Puglisi G, Fresta M, La Rosa C, Ventura C A, Panico A M, Mazzone G
Istituto di Chimica Farmaceutica e Tossicologica, Università di Catania, Italy.
Pharmazie. 1992 Mar;47(3):211-5.
In this paper we report the investigation of the potential of liposomes as drug carrier for citicoline (1; CDP-choline). The aim of our work is to improve the pharmacokinetic and pharmacodynamic parameters of the drug to facilitate the overcoming of the blood-brain barrier. The thermotropic behaviour of hydrated dispersions of various phospholipids and their mixtures containing 1 have been investigated by differential scanning calorimetry (DSC) to have a clear view of the interaction between the drug and the liposome phospholipids. By the values of transition peak temperature (Tm) and transition enthalpy (delta H) we note a strong interaction between 1 and the polar heads of L-alpha-dipalmitoylphosphatidic acid (DPPA) and L-alpha-dipalmitoylphosphatidylserine (DPPS), whereas there is not any considerable interaction between the drug and L-alpha-dipalmitoylphosphatidylcholine (DPPC) or L-alpha-dimyristoylphosphatidylcholine (DMPC); in any case no interaction occurs between 1 and the hydrophobic part of the phospholipid. So we conclude that all the drug is fitted into the aqueous spaces. The results of the encapsulation efficiency experiments demonstrate how the encapsulation capacity increase with using charged phospholipids, reaching the top with DPPA. Moreover, it was noted that the presence of Cholesterol (Chol) enhances the encapsulation capacity (EC) and drug content (DC) values of DPPC, a neutral phospholipid. The size of the liposomes was determined by light scattering (LS).
在本文中，我们报告了对脂质体作为胞磷胆碱（1；CDP - 胆碱）药物载体潜力的研究。我们工作的目的是改善该药物的药代动力学和药效学参数，以促进血脑屏障的跨越。通过差示扫描量热法（DSC）研究了各种磷脂及其含1的混合物的水合分散体的热致行为，以便清楚了解药物与脂质体磷脂之间的相互作用。通过转变峰温度（Tm）和转变焓（ΔH）的值，我们注意到1与L-α-二棕榈酰磷脂酸（DPPA）和L-α-二棕榈酰磷脂酰丝氨酸（DPPS）的极性头部之间有强烈的相互作用，而药物与L-α-二棕榈酰磷脂酰胆碱（DPPC）或L-α-二肉豆蔻酰磷脂酰胆碱（DMPC）之间没有任何显著的相互作用；在任何情况下，1与磷脂的疏水部分之间都不发生相互作用。因此我们得出结论，所有药物都被包入水相空间。包封率实验结果表明，使用带电磷脂时包封能力如何增加，以DPPA时达到最高。此外，还注意到胆固醇（Chol）的存在提高了中性磷脂DPPC的包封能力（EC）和药物含量（DC）值。通过光散射（LS）测定脂质体的大小。
