Department of Pharmacology, Pharmacy and Pharmaceutical Technology, University of Santiago de Compostela, Spain; Industrial Pharmacy Institute, University of Santiago de Compostela, Spain.
Department of Pharmacology, Pharmacy and Pharmaceutical Technology, University of Santiago de Compostela, Spain; Industrial Pharmacy Institute, University of Santiago de Compostela, Spain.
Eur J Pharm Sci. 2018 May 30;117:270-278. doi: 10.1016/j.ejps.2018.02.028. Epub 2018 Mar 6.
Soluble derivatives of β-cyclodextrin (CD) have a high capacity to solubilise hydrophobic molecules and to interact with proteins and membrane component. As consequence CD derivatives shows a significant activity as drug absorption enhancers through different delivery routes, such as the oral, nasal, ocular or topical route. In this paper, the effect of two CD derivatives -methyl-β-cyclodextrin (MBCD) and hydroxypropyl-β-cyclodextrin (HPB)- on the structure and permeability of the nail plate has been studied using the drug model ciclopirox olamine. Results shows that MBCD and HPB interacting with the nail plate components, modifying their microporous structure and swelling characteristics. The ability of the cyclodextrins to interact with aromatic amino acids and to stabilise and unfold protein structures could be the most likely mechanisms responsible of the nail microstructure modifications. Aditionally CD allows to increase the soluble dose of ciclopirox olamine in aqueous lacquers made with poloxamer and N-acetylcysteine via the formation of high solubility complexes with the drug. Finally the studies of diffusion and penetration obtained using bovine hoof model confirm the enhancing effect of the cyclodextrins on the penetration and accumulation of the drug in the nail structure. Results shows the great potential of the CD for the elaboration of aqueous based nail lacquers containing hidrofobic drugs.
β-环糊精（CD）的可溶性衍生物能够高效增溶疏水分子，并与蛋白质和膜成分相互作用。因此，CD 衍生物作为通过不同给药途径（如口服、鼻内、眼部或局部途径）的药物吸收增强剂具有显著的活性。在本文中，使用药物模型环吡罗司胺研究了两种 CD 衍生物-甲基-β-环糊精（MBCD）和羟丙基-β-环糊精（HPB）对指甲板结构和通透性的影响。结果表明，MBCD 和 HPB 与指甲板成分相互作用，改变其微孔结构和溶胀特性。CD 与芳香族氨基酸相互作用以及稳定和展开蛋白质结构的能力可能是导致指甲微观结构发生变化的最主要机制。此外，CD 能够通过与药物形成高溶解度的配合物，增加以泊洛沙姆和 N-乙酰半胱氨酸为基础的水性指甲油中环吡罗司胺的可溶性剂量。最后，使用牛蹄模型进行的扩散和渗透研究证实了 CD 对药物在指甲结构中的渗透和积累的增强作用。结果表明，CD 在制备含有疏水性药物的水性指甲漆方面具有巨大的潜力。
