主页 > 医学信息 >
【文摘发布】醋酸环丙氯地孕酮脂质纳米粒治疗
Author：
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
Resource:Pharmaceutical Research, 24(5),991-1000
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 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.
PMID:17372681
【文摘发布】文摘类新闻投稿格式专贴
http://www.dxy.cn/bbs/post/view?bid=116&id=8600034&sty=1&tpg=1&age=0 Title：Cyproterone Acetate Loading to Lipid Nanoparticles for Topical Acne Treatment: Particle Characterisation and Skin Uptake
标题：醋酸环丙氯地孕酮脂质纳米粒治疗痤疮： 粒子特性及皮肤对药物的吸收
Author：
作者：
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
Resource:
出处： Pharmaceutical Research, 24(5),991-1000
Abstract：摘要：
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.
目的：采取避孕措施的女性外用醋酸环丙氯地孕酮(CPA) 治疗皮肤病应可减少药物副作用的产生。
To improve skin penetration of the poorly absorbed drug, we intended to identify the active moiety and to load it to particulate carrier systems.
为了提高吸收不良药物的皮肤穿透力，我们打算鉴定药物的活性半族，并将其载入粒子载体系统。
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.
材料和方法：
检测项目包括：人成纤维细胞、角质化细胞和皮脂腺细胞株中的CPA代谢；天然CPA的雄激素受体亲和力；水解产物－去乙酰环丙氯地孕酮。
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.
利用离体人皮肤对含0.05% CPA的固体脂质纳米粒(SLN)、纳米结构脂质载体(NLC)、纳米乳剂和微球进行鉴定，以了解药物粒子相互间作用和CPA的吸收情况。
Results：Native CPA proved to be the active agent.
结果：证明天然CPA为活性剂。
Application of CPA attached to SLN increased skin penetration at least four-fold over the uptake from cream and nanoemulsion.
阅读本文的人还阅读：
作者:admin@医学,生命科学 2011-02-19 17:11
医学,生命科学网