University of Vienna, Research Platform 'Characterisation of Drug Delivery Systems on Skin and Investigations of Involved Mechanisms', Althanstraße 14, 1090 Vienna, Austria.
University of Vienna, Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Life Sciences, Althanstraße 14, 1090 Vienna, Austria.
Int J Pharm. 2015 Feb 1;479(1):70-6. doi: 10.1016/j.ijpharm.2014.12.048. Epub 2014 Dec 24.
The choice of appropriate excipients is crucial for the success of a dermal drug delivery system. Especially surfactants should be chosen carefully, because of their possible interactions with the skin or the applied drug. Since monoacyl phosphatidylcholine (MAPL) exhibits great emulsification properties and can be derived from natural sources, it is of great interest as surfactant in microemulsions. Therefore, the aim of the present study was to investigate the effect of the MAPL content on the formation of microemulsions. The great emulsification power of MAPL was confirmed by increased isotropic areas with increasing MAPL content. Moreover, a decrease in particle size, particle size distribution and viscosity with increasing MAPL content was determined. Besides its effects on microemulsion structure, MAPL exhibited a significant influence on the skin permeation of flufenamic acid. Interestingly, the higher the MAPL content, the lower was the skin permeation of flufenamic acid. A possible explanation might be that the hydrophilic MAPL could hinder the permeation of the lipophilic drug. In contrast, the skin permeation enhancing effects of the microemulsion with the lowest MAPL content might be attributed to formation of a patch-like structure and therefore better contact between the formulation and the skin.
选择合适的赋形剂对于经皮药物传递系统的成功至关重要。特别是表面活性剂的选择应格外谨慎，因为它们可能与皮肤或应用药物相互作用。由于单酰基磷脂酰胆碱 (MAPL) 具有出色的乳化性能，并且可以从天然来源中获得，因此它作为微乳液中的表面活性剂具有很大的应用潜力。因此，本研究的目的是研究 MAPL 含量对微乳液形成的影响。随着 MAPL 含量的增加，各向同性区域的增加证实了 MAPL 的强大乳化能力。此外，还确定了随着 MAPL 含量的增加，粒径、粒径分布和粘度减小。除了对微乳液结构的影响外，MAPL 对 flufenamic acid 的经皮渗透也有显著影响。有趣的是，MAPL 含量越高，flufenamic acid 的经皮渗透越低。一种可能的解释是亲水性的 MAPL 可能会阻碍亲脂性药物的渗透。相比之下，具有最低 MAPL 含量的微乳液的皮肤渗透增强作用可能归因于形成片状结构，从而使制剂与皮肤更好地接触。
