Department of Pharmaceutics and Biopharmaceutics, Philipps-Universität Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany.
Molecules. 2021 Mar 15;26(6):1633. doi: 10.3390/molecules26061633.
Poor aqueous solubility of active compounds is a major issue in today's drug delivery. In this study the smartFilm-technology was exploited to improve the dermal penetration efficacy of a poorly soluble active compound (curcumin). Results were compared to the dermal penetration efficacy of curcumin from curcumin bulk suspensions and nanocrystals, respectively. The smartFilms enabled an effective dermal and transdermal penetration of curcumin, whereas curcumin bulk- and nanosuspensions were less efficient when the curcumin content was similar to the curcumin content in the smartFilms. Interestingly, it was found that increasing numbers of curcumin particles within the suspensions increased the passive dermal penetration of curcumin. The effect is caused by an aqueous meniscus that is created between particle and skin if the dispersion medium evaporates. The connecting liquid meniscus causes a local swelling of the stratum corneum and maintains a high local concentration gradient between drug particles and skin. Thus, leading to a high local passive dermal penetration of curcumin. The findings suggest a new dermal penetration mechanism for active compounds from nano-particulate drug delivery systems, which can be the base for the development of topical drug products with improved penetration efficacy in the future.
活性化合物的水溶性差是当今药物输送中的一个主要问题。在这项研究中，利用智能薄膜技术来提高一种水溶性差的活性化合物（姜黄素）的经皮渗透效果。结果与姜黄素块状悬浮液和纳米晶体的经皮渗透效果进行了比较。智能薄膜能够有效促进姜黄素的经皮和透皮渗透，而当姜黄素含量与智能薄膜中的姜黄素含量相同时，姜黄素块状和纳米悬浮液的效率则较低。有趣的是，研究发现，悬浮液中姜黄素颗粒数量的增加会增加姜黄素的被动经皮渗透。这种作用是由分散介质蒸发时在颗粒和皮肤之间形成的水弯月面引起的。连接的液体弯月面会导致角质层局部肿胀，并在药物颗粒和皮肤之间保持高的局部浓度梯度。因此，导致姜黄素的局部经皮渗透增加。这些发现为纳米颗粒药物输送系统中活性化合物的经皮渗透机制提供了新的认识，这可能为未来开发具有改善渗透效果的局部药物产品提供基础。
