34554-28-4Relevant articles and documents
Cyproterone acetate loading to lipid nanoparticles for topical acne treatment: Particle characterisation and skin uptake
Stecova, Jana,Mehnert, Wolfgang,Blaschke, Tobias,Kleuser, Burkhard,Sivaramakrishnan, Ramadurai,Zouboulis, Christos C.,Seltmann, Holger,Korting, Hans Christian,Kramer, Klaus D.,Schaefer-Korting, Monika
, p. 991 - 1000 (2007)
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 within 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.
Novel 17-esters of 17α-hydroxy gestogens, compositions containing such compounds, processes for their preparation and methods of treatment therewith
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, (2008/06/13)
This invention relates to novel 17α-esters of gestogens having an antitumour activity and to the preparation thereof. The invention is also concerned with pharmaceutical compositions containing the said compounds, and method of treatment therewith.
