Braem C, Blaschke T, Panek-Minkin G, Herrmann W, Schlupp P, Paepenmüller T, Müller-Goyman C, Mehnert W, Bittl R, Schäfer-Korting M, Kramer K D
Freie Universität Berlin, Fachbereich Pharmazie, Germany.
J Control Release. 2007 May 14;119(1):128-35. doi: 10.1016/j.jconrel.2007.01.017. Epub 2007 Feb 8.
According to recent investigations of nanoparticular carrier systems the mode of drug-particle interaction appears to influence drug penetration into the skin. For a more detailed insight into the molecular structure of drug loaded particles the two independent analytical methods, namely the parelectric spectroscopy (PS) and the electron spin resonance (ESR) have been applied to 4,5,5,-trimethyl-1-yloxy-3-imidazoline-2-spiro-3'-(5'()-cholestane) as a model drug. Spectra have been analyzed in dependence on the concentration of the spin label. Changes in the concentration-dependent dipole mobility and dipole density given by PS and the concentration-dependent rotational correlation time (ESR) which are a measure of the vicinity of carrier and/or the surfactant and guest molecule were studied with cholestane-labeled solid lipid nanoparticles (SLN), nanoparticular lipid carriers (NLC) and nanoemulsions (NE). The spin probes were attached to the SLN surface which consists of two distinct sub-compartments: the rim and the flat surface of the disk-like shapes. The shape could be observed by freeze-fraction electron microscopy. Spin probes, however, were incorporated into the carrier matrix in the cases of NLC and NE. Results of PS are verified by ESR which allows a more detailed insight. Taking the results together a detailed new model of 'drug'-particle interaction could be established.
根据最近对纳米颗粒载体系统的研究,药物与颗粒的相互作用模式似乎会影响药物渗透进入皮肤。为了更深入了解载药颗粒的分子结构,已将两种独立的分析方法,即顺电光谱法(PS)和电子自旋共振法(ESR)应用于4,5,5-三甲基-1-乙氧基-3-咪唑啉-2-螺-3'-(5'-胆甾烷)作为模型药物。已根据自旋标记物的浓度对光谱进行了分析。用胆甾烷标记的固体脂质纳米粒(SLN)、纳米颗粒脂质载体(NLC)和纳米乳剂(NE)研究了PS给出的浓度依赖性偶极迁移率和偶极密度的变化以及ESR给出的浓度依赖性旋转相关时间(作为载体和/或表面活性剂与客体分子接近程度的一种度量)。自旋探针附着在由两个不同子隔室组成的SLN表面:盘状形状的边缘和平坦表面。形状可通过冷冻蚀刻电子显微镜观察到。然而,在NLC和NE的情况下,自旋探针被掺入载体基质中。PS的结果通过ESR得到验证,这使得能有更详细的了解。综合这些结果,可以建立一个关于“药物”与颗粒相互作用的详细新模型。