hi many thanks thats a great shame i have read and been interested in his posts for many years over the hairloss forums.
Topical Finasteride
- Thread starter Jrthomas85
- Start date
hi many thanks thats a great shame i have read and been interested in his posts for many years over the hairloss forums.
Yea, sad, sad day when Bryan passed away doke. 
Topical dutasteride - I don't know of ANY studies show it working. But no reason to think it would not if topical finasteride does work. However, its moleculer size is a bit bigger than finasteride, so that could make penetration to the folicle a bit less. Although I think it is still under 500 daltons, so should have decent penetration.
Topical dutasteride - I don't know of ANY studies show it working. But no reason to think it would not if topical finasteride does work. However, its moleculer size is a bit bigger than finasteride, so that could make penetration to the folicle a bit less. Although I think it is still under 500 daltons, so should have decent penetration.
supermusic
Established Member
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- 34
I noticed minoxidilmax released a new finasteride + minoxidil topical Dualgen. Does anybody try it?
Dear all,
this thread seems a bit inconclusive to me. Obviously the participants don't entirely agree, yet maybe we could have some sort of an overview about the present state of topical DHT blockers (maybe even including 5-Alpha-reductase-inhibitors), something like: There's a) ………, b) ………, and c)……… as main substances that with some backup claim effect when used topically. A is backed up by this and this study, contradicted by this one. It is available in this and that product. B is … ?
I know it's a lot to ask, but I do feel a bit lost in all the quarrel, and I really am far from any expertise. And maybe there's hope that all disagreements at least will be collected and overviewed in such a list?
Certainly such a list would be of great interest to many, all those who seem to worry about the systemic side effects of non-topical application.
Thanks
this thread seems a bit inconclusive to me. Obviously the participants don't entirely agree, yet maybe we could have some sort of an overview about the present state of topical DHT blockers (maybe even including 5-Alpha-reductase-inhibitors), something like: There's a) ………, b) ………, and c)……… as main substances that with some backup claim effect when used topically. A is backed up by this and this study, contradicted by this one. It is available in this and that product. B is … ?
I know it's a lot to ask, but I do feel a bit lost in all the quarrel, and I really am far from any expertise. And maybe there's hope that all disagreements at least will be collected and overviewed in such a list?
Certainly such a list would be of great interest to many, all those who seem to worry about the systemic side effects of non-topical application.
Thanks
cthulhu2.0
Established Member
- Reaction score
- 20
[h=1]Whole lotta research on this recently:
Topical Formulations Containing Finasteride. Part I: In Vitro Permeation/Penetration Study and In Vivo Pharmacokinetics in Hairless Rat.[/h]Monti D1, Tampucci S, Burgalassi S, Chetoni P, Lenzi C, Pirone A, Mailland F.
[h=3]Author information[/h]
[h=3]Abstract[/h]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.
J Pharm Sci. 2014 Jun 10. doi: 10.1002/jps.24045. [Epub ahead of print]
[h=1]Topical Formulations Containing Finasteride. Part II: Determination of Finasteride Penetration into Hair Follicles using the Differential Stripping Technique.[/h]Tampucci S1, Burgalassi S, Chetoni P, Lenzi C, Pirone A, Mailland F, Caserini M, Monti D.
[h=3]Author information[/h]
[h=3]Abstract[/h]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.
Pak J Pharm Sci. 2014 May;27(3):525-9.
[h=1]A validated RP-HPLC method to investigate finasteride in human skin after in vitro topically applying vesicular nanocarrier.[/h]Zheng F1, Rao Y2, Lou Y2, Lu X2.
[h=3]Author information[/h]
[h=3]Abstract[/h]
Int J Nanomedicine. 2014 Mar 7;9:1231-42. doi: 10.2147/IJN.S45561. eCollection 2014.
[h=1]Lipid nanoparticles for topical and transdermal application for alopecia treatment: development, physicochemical characterization, and in vitro release and penetration studies.[/h]Gomes MJ1, Martins S2, Ferreira D3, Segundo MA1, Reis S1.
[h=3]Author information[/h]
[h=3]Abstract[/h]Alopecia is a dermatological disorder, commonly known as hair loss, which affects up to half of the Caucasian male population by middle age, and almost all (95%) Caucasian men by old age. Considering that alopecia affects so many people and that there is currently no scientifically proven treatment with few side effects, new drug-delivery systems able to improve alopecia therapy are urgently required. With this purpose in mind, the present study aimed to develop lipid nanoparticles (nanostructured lipid carriers) with the ability to incorporate and deliver anti-alopecia active compounds (minoxidil and finasteride) into the dermis and hair follicles. Lipid nanoparticles, prepared by ultrasonication method, showed mean particle sizes around 200 nm, which is sufficient for reaching the dermis and hair follicles, and zeta potential values around -30 mV, which indicates good physical stability. Over 28 days of storage, no significant variations in these parameters were observed, which indicates that all nanoformulations are stable in storage over that period. Cryo-scanning electron microscope measurements showed that all the lipid nanoparticles exhibited a spherical shape and a smooth surface regardless of their composition. Differential scanning calorimetry studies allowed the determination of phase transition temperatures and confirmed the recrystallization of the lipid nanoparticles (recrystallization index between 11% and 86%). A high loading efficiency was achieved for finasteride (between 70% and 90%), while less than 30% was achieved for minoxidil nanoparticles, over 28 days. Controlled release assays in physiological conditions demonstrated that nanoparticles loaded with minoxidil yielded a prolonged release, as desired. Penetration assays through pig ear skin demonstrated that nanoparticles loaded with minoxidil andfinasteride had low levels of penetration. These results suggest that the proposed novel formulation presents several good characteristics indicating their suitability for dermal delivery of anti-alopecia active compounds.
