Berton Paula, Di Bona Kristin R, Yancey Denise, Rizvi Syed A A, Gray Marquita, Gurau Gabriela, Shamshina Julia L, Rasco Jane F, Rogers Robin D
Department of Chemistry, The University of Alabama, Tuscaloosa, Alabama 35487, United States.
Department of Chemistry, McGill University, 801 Sherbrooke Street West, Montreal, Quebec H3A 0B8, Canada.
ACS Med Chem Lett. 2017 Apr 12;8(5):498-503. doi: 10.1021/acsmedchemlett.6b00504. eCollection 2017 May 11.
Tuning the bioavailability of lidocaine was explored by its incorporation into the ionic liquid lidocainium docusate ([Lid][Doc]) and the deep eutectic Lidocaine·Ibuprofen (Lid·Ibu) and comparing the transdermal absorption of these with the crystalline salt lidocainium chloride ([Lid]Cl). Each form of lidocaine was dissolved in a vehicle cream and topically applied to Sprague-Dawley rats. The concentrations of the active pharmaceutical ingredients (APIs) in blood plasma were monitored over time as an indication of systemic absorption. The concentration of lidocaine in plasma varied between applied API-based creams, with faster and higher systemic absorption of the hydrogen bonded deep eutectic Lid·Ibu than the absorption of the salts [Lid]Cl or [Lid][Doc]. Interestingly, a differential transdermal absorption was observed between lidocaine and ibuprofen when Lid·Ibu was applied, possibly indicating different interactions with the tissue components.
通过将利多卡因掺入离子液体多库酯利多卡因（[Lid][Doc]）和低共熔物利多卡因·布洛芬（Lid·Ibu）中，并将它们与结晶盐氯化利多卡因（[Lid]Cl）的经皮吸收进行比较，来探索调节利多卡因的生物利用度。每种形式的利多卡因都溶解在赋形剂乳膏中，并局部应用于Sprague-Dawley大鼠。随着时间的推移监测血浆中活性药物成分（API）的浓度，作为全身吸收的指标。基于所应用的含API乳膏，血浆中利多卡因的浓度有所不同，与盐[Lid]Cl或[Lid][Doc]相比，通过氢键结合的低共熔物Lid·Ibu的全身吸收更快且更高。有趣的是，当应用Lid·Ibu时，观察到利多卡因和布洛芬之间存在差异经皮吸收，这可能表明它们与组织成分的相互作用不同。
