Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Mercer University, Atlanta, Georgia 30341, USA.
AAPS J. 2011 Sep;13(3):473-81. doi: 10.1208/s12248-011-9288-3. Epub 2011 Jul 6.
Transdermal delivery of therapeutic agents for cosmetic therapy is limited to small and lipophilic molecules by the stratum corneum barrier. Microneedle technology overcomes this barrier and offers a minimally invasive and painless route of administration. DermaRoller(®), a commercially available handheld device, has metal microneedles embedded on its surface which offers a means of microporation. We have characterized the microneedles and the microchannels created by these microneedles in a hairless rat model, using models with 370 and 770 μm long microneedles. Scanning electron microscopy was employed to study the geometry and dimensions of the metal microneedles. Dye binding studies, histological sectioning, and confocal microscopy were performed to characterize the created microchannels. Recovery of skin barrier function after poration was studied via transepidermal water loss (TEWL) measurements, and direct observation of the pore closure process was investigated via calcein imaging. Characterization studies indicate that 770 μm long metal microneedles with an average base width of 140 μm and a sharp tip with a radius of 4 μm effectively created microchannels in the skin with an average depth of 152.5 ± 9.6 μm and a surface diameter of 70.7 ± 9.9 μm. TEWL measurements indicated that skin regains it barrier function around 4 to 5 h after poration, for both 370 and 770 μm microneedles. However, direct observation of pore closure, by calcein imaging, indicated that pores closed by 12 h for 370 μm microneedles and by 18 h for 770 μm microneedles. Pore closure can be further delayed significantly under occluded conditions.
经皮传递治疗剂用于美容治疗受到角质层屏障的限制,只能传递小的亲脂性分子。微针技术克服了这一障碍,提供了一种微创、无痛的给药途径。DermaRoller(®)是一种市售的手持设备,其表面嵌入有金属微针,提供了微孔的方法。我们已经在无毛大鼠模型中对微针及其在该模型中产生的微通道进行了特征描述,使用了 370μm 和 770μm 长的微针模型。扫描电子显微镜用于研究金属微针的几何形状和尺寸。通过染料结合研究、组织切片和共聚焦显微镜对创建的微通道进行了特征描述。通过经皮水分丢失(TEWL)测量研究了穿孔后皮肤屏障功能的恢复情况,并通过钙黄绿素成像直接观察了孔的闭合过程。特征描述研究表明,770μm 长的金属微针,平均基底宽度为 140μm,尖端锋利,半径为 4μm,能够有效地在皮肤中形成微通道,微通道的平均深度为 152.5±9.6μm,表面直径为 70.7±9.9μm。TEWL 测量表明,对于 370μm 和 770μm 微针,皮肤在穿孔后 4 到 5 小时恢复其屏障功能。然而,通过钙黄绿素成像直接观察孔的闭合情况表明,370μm 微针的孔在 12 小时关闭,770μm 微针的孔在 18 小时关闭。在封闭条件下,孔的闭合可以进一步显著延迟。