Hatziantoniou Sophia, Demetzos Costas
Dept. of Pharmaceutical Technology, School of Pharmacy, University of Athens, Panepistimiopolis, Athens, Greece.
J Liposome Res. 2006;16(4):321-30. doi: 10.1080/08982100600992278.
Liposomes are widely used vehicles for the delivery of bioactive molecules. They are composed mainly from acyl-phosphatidylcholines, cholesterol, and charged lipids (e.g., stearylamine, dipalmitoylphosphatidylglycerol (DPPG), phosphatidylethanolamine). The incorporation efficiencies of the bioactive molecule and the drug to lipid molar ratio are important factors for the assessment of the liposomal formulation. In order to successfully characterize a liposomal formulation, it is necessary to be able to accurately measure the lipids and the encapsulated molecule, using the smallest possible sample. The present work describes an analytical methodology on qualitative and quantitative determination of all the lipid ingredients that are involved in the liposome formulation, as well as the drug incorporation and the drug-lipid ratio, by a simultaneous measurement of all the liposomal ingredients using thin-layer chromatography coupled with a flame ionization detector (HPTLC/FID). The procedure requires only one measurement per sample, and it can be applied even in very small or much diluted samples. The proposed analytical method can be applied in general on all steps of the development of liposomal formulations. The purity and stability of the raw materials can also be easily evaluated. In addition the preparation procedure can be tracked in order to locate possible losses of raw material and errors of the preparation method resulting in the amelioration of the method.
脂质体是广泛用于递送生物活性分子的载体。它们主要由酰基磷脂酰胆碱、胆固醇和带电脂质(如硬脂胺、二棕榈酰磷脂酰甘油(DPPG)、磷脂酰乙醇胺)组成。生物活性分子的包封效率以及药物与脂质的摩尔比是评估脂质体制剂的重要因素。为了成功地表征脂质体制剂,有必要能够使用尽可能小的样品准确测量脂质和包封的分子。本工作描述了一种分析方法,通过使用薄层色谱结合火焰离子化检测器(HPTLC/FID)同时测量所有脂质体成分,对脂质体制剂中涉及的所有脂质成分以及药物包封率和药物-脂质比进行定性和定量测定。该方法每个样品仅需一次测量,甚至可应用于非常小或高度稀释的样品。所提出的分析方法通常可应用于脂质体制剂开发的所有步骤。还可以轻松评估原材料的纯度和稳定性。此外,可以跟踪制备过程,以定位原材料可能的损失和制备方法的误差,从而改进该方法。