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柠檬酸铁脂质体的释放动力学和降解热力学研究。

Study of release kinetics and degradation thermodynamics of ferric citrate liposomes.

机构信息

College of Chemistry and Material Science, Hebei Normal University, Shijiazhuang, 050024, China.

College of Chemistry and Material Science, Hebei Normal University, Shijiazhuang, 050024, China.

出版信息

Chem Phys Lipids. 2019 Dec;225:104811. doi: 10.1016/j.chemphyslip.2019.104811. Epub 2019 Aug 23.

Abstract

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.

摘要

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。

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