodstream. So you would definitely expect that for the same systemic concentration of fin, the topical would have a much higher concentration in the scalp.

    And while I fully agree that it's time we had something better than fin anyway, unfortunately with the exception of CB there is nothing even really on horizon in terms of drug treatments. I'll take improved fin over regular fin... and both of them over nothing at all.

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