载达卡巴嗪立方液晶的制剂。第三部分。理化性质表征。
Formulation of dacarbazine-loaded cubosomes. Part III. Physicochemical characterization.
机构信息
Laboratory of Future Nanomedicines and Theoretical Chronopharmaceutics, Division of Pharmaceutical Sciences, University of Missouri-Kansas City School of Pharmacy, 2464 Charlotte, Kansas City, Missouri 64108, USA.
出版信息
AAPS PharmSciTech. 2010 Sep;11(3):1243-9. doi: 10.1208/s12249-010-9496-7. Epub 2010 Aug 6.
Abstract
The purpose of this study was to investigate the physicochemical properties of dacarbazine-loaded cubosomes. The drug-loaded cubosome nanocarriers were prepared by a fragmentation method and then freeze dried. They were then characterized for size, morphology, thermal behavior, and crystallography using dynamic light scattering, transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD), respectively. The drug loading and encapsulation efficiency were determined by UV spectrophotometry. The results showed that the prepared dacarbazine-loaded cubosomes had mean diameters ranging from 86 to 106 nm. In addition to the TEM, the characteristic peaks from PXRD data suggested that the freeze-dried nanoformulations were indeed cubic in nature. DSC and PXRD analysis suggested the 0.06 or 0.28% w/w actual drug loaded inside cubosomes was in the amorphous or molecular state. These physicochemical characteristics would affect the nanoformulation shelf-life, efficacy, and safety.
摘要
本研究旨在探究载达卡巴嗪立方相的理化性质。采用碎化法制备载药立方相纳米载体，并经冷冻干燥。采用动态光散射、透射电子显微镜（TEM）、差示扫描量热法（DSC）和粉末 X 射线衍射（PXRD）分别对其粒径、形态、热行为和结晶度进行了表征。采用紫外分光光度法测定载药量和包封率。结果表明，所制备的载达卡巴嗪立方相平均粒径为 86-106nm。除 TEM 外，PXRD 数据的特征峰表明冷冻干燥纳米制剂确实为立方结构。DSC 和 PXRD 分析表明，立方相内实际载药量为 0.06 或 0.28%w/w 的药物呈无定形或分子状态。这些理化特性将影响纳米制剂的货架期、疗效和安全性。
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