The pharmacotherapeutic efficiency of topical drug delivery systems is mainly dominated by the skin distribution of therapeutic agents. In this work, a sensitive, rapid and fully-validated reversed-phase high performance liquid chromatography (RP-HPLC) method was developed to determine finasteride in human cadaver skin after different vesicular formulations were applied. Drug in different depth of skin layers were measured with an EclipseXDB-C18 column. The mobile phase consisted of 75% (v/v) methanol containing 0.2% phosphoric acid buffered to pH 3.0 with triethylamine under isocratic conditions. The system was operated at 40°C and the mobile phase flow rate was set at 1 mL/min. The standard-calibration curve was linear within range of 5 to 200 ng/ml with correlation coefficient 0.9996. The intra-assay precision was less than 3.9% while the inter-assay precision was less than 7.1% with the bias range of -8.6 to 4.1%. This method was found to be specific, accurate, and sensitive and was successfully used to determine the accumulation of finasteride after in-vitro percutaneous delivery by liposomal or ethosomal drug delivery nanocarriers.
Eur J Pharm Sci. 2014 Feb 14;52:165-72. doi: 10.1016/j.ejps.2013.11.008. Epub 2013 Nov 19.
[h=1]Chitosan-decorated polystyrene-b-poly(acrylic acid) polymersomes as novel carriers for topicaldelivery of finasteride.[/h]Caon T1, Porto LC2, Granada A1, Tagliari MP1, Silva MA1, Simões CM1, Borsali R3, Soldi V4.
[h=3]Author information[/h]
[h=3]Abstract[/h]In view of the fact that the oral administration of finasteride (finasteride) has resulted in various undesirable systemic side effects, the topicalapplication of polystyrene and poly(acrylic acid)-based polymersomes (underexplored system) was investigated. Undecorated PS139-b-PAA17 and PS404-b-PAA63 vesicles (C3 and C7, respectively) or vesicles decorated with chitosan samples of different molecular weight (C3/CS-oligo, C7/CS-oligo, C3/CS-37 and C7/CS-37) were prepared by the co-solvent self-assembly method and characterized by small-angle X-ray scattering,transmission electron microscopy and dynamic light scattering techniques. In vitro release experiments and ex vivo permeation using Franz diffusion cells were carried out (through comparison with hydroethanolicfinasteride solution). The ideal system should provide high finasteride retention in the dermis and epidermis while allowing some control of the drug release. The particle size and in vitro release were negatively correlated with the permeation coefficient and skin retention in both the epidermis and dermis. The findings that the longest lag time was obtained for the hydroethanolic drug solution and lowest permeation for the systems able to release the drug faster support the hypothesis that nanostructured systems may be required to enhance the penetration and permeation of the drug. Chitosan-decorated polymersomes interacted more strongly with the skin components than non-decorated samples, probably due to the positive surface charge, which increased the finasteride retention and reduced the lag time. C7 polymersomes decorated with chitosan were more appropriate for topical applications (high retention in the dermis and epidermis and controlled drug delivery).
Topical Formulations Containing Finasteride. Part I: In Vitro Permeation/Penetration Study and In Vivo Pharmacokinetics in Hairless Rat.[/h]Monti D1, Tampucci S, Burgalassi S, Chetoni P, Lenzi C, Pirone A, Mailland F.
[h=3]Author information[/h]
[h=3]Abstract[/h]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.
J Pharm Sci. 2014 Jun 10. doi: 10.1002/jps.24045. [Epub ahead of print]
[h=1]Topical Formulations Containing Finasteride. Part II: Determination of Finasteride Penetration into Hair Follicles using the Differential Stripping Technique.[/h]Tampucci S1, Burgalassi S, Chetoni P, Lenzi C, Pirone A, Mailland F, Caserini M, Monti D.
[h=3]Author information[/h]
[h=3]Abstract[/h]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.
Pak J Pharm Sci. 2014 May;27(3):525-9.
[h=1]A validated RP-HPLC method to investigate finasteride in human skin after in vitro topically applying vesicular nanocarrier.[/h]Zheng F1, Rao Y2, Lou Y2, Lu X2.
[h=3]Author information[/h]
[h=3]Abstract[/h]
Int J Nanomedicine. 2014 Mar 7;9:1231-42. doi: 10.2147/IJN.S45561. eCollection 2014.
