Abstract

The aim of this study was to evaluate the oral bioavailability of liposomal vitamin C and non-liposomal vitamin C in healthy, adult, human subjects under fasting conditions through an open label, randomized, single-dose, two-treatment, two-sequence, two-period, two-way crossover, study. The vitamin C loaded liposome was well characterized using transmission electron microscopy (TEM), dynamic light scattering (DLS) and zeta potential measurements for evaluating morphology, particle size and stabilities, respectively. Microscopic image shows the core-type structure that confirms the characteristic pattern of liposome. The encapsulation efficiency (EE%) and the particle size were 65.85 ± 1.84% and below 100 nm, respectively. The results of the clinical studies of liposomal vitamin C by oral delivery to be 1.77 times more bioavailable than non-liposomal vitamin C. The liposomal vitamin C demonstrated higher values of C_max, AUC_0–t and AUC_0-∞ related to non-liposomal vitamin C due to liposomal encapsulation. No adverse events were reported. It could be concluded that liposomal encapsulated ascorbic acid (vitamin C) shows well-organized morphological pattern, uniform particle size and highly efficient, which leads to have enhanced bioavailability.

摘要

本研究的目的是通过开放标签、随机、单剂量、两种治疗、两种序列、两期，双向交叉，学习。使用透射电子显微镜 (TEM)、动态光散射 (DLS) 和 zeta 电位测量分别对加载维生素 C 的脂质体进行了表征，以分别评估形态、粒径和稳定性。显微图像显示了核型结构，证实了脂质体的特征模式。封装效率 (EE%) 和粒径分别为 65.85 ± 1.84% 和 100 nm 以下。口服给药脂质体维生素 C 的临床研究结果为 1。由于脂质体封装，与非脂质体维生素 C 相关的_max、AUC _{0– t}和 AUC _0-∞。没有报告不良事件。可以得出结论，脂质体包裹的抗坏血酸（维生素C）显示出组织良好的形态模式、均匀的粒径和高效的，从而提高了生物利用度。