College of Chemistry and Material Science, Hebei Normal University, Shijiazhuang, 050024, China.
College of Chemistry and Material Science, Hebei Normal University, Shijiazhuang, 050024, China.
Chem Phys Lipids. 2019 Dec;225:104811. doi: 10.1016/j.chemphyslip.2019.104811. Epub 2019 Aug 23.
Ferric citrate liposome (FAC-Lip) with good sustained-released property was prepared by the rotary-evaporated film-ultrasonic method, and characterized by TEM, DLS, zeta potential and encapsulation efficiency (EE%). The effects of membrane material ratios (m: m = 8:1, 10:1 and 12:1) and drug lipid ratios (m: m = 1:4, 1:6.5 and 1:8) on the release of FAC-Lip were examined. The in vitro release kinetic models and mechanisms of FAC-Lip in artificial gastric juice (SGF) and artificial intestinal juice (SIF) compared with free-FAC were determined. The thermal degradation in PBS was also determined. The results showed that FAC-Lip with membrane material ratio (10:1) and drug lipid ratio (1:6.5) had the optimal sustained-released property, unilamellar vesicles with uniform size (178 ± 2.12 nm), negative charge (-56 ± 3.51 mV) and high encapsulation efficiency (72.77 ± 0.42%). The in vitro release kinetic models of FAC-Lip were two-phase kinetics model and the release mechanisms were non-Fick diffusion both in SGF and SIF. The thermal degradation of FAC-Lip was an endothermic and spontaneous reaction. The results may be helpful in optimizing drug-liposome design, application in food and medicine industries, and furthermore, predicting and guiding medication in vivo.
采用旋转蒸发薄膜-超声法制备了具有良好缓释性能的柠檬酸铁脂质体（FAC-Lip），并通过 TEM、DLS、zeta 电位和包封效率（EE%）进行了表征。考察了膜材比（m:m=8:1、10:1 和 12:1）和载药脂质比（m:m=1:4、1:6.5 和 1:8）对 FAC-Lip 释放的影响。比较了游离-FAC 的体外释放动力学模型和机制。还测定了在 PBS 中的热降解情况。结果表明，膜材比（10:1）和载药脂质比（1:6.5）的 FAC-Lip 具有最佳的缓释性能，具有均匀大小（178±2.12nm）、带负电荷（-56±3.51mV）和高包封效率（72.77±0.42%）的单层囊泡。FAC-Lip 的体外释放动力学模型为两相动力学模型，在 SGF 和 SIF 中的释放机制均为非菲克扩散。FAC-Lip 的热降解是一个吸热和自发的反应。结果可能有助于优化药物脂质体的设计、在食品和医药行业的应用，以及预测和指导体内用药。
