Skin penetration enhancement by a microneedle device (Dermaroller®) in vitro: Dependency on needle size and applied formulation

This study focused on the in vitro evaluation of skin perforation using a new microneedle device (Dermaroller (R)) with different needle lengths (150, 500 and 1500 mu m). The influence of the microneedle treatment on the morphology of the skin surface (studied by light and scanning electron microscopy), on the transepidermal water loss (TEWL) and on the penetration and permeation of hydrophilic model drugs was investigated using excised human full-thickness skin. Furthermore, invasomes - highly flexible phospholipid vesicles containing terpenes and ethanol as penetration enhancer - were compared with an aqueous solution. Elevated TEWL values were measured after Dermaroller (R)) treatment compared to untreated human skin with a gradual increase of the TEWL over the first hour whereas afterwards the TEWL values decreased probably caused by a reduction of the pore size with time. Skin perforation with the Dermarollers (R) enhanced drug penetration and permeation for both formulations tested. Invasomes were more effective to deliver hydrophilic compounds into and through the skin compared to the aqueous drug solutions and the combination with skin perforation further enhanced drug penetration and permeation. In conclusion, Dermarollers (R) being already commercially available for cosmetic purposes appear also promising for drug delivery purposes particularly those with medium (500 mu m) and shorter (150 mu m) needle lengths. (c) 2008 Elsevier B.V. All rights reserved.