Transdermal delivery of mixnoxidil with block copolymer nanoparticles.
We evaluated the effect of hydrodynamic size of self-assembled nanoparticles on skin penetration of minoxidil in vitro and in vivo. Self-assembled 40- and 130-nm nanoparticles, both containing minoxidil, were prepared by solvent evaporation of poly(-caprolactone)-block-poly(ethyleneglycol) and were applied onto the skin of both hairy and hairless guinea pigs in the Franz diffusion cell. In hairy guinea pig skin, the permeation of the minoxidil that incorporated in 40-nm nanoparticles was 1.5-fold higher in the epidermal layer and 1.7-fold higher in the receptor solution than that of 130-nm nanoparticles. Nanoparticle size dependence on the permeation behavior of minoxidil was not observed for hairless guinea pig skin in either the epidermal layer or the receptor solution. Phospholipid liposomes and ethanol-water admixture, on the other hand, containing the same amount of minoxidil did not show differences in the amount of permeation irrespective of the existence of hair follicles. Confocal microscopy coupled with in vivo and in vitro skin permeation results demonstrated that nanoparticles containing solutes penetrated mainly via shunt routes like hair follicles, resulting in skin absorption of solutes.
Shim
Jongwon
J
Nanotechnology Research Laboratory, Skin Research Institute, R&D Center, AMOREPACIFIC Corp., 314-1 Bora-ri, Giheug-eup, Yeongin-si, Gyeonggi-do, Seoul 449-729, South Korea. jwshim@mac.com
Seok Kang
Hyung
H
Park
Won-Seok
WS
Han
Sang-Hun
SH
Kim
Junoh
J
Chang
Ih-Seop
IS
D000279:Administration, Cutaneous; D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007773:Lactates / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051379:Mice; D008812:Mice, Hairless; D008810:Mice, Inbred C57BL; D008914:Minoxidil / Q000008:administration & dosage* / Q000493:pharmacokinetics; D049329:Nanostructures; D010316:Particle Size; D011092:Polyethylene Glycols / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology
D007773:Lactates; C088513:poly(lactic acid-ethylene glycol); D011092:Polyethylene Glycols; D008914:Minoxidil