Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Szeged, H-6720, Hungary.
Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Szeged, H-6720, Hungary.
J Pharm Biomed Anal. 2018 May 30;154:1-6. doi: 10.1016/j.jpba.2018.02.056. Epub 2018 Mar 6.
The application of local anesthetics, usually administered by subcutaneous injection, is common in the course of diagnostic, therapeutic, and cosmetic dermatology procedures. The effective dermal delivery of lidocaine could offer a solution to many adverse effects caused by needle insertion, such as pain, local reactions or toxicity, and additionally, it avoids the disruption of anatomical landmarks. Therefore, novel dermal formulations of local anesthetics are needed to overcome the barrier function of the skin and provide sufficient and prolonged anesthesia. In our study, we aimed to investigate and compare the penetration profiles of four different lidocaine containing formulations (hydrogel, oleogel, lyotropic liquid crystal and nanostructured lipid carrier) by Raman microscopic mapping of the drug. The application of Raman spectroscopy provided information about the spatial distribution of lidocaine in the skin ex vivo. The penetration of lidocaine from lyotropic liquid crystal and nanostructured carrier reached deeper skin layers and a higher amount of the drug was diffused into the skin, compared with hydrogel and oleogel. This study confirmed that nanostructured carriers can improve skin penetration properties of lidocaine and proved the applicability of Raman spectroscopy in the research of dermatological preparations ex vivo as a nondestructive, relatively easy and fast technique.
局部麻醉剂的应用,通常通过皮下注射给药,在诊断、治疗和美容皮肤科手术过程中很常见。将利多卡因有效递送至皮肤,可以解决因针刺引起的许多不良反应,如疼痛、局部反应或毒性,并且还可以避免破坏解剖学标志。因此,需要新型的局部麻醉剂透皮制剂来克服皮肤的屏障功能,提供足够和持久的麻醉效果。在我们的研究中,我们旨在通过拉曼显微镜图谱研究和比较四种不同含有利多卡因的制剂(水凝胶、油凝胶、溶致液晶和纳米结构脂质载体)的渗透特性。拉曼光谱的应用提供了关于药物在皮肤中空间分布的信息。与水凝胶和油凝胶相比,溶致液晶和纳米结构载体中的利多卡因渗透到更深的皮肤层,并且更多的药物扩散到皮肤中。这项研究证实了纳米结构载体可以改善利多卡因的皮肤渗透性能,并证明了拉曼光谱在作为一种非破坏性、相对简单和快速的技术的体外研究皮肤科制剂中的适用性。