Hefei National Laboratory for Physical Sciences at Microscale and School of Life Sciences, University of Science & Technology of China, Hefei, Anhui 230027, People's Republic of China.
Med Oncol. 2010 Jun;27(2):203-12. doi: 10.1007/s12032-009-9192-1. Epub 2009 Mar 12.
Realgar has been used successfully to treat diseases for thousands of years, but its poor water solubility and high toxicity hampered its further medical uses. Here, we first applied transdermal drug delivery system to deliver realgar nanoparticles to investigate its anticancer effect and toxicity in vivo. In this study, MTT assay and flow cytometry analysis demonstrated that realgar significantly suppressed the proliferation and induced apoptosis of B16 melanoma cells in a dose-dependent manner. Transdermal penetration studies in vitro showed realgar nanoparticles could be delivered efficiently through skin. Tests on tumor-bearing C57BL/6 mice displayed that realgar could decrease the tumor volume markedly via transdermal drug delivery compared with the intraperitoneal administration and the control. Hematoxylin-eosin and immunohistochemical staining revealed that it could inhibit angiogenesis. The monitoring of the hepatic injury, body weight, feeding behavior, motor activity, and skin irritation of each animal indicated little toxicity of realgar to mice. The results demonstrated that realgar nanoparticles can be dermally delivered to achieve high efficacy against menaloma in vivo with low toxicity.
雄黄在治疗疾病方面已经有几千年的历史了，但由于其水溶性差和毒性高，限制了其在医学上的进一步应用。在这里，我们首次应用经皮给药系统将雄黄纳米颗粒递送至体内，以研究其在体内的抗癌作用和毒性。在这项研究中，MTT 法和流式细胞术分析表明，雄黄纳米颗粒能够剂量依赖性地显著抑制 B16 黑素瘤细胞的增殖并诱导其凋亡。体外经皮渗透研究表明，雄黄纳米颗粒可以有效地透过皮肤传递。荷瘤 C57BL/6 小鼠的实验表明，与腹腔给药和对照组相比，经皮给药可以显著降低肿瘤体积。苏木精-伊红和免疫组织化学染色显示，它可以抑制血管生成。对每只动物的肝损伤、体重、摄食行为、运动活动和皮肤刺激的监测表明，雄黄对小鼠的毒性很小。结果表明，雄黄纳米颗粒可以经皮给药，从而在体内实现高效治疗黑素瘤，且毒性低。
