[Transdermal delivery of cyclosporin A solubilized in mixed micelles through mice skin].
OBJECTIVE
To investigate the transdermal delivery effects of cyclosporine A solubilized in mixed micelles composed of phospholipid and different surfactants.


METHODS
When applied onto the excised abdominal skin of the mice occlusively, the enhancing effects of various mixed micelles on the penetration of cyclosporin A were assessed by an in vitro permeation technique. In vivo study was carried out by topical application of sodium cholate-phospholipid mixed micelles onto the mice skin and drug blood concentration was detected.


RESULTS
In vitro, mixed micelles containing different surfactants displayed distinct permeability and corresponded to the following order: sodium cholate > sodium deoxycholate > Trition X-100 > Tween-20. In vivo, peak drug concentration was detected at 5 h and after that the concentration fell down slowly.


CONCLUSIONS
Mixed micelles were shown to be efficient carrier for the transdermal delivery of the lipophilic polypeptide when kept in solution during the application process.
Wu
T
T
Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China.
Guo
J X
JX
Ping
Q N
QN
Jin
F Y
FY
Sun
X W
XW
D000279:Administration, Cutaneous; D000818:Animals; D016572:Cyclosporine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D003840:Deoxycholic Acid / Q000737:chemistry; D004337:Drug Carriers; D016503:Drug Delivery Systems; D051379:Mice; D008823:Micelles; D010539:Permeability; D010743:Phospholipids; D011136:Polysorbates / Q000737:chemistry; D012869:Skin Absorption / Q000187:drug effects; D020358:Sodium Cholate / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry
D004337:Drug Carriers; D008823:Micelles; D010743:Phospholipids; D011136:Polysorbates; D013501:Surface-Active Agents; D003840:Deoxycholic Acid; D016572:Cyclosporine; D020358:Sodium Cholate