Oh Jae-Ho, Park Hyoun-Hyang, Do Ki-Young, Han Manhee, Hyun Dong-Hun, Kim Chang-Gyu, Kim Chang-Hyeon, Lee Seung S, Hwang Sung-Joo, Shin Sang-Chul, Cho Cheong-Weon
Chungnam National University, Daejeon, South Korea.
Eur J Pharm Biopharm. 2008 Aug;69(3):1040-5. doi: 10.1016/j.ejpb.2008.02.009. Epub 2008 Feb 19.
Despite the advantages of drug delivery through the skin, such as easy accessibility, convenience, prolonged therapy, avoidance of the liver first-pass metabolism and a large surface area, transdermal drug delivery is only used with a small subset of drugs because most compounds cannot cross the skin at therapeutically useful rates. Recently, a new concept was introduced known as microneedles and these could be pierced to effectively deliver drugs using micron-sized needles in a minimally invasive and painless manner. In this study, biocompatible polycarbonate (PC) microneedle arrays with various depths (200 and 500 microm) and densities (45, 99 and 154 ea/cm2) were fabricated using a micro-mechanical process. The skin permeability of a hydrophilic molecule, calcein (622.5D), was examined according to the delivery systems of microneedle, drug loading, depth of the PC microneedle, and density of the PC microneedle. The skin permeability of calcein was the highest when the calcein gel was applied to the skin with the 500 microm-depth PC microneedle, simultaneously. In addition, the skin permeability of calcein was the highest when 0.1g of calcein gel was coupled to the 500 microm-depth PC microneedle (154 ea/cm2) as well as longer microneedles and larger density of microneedles. Taken together, this study suggests that a biocompatible PC microneedle might be a suitable tool for transdermal drug delivery system of hydrophilic molecules with the possible applications to macromolecules such as proteins and peptides.
尽管通过皮肤给药具有诸多优势，如易于给药、方便、治疗时间长、避免肝脏首过代谢以及皮肤表面积大等，但透皮给药仅适用于一小部分药物，因为大多数化合物无法以治疗有效的速率穿过皮肤。最近，引入了一种称为微针的新概念，这些微针可以通过微米级的针头以微创且无痛的方式有效给药。在本研究中，使用微机械工艺制造了具有不同深度（200和500微米）和密度（45、99和154根/平方厘米）的生物相容性聚碳酸酯（PC）微针阵列。根据微针给药系统、药物负载量、PC微针的深度和PC微针的密度，研究了亲水性分子钙黄绿素（622.5D）的皮肤渗透率。当将钙黄绿素凝胶与500微米深度的PC微针同时应用于皮肤时，钙黄绿素的皮肤渗透率最高。此外，当0.1克钙黄绿素凝胶与500微米深度的PC微针（154根/平方厘米）以及更长的微针和更大的微针密度结合时，钙黄绿素的皮肤渗透率也最高。综上所述，本研究表明，生物相容性PC微针可能是亲水性分子透皮给药系统的合适工具，并可能应用于蛋白质和肽等大分子。
