Pharmaceutical Sciences Depatrment, MCPHS University-Boston, 179 longwood ave, Boston, USA.
Pharmaceutical Sciences Biomedical and Pharmaceutical Sciences Department, College of Pharmacy, California Northstate University, 9700 Taron Dr, Elk Grove, California, 95757, USA.
AAPS PharmSciTech. 2018 Jan;19(1):114-122. doi: 10.1208/s12249-017-0800-7. Epub 2017 Jun 15.
The permeability enhancement effect of oleic acid (OA) and propylene glycol (PG) as well as their (1:1 v/v) combined mixture was studied using rat skin. The percutaneous drug administration is a challenge and an opportunity for drug delivery. To date, there is limited research that illustrates the mechanism of penetration enhancers and their combinations on the skin. This project aims to explore the skin diffusion and penetration enhancement of PG, OA, and a combination of PG-OA (1:1 v/v) on rat skin and to identify the potential synergistic effect of the two enhancers utilizing Raman spectroscopy. Dissected dorsal skin was treated with either PG or OA or their combination for predetermined time intervals after which the Raman spectra of the treated skin were collected with the enhancer. A spectrum of the wiped and the washed skin were also collected. The skin integrity was tested before and after exposure to PG. The skin histology proved that the skin integrity has been maintained during experiments and the results indicated that OA disrupted rat skin lipid as evident by changes in the lipid peak. The results also showed that PG and OA improved the diffusion of each other and created faster, yet reversible changes of the skin peaks. In conclusion, Raman spectroscopy is a potential tool for ex vivo skin diffusion studies. We also concluded that PG and OA have potential synergistic reversible effect on the skin.
油酸(OA)和丙二醇(PG)及其(1:1v/v)混合物的通透性增强作用已在大鼠皮肤中进行了研究。经皮给药是药物输送的挑战和机遇。迄今为止,有关渗透促进剂及其在皮肤上的组合的渗透机制的研究有限。本项目旨在探索 PG、OA 以及 PG-OA(1:1v/v)混合物对大鼠皮肤的皮肤扩散和渗透增强作用,并利用拉曼光谱鉴定两种增强剂的潜在协同作用。在预定的时间间隔后,用 PG 或 OA 或它们的组合处理解剖的背部皮肤,然后用增强剂收集处理过的皮肤的拉曼光谱。还收集了擦拭和清洗过的皮肤的光谱。在接触 PG 之前和之后测试了皮肤的完整性。皮肤组织学证明,在实验过程中保持了皮肤的完整性,结果表明 OA 破坏了大鼠皮肤脂质,脂质峰发生了变化。结果还表明,PG 和 OA 改善了彼此的扩散,并使皮肤峰更快但可逆地发生变化。总之,拉曼光谱是一种用于离体皮肤扩散研究的潜在工具。我们还得出结论,PG 和 OA 对皮肤具有潜在的协同可逆作用。