Advanced Materials and Healthcare Technologies, School of Pharmacy, University of Nottingham, NG7 2RD, UK.
Walgreens Boots Alliance, Nottingham NG90 1BS, UK.
Int J Pharm. 2019 May 30;563:21-29. doi: 10.1016/j.ijpharm.2019.03.028. Epub 2019 Mar 15.
Vitamin C (ascorbic acid) is a naturally occurring, powerful anti-oxidant with the potential to deliver numerous benefits to the skin when applied topically. However, topical use of this compound is currently restricted by an instability in traditional formulations and the delivery and eventual fate of precursor compounds has been largely unexplored. Time of flight secondary ion mass spectrometry (ToF-SIMS) is an emerging technique in the field of skin research and offers detailed chemical analysis, with high mass and spatial resolution, as well as profiling capabilities that allow analysis as a function of sample depth. This work demonstrates the successful use of ToF-SIMS to obtain, in situ, accurate 3D permeation profiles of both ascorbic acid and a popular precursor, ascorbyl glucoside, from ex vivo porcine skin. The significant permeation enhancing effect of a supramolecular hydrogel formulation, produced from an amphiphilic gemini imidazolium-based surfactant, was also demonstrated for both compounds. Using ToF-SIMS, it was also possible to detect and track the breakdown of ascorbyl glucoside into ascorbic acid, elucidating the ability of the hydrogel formulation to preserve this important conversion until the targeted epidermal layer has been reached. This work demonstrates the potential of ToF-SIMS to provide 3D permeation profiles collected in situ from ex vivo tissue samples, offering detailed analysis on compound localisation and degradation. This type of analysis has significant advantages in the area of skin permeation, but can also be readily translated to other tissue types.
维生素 C(抗坏血酸)是一种天然存在的、强大的抗氧化剂,当局部应用于皮肤时,有可能带来许多益处。然而,由于传统配方的不稳定性,以及前体化合物的传递和最终命运在很大程度上仍未得到探索,因此该化合物的局部应用目前受到限制。飞行时间二次离子质谱(ToF-SIMS)是皮肤研究领域的一项新兴技术,提供了详细的化学分析,具有高质量和空间分辨率,以及能够分析随样本深度变化的功能。这项工作展示了成功使用 ToF-SIMS 原位获得抗坏血酸和一种流行的前体化合物抗坏血基葡萄糖苷从离体猪皮中 3D 渗透分布的情况。还证明了一种由两亲Gemini 咪唑啉基表面活性剂形成的超分子水凝胶配方对这两种化合物都具有显著的增强渗透作用。通过 ToF-SIMS,还可以检测和跟踪抗坏血基葡萄糖苷分解为抗坏血酸,阐明水凝胶配方能够保持这种重要转化,直到达到目标表皮层。这项工作展示了 ToF-SIMS 从离体组织样本原位提供 3D 渗透分布的潜力,提供了关于化合物定位和降解的详细分析。这种类型的分析在皮肤渗透领域具有显著的优势,但也可以很容易地转化到其他组织类型。