A nanoparticulate drug-delivery system for glaucocalyxin A: formulation, characterization, increased in vitro, and vivo antitumor activity
A nanoparticulate drug-delivery system for glaucocalyxin A: formulation, characterization, increased in vitro, and vivo antitumor activity
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DOI：
10.3109/10717544.2015.1012311
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发表时间：
2016-09-01
期刊：
影响因子：
6
通讯作者：
Wang, Xiangtao
中科院分区：
文献类型：
--
作者：
Han, Meihua;Li, Zhitao;Wang, Xiangtao
蓝萼甲素（GLA）是一种具有多种药理活性的植物化学成分；然而，其溶解性差限制了蓝萼甲素的更广泛应用。在本研究中，采用沉淀 - 超声联合法制备了蓝萼甲素纳米混悬剂，并通过动态光散射（DLS）、透射电子显微镜（TEM）和差示扫描量热法（DSC）对其进行了表征。蓝萼甲素纳米混悬剂呈球形，表面光滑，粒径小至143nm，载药量达到8.95%，蓝萼甲素的最大浓度达到1mg/mL。蓝萼甲素纳米混悬剂的冻干粉为无定形，呈现出双相药物释放模式，即初始的突释和随后的缓释。与游离药物溶液相比，蓝萼甲素纳米混悬剂对HepG2细胞显示出更高的体外抗肿瘤活性（24小时时的半数抑制浓度IC50值为1.793μg/mL对比2.884μg/mL，p<...（此处原文似乎不完整）
Glaucocalyxin A (GLA) is a phytochemical component with multiple pharmacological activities; however, glaucocalyxin A's wider use has been restricted by its poor solubility. In this study, GLA nanosuspensions were prepared with precipitation-combined ultrasonication and were characterized by dynamic light scattering (DLS), transmission electron microscope (TEM), and differential scanning calorimetry (DSC). The GLA nanosuspensions were spherical with a smooth surface and a small size of 143nm, the drug payload achieved 8.95%, and the maximum GLA concentration reached 1mg/mL. The lyophilized powders for the GLA nanosuspensions were amorphous and displayed a biphasic drug release pattern with an initial burst release and a consequent sustained release. In contrast to the free drug solution, GLA nanosuspensions showed higher in vitro antitumor activity against HepG2 cells (IC50 value of 1.793 versus 2.884g/mL at 24h, p