Preparation of oridonin-loaded solid lipid nanoparticles and studies on them in vitro and in vivo
Preparation of oridonin-loaded solid lipid nanoparticles and studies on them in vitro and in vivo
复制标题
冬凌草甲素固体脂质纳米粒的制备及其体内外研究
DOI：
10.1088/0957-4484/17/23/018
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发表时间：
2006-11
期刊：
影响因子：
3.5
通讯作者：
Gao, Lei
中科院分区：
文献类型：
--
作者：
Tan, Tianwei;Zhang, Dianrui;Gao, Lei
冬凌草甲素是一种亲脂性中药，由于其溶解性差，口服生物利用度很低。本研究以硬脂酸、大豆卵磷脂和普朗尼克F68为原料，制备了冬凌草甲素固体脂质纳米粒。采用乳液蒸发-低温固化法制备SLN分散体。通过透射电子显微镜（TEM）检查颗粒的大小和形态，并通过电视微电泳仪测量zeta电位。工艺和配方变量进行了研究和优化的包封率的基础上。进行差示扫描量热法（DSC）和粉末X射线衍射（PXRD）研究以表征药物的状态。在磷酸盐缓冲溶液（PBS）（pH 7.4）中进行体外释放研究。研究了SLN在小鼠体内的组织分布和在家兔体内的药代动力学，以评价SLN的组织靶向性。开发了平均粒径范围为15-35 nm，平均zeta电位为-45.07 mV的稳定的冬凌草甲素SLN制剂。SLN包封率超过40%。DSC和PXRD分析表明，冬凌草甲素以无定形状态分散在SLN中。药物的释放模式进行了分析，发现遵循Higuchi方程。在体研究表明，载药SLNs可明显增加冬凌草甲素在肝、肺、脾中的浓度，但降低其在心、肾中的分布。
Oridonin, a lipophilic Chinese medicine, has very low oral bioavailability due to its poor solubility. Solid lipid nanoparticle (SLN) delivery systems of oridonin have been formed using stearic acid, soybean lecithin and pluronic F68 in our studies to overcome this problem. Emulsion evaporation–solidification at low temperature was used to prepare SLN dispersions. The particle size and morphology were examined by transmission electron microscopy (TEM), and the zeta potential was measured by a television micro-electrophoresis apparatus. Process and formulation variables have been studied and optimized on the basis of entrapment efficiency. Differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies were performed to characterize the state of the drug. In vitro release studies were performed in phosphate-buffer solution (PBS) (pH 7.4). The tissue distribution in mice and the pharmacokinetics in rabbits were studied to evaluate the tissue targeted property of SLNs. Stable SLN formulations of oridonin having a mean size range of 15–35 nm and mean zeta potential −45.07 mV were developed. More than 40% oridonin was entrapped in SLNs. DSC and PXRD analysis showed that oridonin is dispersed in SLNs in an amorphous state. The release pattern of the drug was analysed and found to follow the Higuchi equations. In vivo studies demonstrated that oridonin-loaded SLNs obviously increased the concentration of oridonin in liver, lung and spleen, while its distribution in heart and kidney decreased.
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影响因子：
4.6
作者：
Kim, BD;Na, K;Choi, HK
通讯作者：
Choi, HK
影响因子：
3.8
作者：
OSAWA, K;YASUDA, H;ITOKAWA, H
通讯作者：
ITOKAWA, H
DOI：
10.1016/j.jconrel.2004.02.029
发表时间：
2004-06
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Kerstin Tabatt;C. Kneuer;M. Sameti;C. Olbrich;R. Müller;C. Lehr;U. Bakowsky
通讯作者：
Kerstin Tabatt;C. Kneuer;M. Sameti;C. Olbrich;R. Müller;C. Lehr;U. Bakowsky
影响因子：
5.2
作者：
Sophie S. Chen;Jian Gao;H. Halicka;Xuan Huang;F. Traganos;Z. Darżynkiewicz
通讯作者：
Sophie S. Chen;Jian Gao;H. Halicka;Xuan Huang;F. Traganos;Z. Darżynkiewicz
影响因子：
5.8
作者：
Cavalli, R;Gasco, MR;Saettone, MF
通讯作者：
Saettone, MF