DSC 研究新型 sigma 配体 PPCC 对 DMPC 脂质膜的影响。
DSC investigation of the effect of the new sigma ligand PPCC on DMPC lipid membrane.
机构信息
Department of Drug Sciences, University of Catania, Viale A. Doria, 6, Catania 95125, Italy.
Department of Health Sciences, University "Magna Graecia" of Catanzaro, Viale S. Venuta, Germaneto - Catanzaro 88100, Italy.
出版信息
Int J Pharm. 2014 Jul 20;469(1):88-93. doi: 10.1016/j.ijpharm.2014.04.052. Epub 2014 Apr 23.
The new sigma ligand cis-(±)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl) methyl]-1-(4-methylphenyl) cyclopropanecarboxylate [(±)-PPCC] is a promising tool for the treatment of various diseases. With the aim to investigate the absorption of (±)-PPCC by the cell membranes, in this study we evaluated the influence on thermotropic behavior of membrane model exerted by PPCC both as free base or as oxalic salt. To fulfill this purpose differential scanning calorimetry was used. The findings highlight that PPCC affects the thermodynamic parameters of phospholipids in different manner depending on whether it is in the salt or base form as well as function of the amount of drugs dispersed in the lipid matrix. The salt form of PPCC was uptaken by the membrane model faster than the free base. In addition, preliminary information on the use of a lipophilic carrier for PPCC was obtained.
新型西格玛配体顺式-(±)-甲基(1R,2S/1S,2R)-2-[(4-羟基-4-苯基哌啶-1-基)甲基]-1-(4-甲基苯基)环丙烷羧酸酯[(±)-PPCC]是治疗各种疾病的有前途的工具。为了研究细胞膜对(±)-PPCC 的吸收，本研究评估了 PPCC 作为游离碱或草酸盐对膜模型热性质的影响。为了实现这一目的，使用了差示扫描量热法。研究结果表明，PPCC 以不同的方式影响磷脂的热力学参数，这取决于它是盐还是碱的形式以及药物在脂质基质中的分散量。PPCC 的盐形式比游离碱更快地被膜模型吸收。此外，还获得了关于使用亲脂载体来负载 PPCC 的初步信息。
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