Shim Jongwon, Seok Kang Hyung, Park Won-Seok, Han Sang-Hun, Kim Junoh, Chang Ih-Seop
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.
J Control Release. 2004 Jul 7;97(3):477-84. doi: 10.1016/j.jconrel.2004.03.028.
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.
我们在体外和体内评估了自组装纳米颗粒的流体动力学尺寸对米诺地尔经皮渗透的影响。通过聚（ε-己内酯）-嵌段-聚（乙二醇）的溶剂蒸发制备了均含有米诺地尔的40纳米和130纳米自组装纳米颗粒，并将其应用于Franz扩散池中多毛和无毛豚鼠的皮肤。在多毛豚鼠皮肤中，包载于40纳米纳米颗粒中的米诺地尔在表皮层的渗透量比130纳米纳米颗粒高1.5倍，在受体溶液中的渗透量高1.7倍。对于无毛豚鼠皮肤，无论是在表皮层还是受体溶液中，均未观察到纳米颗粒大小对米诺地尔渗透行为的影响。另一方面，含有相同量米诺地尔的磷脂脂质体和乙醇-水混合物，无论毛囊是否存在，其渗透量均无差异。共聚焦显微镜结合体内和体外皮肤渗透结果表明，含溶质的纳米颗粒主要通过毛囊等旁路途径渗透，从而实现溶质的皮肤吸收。
