Corrias Francesco, Schlich Michele, Sinico Chiara, Pireddu Rosa, Valenti Donatella, Fadda Anna Maria, Marceddu Salvatore, Lai Francesco
Dept. Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, CNBS, University of Cagliari, Cagliari 09124, Italy.
Dept. Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, CNBS, University of Cagliari, Cagliari 09124, Italy; Istituto di Scienze delle Produzioni Alimentari (ISPA)-CNR, sez. di Sassari, 07040 Baldinca, Italy.
Int J Pharm. 2017 May 30;524(1-2):1-8. doi: 10.1016/j.ijpharm.2017.03.042. Epub 2017 Mar 21.
The strategy of formulating poorly soluble actives as nanosuspension has been explored by more than a thousand research papers, with some medicinal products for oral and intravenous use having reached the market or advanced clinical trials. Interestingly, there is a limited number of reports of nanosuspensions formulated for dermal and transdermal drug delivery. In the present work, a nanocrystals suspension of the fluorescent, water-insoluble dye Nile Red, is prepared through a media milling technique and exploited to characterize the fate of the nanosuspended drug when applied on the skin. More in detail, the accumulation of Nile Red nanocrystals inside the hair follicles is evidenced by scanning electron microscopy, and the diffusion of drug molecules in the different skin layers is evaluated by confocal microscopy and skin permeation studies. Overall, the combination of the analytical techniques provide a description of the mechanisms underlying dermal accumulation, and transdermal penetration of a drug formulated as a nanosuspension.
将难溶性活性成分制成纳米混悬液的策略已被一千多篇研究论文探讨过,一些口服和静脉用药品已上市或进入临床试验阶段。有趣的是,为皮肤和透皮给药制备纳米混悬液的报道数量有限。在本研究中,通过介质研磨技术制备了荧光性、水不溶性染料尼罗红的纳米晶体混悬液,并用于表征纳米混悬药物应用于皮肤后的命运。更详细地说,通过扫描电子显微镜证实了尼罗红纳米晶体在毛囊内的积累,并通过共聚焦显微镜和皮肤渗透研究评估了药物分子在不同皮肤层中的扩散。总体而言,这些分析技术的结合描述了纳米混悬液剂型药物在皮肤内蓄积和透皮渗透的潜在机制。