Department of Mechanical Engineering, K. N. Toosi University of Technology, Tehran, Iran.
Department of Mechanical Engineering, K. N. Toosi University of Technology, Tehran, Iran; Division of Nuclear medicine, Department of Radiology and Radiological Science, Johns Hopkins University, School of Medicine, Baltimore, MD, USA.; University of Waterloo, Waterloo, Ontario, Canada.
J Control Release. 2017 Sep 10;261:87-92. doi: 10.1016/j.jconrel.2017.06.016. Epub 2017 Jun 20.
Recently-introduced biocompatible polymeric microneedles offer an efficient method for drug delivery. Tranexamic acid is a novel drug for treating melasma that is administered both locally and orally and inhibits excessive melanin via melanocyte. The tranexamic acid biocompatible polymer microneedle used in this study was fabricated from PVP and methacrylic acid, using the lithography method. The required mechanical strength to pierce skin was attained by optimizing the ratio of PVP to methacrylic acid. Acute dermal toxicity was done, and drug diffusion in skin layers was simulated by calculating the diffusion coefficient of tranexamic acid in interstitial fluid (plasma). The biocompatible polymer microneedle was fabricated at 60°C. Needles could sustain 0.6N that is enough to pierce stratum corneum. 34% of the released drug was locally effective and the rest permeated through the skin. The pyramidal polymer microneedle in this study was fully released in skin in approx. 7h. This polymer microneedle has no dermal toxicity.
最近出现的生物相容聚合物微针为药物输送提供了一种有效的方法。氨甲环酸是一种新型的治疗黄褐斑的药物，它可以局部和口服给药，并通过黑素细胞抑制过量的黑色素。本研究中使用的氨甲环酸生物相容聚合物微针是由 PVP 和甲基丙烯酸使用光刻法制成的。通过优化 PVP 与甲基丙烯酸的比例，获得了刺穿皮肤所需的机械强度。进行了急性皮肤毒性试验，并通过计算氨甲环酸在间质液（血浆）中的扩散系数来模拟药物在皮肤层中的扩散。生物相容聚合物微针在 60°C 下制造。针能够承受 0.6N 的力，足以刺穿角质层。66%的释放药物具有局部疗效，其余药物渗透皮肤。本研究中的金字塔聚合物微针在大约 7 小时内在皮肤中完全释放。这种聚合物微针没有皮肤毒性。