[h=1]Lipid nanoparticles for topical and transdermal application for alopecia treatment: development, physicochemical characterization, and in vitro release and penetration studies.[/h]Gomes MJ1, Martins S2, Ferreira D3, Segundo MA1, Reis S1.
[h=3]Author information[/h]
[h=3]Abstract[/h]Alopecia is a dermatological disorder, commonly known as hair loss, which affects up to half of the Caucasian male population by middle age, and almost all (95%) Caucasian men by old age. Considering that alopecia affects so many people and that there is currently no scientifically proven treatment with few side effects, new drug-delivery systems able to improve alopecia therapy are urgently required. With this purpose in mind, the present study aimed to develop lipid nanoparticles (nanostructured lipid carriers) with the ability to incorporate and deliver anti-alopecia active compounds (minoxidil and finasteride) into the dermis and hair follicles. Lipid nanoparticles, prepared by ultrasonication method, showed mean particle sizes around 200 nm, which is sufficient for reaching the dermis and hair follicles, and zeta potential values around -30 mV, which indicates good physical stability. Over 28 days of storage, no significant variations in these parameters were observed, which indicates that all nanoformulations are stable in storage over that period. Cryo-scanning electron microscope measurements showed that all the lipid nanoparticles exhibited a spherical shape and a smooth surface regardless of their composition. Differential scanning calorimetry studies allowed the determination of phase transition temperatures and confirmed the recrystallization of the lipid nanoparticles (recrystallization index between 11% and 86%). A high loading efficiency was achieved for finasteride (between 70% and 90%), while less than 30% was achieved for minoxidil nanoparticles, over 28 days. Controlled release assays in physiological conditions demonstrated that nanoparticles loaded with minoxidil yielded a prolonged release, as desired. Penetration assays through pig ear skin demonstrated that nanoparticles loaded with minoxidil andfinasteride had low levels of penetration. These results suggest that the proposed novel formulation presents several good characteristics indicating their suitability for dermal delivery of anti-alopecia active compounds.
The pharmacotherapeutic efficiency of topical drug delivery systems is mainly dominated by the skin distribution of therapeutic agents. In this work, a sensitive, rapid and fully-validated reversed-phase high performance liquid chromatography (RP-HPLC) method was developed to determine finasteride in human cadaver skin after different vesicular formulations were applied. Drug in different depth of skin layers were measured with an EclipseXDB-C18 column. The mobile phase consisted of 75% (v/v) methanol containing 0.2% phosphoric acid buffered to pH 3.0 with triethylamine under isocratic conditions. The system was operated at 40°C and the mobile phase flow rate was set at 1 mL/min. The standard-calibration curve was linear within range of 5 to 200 ng/ml with correlation coefficient 0.9996. The intra-assay precision was less than 3.9% while the inter-assay precision was less than 7.1% with the bias range of -8.6 to 4.1%. This method was found to be specific, accurate, and sensitive and was successfully used to determine the accumulation of finasteride after in-vitro percutaneous delivery by liposomal or ethosomal drug delivery nanocarriers.
Eur J Pharm Sci. 2014 Feb 14;52:165-72. doi: 10.1016/j.ejps.2013.11.008. Epub 2013 Nov 19.
[h=1]Chitosan-decorated polystyrene-b-poly(acrylic acid) polymersomes as novel carriers for topicaldelivery of finasteride.[/h]Caon T1, Porto LC2, Granada A1, Tagliari MP1, Silva MA1, Simões CM1, Borsali R3, Soldi V4.
[h=3]Author information[/h]
[h=3]Abstract[/h]In view of the fact that the oral administration of finasteride (finasteride) has resulted in various undesirable systemic side effects, the topicalapplication of polystyrene and poly(acrylic acid)-based polymersomes (underexplored system) was investigated. Undecorated PS139-b-PAA17 and PS404-b-PAA63 vesicles (C3 and C7, respectively) or vesicles decorated with chitosan samples of different molecular weight (C3/CS-oligo, C7/CS-oligo, C3/CS-37 and C7/CS-37) were prepared by the co-solvent self-assembly method and characterized by small-angle X-ray scattering,transmission electron microscopy and dynamic light scattering techniques. In vitro release experiments and ex vivo permeation using Franz diffusion cells were carried out (through comparison with hydroethanolicfinasteride solution). The ideal system should provide high finasteride retention in the dermis and epidermis while allowing some control of the drug release. The particle size and in vitro release were negatively correlated with the permeation coefficient and skin retention in both the epidermis and dermis. The findings that the longest lag time was obtained for the hydroethanolic drug solution and lowest permeation for the systems able to release the drug faster support the hypothesis that nanostructured systems may be required to enhance the penetration and permeation of the drug. Chitosan-decorated polymersomes interacted more strongly with the skin components than non-decorated samples, probably due to the positive surface charge, which increased the finasteride retention and reduced the lag time. C7 polymersomes decorated with chitosan were more appropriate for topical applications (high retention in the dermis and epidermis and controlled drug delivery).
supermusic
Established Member
- Reaction score
- 34
Any news???
