Formulation and Drug Delivery Research Group, School of Pharmacy and Biomolecular Sciences, Liverpool John Moores University, Liverpool, UK.
Institute of Clinical Sciences, University of Liverpool Dental School, Liverpool, UK.
J Pharm Sci. 2018 May;107(5):1237-1246. doi: 10.1016/j.xphs.2018.01.005. Epub 2018 Jan 11.
Understanding the effect of surfactant properties is critical when designing vesicular delivery systems. This review evaluates previous studies to explain the influence of surfactant properties on the behavior of lipid vesicular systems, specifically their size, charge, stability, entrapment efficiency, pharmacokinetics, and pharmacodynamics. Generally, the size of vesicles decreases by increasing the surfactant concentration, carbon chain length, the hydrophilicity of the surfactant head group, and the hydrophilic-lipophilic balance. Increasing surfactant concentration can also lead to an increase in charge, which in turn reduces vesicle aggregation and enhances the stability of the system. The vesicles' entrapment efficiency not only depends on the surfactant properties but also on the encapsulated drug. For example, the encapsulation of a lipophilic drug could be enhanced by using a surfactant with a low hydrophilic-lipophilic balance value. Moreover, the membrane permeability of vesicles depends on the surfactant's carbon chain length and transition temperature. In addition, surfactants have a clear influence on pharmacokinetics and pharmacodynamics such as sustaining drug release, enhancing the circulation time of vesicles, improving targeting and cellular uptake.
当设计囊泡递药系统时,了解表面活性剂性质的影响至关重要。本综述评估了以往的研究,以解释表面活性剂性质对脂质囊泡系统行为的影响,特别是对其大小、电荷、稳定性、包封效率、药代动力学和药效学的影响。通常,通过增加表面活性剂浓度、碳链长度、表面活性剂亲水基团的亲水性和亲水亲油平衡,可以减小囊泡的大小。增加表面活性剂浓度还可能导致电荷增加,从而减少囊泡聚集并增强系统稳定性。囊泡的包封效率不仅取决于表面活性剂的性质,还取决于包封的药物。例如,使用亲水亲油平衡值低的表面活性剂可以增强亲脂性药物的包封。此外,囊泡的膜通透性取决于表面活性剂的碳链长度和相变温度。此外,表面活性剂对药代动力学和药效学有明显的影响,如维持药物释放、延长囊泡的循环时间、提高靶向性和细胞摄取。