a liposomal lotion containing cyproterone acetate as the active substance may just as well be a good alternative to topical liposomal RU for all those diffuse thinners out there who are not willing to order RU from china and are fed up with oral drugs killing their libido and messing up with their hormones. In addition cyproterone has proven to be really effective as a topical treatment with minimal systemic absorption even in an alcohol base.
read the article hereunder and let me know what you think
Jana Štecová1, Wolfgang Mehnert1, Tobias Blaschke2, Burkhard Kleuser1, Ramadurai Sivaramakrishnan2, Christos C. Zouboulis3, Holger Seltmann3, Hans Christian Korting4, Klaus D. Kramer2 and Monika Schäfer-Korting1
(1) Institut für Pharmazie, Freie Universität Berlin, Königin-Luise-Straße 2-4, D-14195 Berlin, Germany
(2) Institut für Physik, Freie Universität Berlin, Berlin, Germany
(3) Dermatologische Klinik, Charité-Universitätsmedizin Berlin, Campus Benjamin Franklin, Germany
(4) Dermatologische Klinik, Ludwig-Maximilians-Universität, München, Germany
Received: 5 July 2006 Accepted: 22 December 2006 Published online: 20 March 2007
Abstract
Purpose Topical cyproterone acetate (CPA) treatment of skin diseases should reduce side effects currently excluding the use in males and demanding contraceptive measures in females. To improve skin penetration of the poorly absorbed drug, we intended to identify the active moiety and to load it to particulate carrier systems.
Materials and Methods CPA metabolism in human fibroblasts, keratinocytes and a sebocyte cell line as well as androgen receptor affinity of native CPA and the hydrolysis product cyproterone were determined. CPA 0.05% loaded solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), a nanoemulsion and micropheres were characterized for drug-particle interaction and CPA absorption using human skin ex-vivo.
Results Native CPA proved to be the active agent. Application of CPA attached to SLN increased skin penetration at least four-fold over the uptake from cream and nanoemulsion. Incorporation into the lipid matrix of NLC and microspheres resulted in a 2–3-fold increase in CPA absorption. Drug amounts with hair
in the dermis were low with all preparations. No difference was seen in the penetration into intact and stripped skin.
Conclusion With particulate systems topical CPA treatment may be an additional therapeutic option for acne and other diseases of the pilosebaceous unit.
Key words cyproterone acetate - lipid particles - nanostructured lipid carriers - parelectric spectroscopy - pharmacological effects - skin absorption
P.S. in the end even if you don't pop a pill every single day you can keep a full head of hair!!!
read the article hereunder and let me know what you think
Jana Štecová1, Wolfgang Mehnert1, Tobias Blaschke2, Burkhard Kleuser1, Ramadurai Sivaramakrishnan2, Christos C. Zouboulis3, Holger Seltmann3, Hans Christian Korting4, Klaus D. Kramer2 and Monika Schäfer-Korting1
(1) Institut für Pharmazie, Freie Universität Berlin, Königin-Luise-Straße 2-4, D-14195 Berlin, Germany
(2) Institut für Physik, Freie Universität Berlin, Berlin, Germany
(3) Dermatologische Klinik, Charité-Universitätsmedizin Berlin, Campus Benjamin Franklin, Germany
(4) Dermatologische Klinik, Ludwig-Maximilians-Universität, München, Germany
Received: 5 July 2006 Accepted: 22 December 2006 Published online: 20 March 2007
Abstract
Purpose Topical cyproterone acetate (CPA) treatment of skin diseases should reduce side effects currently excluding the use in males and demanding contraceptive measures in females. To improve skin penetration of the poorly absorbed drug, we intended to identify the active moiety and to load it to particulate carrier systems.
Materials and Methods CPA metabolism in human fibroblasts, keratinocytes and a sebocyte cell line as well as androgen receptor affinity of native CPA and the hydrolysis product cyproterone were determined. CPA 0.05% loaded solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), a nanoemulsion and micropheres were characterized for drug-particle interaction and CPA absorption using human skin ex-vivo.
Results Native CPA proved to be the active agent. Application of CPA attached to SLN increased skin penetration at least four-fold over the uptake from cream and nanoemulsion. Incorporation into the lipid matrix of NLC and microspheres resulted in a 2–3-fold increase in CPA absorption. Drug amounts with hair
in the dermis were low with all preparations. No difference was seen in the penetration into intact and stripped skin.
Conclusion With particulate systems topical CPA treatment may be an additional therapeutic option for acne and other diseases of the pilosebaceous unit.
Key words cyproterone acetate - lipid particles - nanostructured lipid carriers - parelectric spectroscopy - pharmacological effects - skin absorption
P.S. in the end even if you don't pop a pill every single day you can keep a full head of hair!!!
