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Preparation of oridonin-loaded solid lipid nanoparticles and studies on them in vitro and in vivo

机译：冬凌草甲素固体脂质纳米粒的制备及体内外研究

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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 F_(68) 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 percent 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.
机译：Oridonin是一种亲脂性中药，由于其不良的溶解性而使其口服生物利用度非常低。在我们的研究中，使用硬脂酸，大豆卵磷脂和普朗尼克F_（68）形成了冬凌草甲素的固体脂质纳米颗粒（SLN）递送系统。使用低温下的乳液蒸发-固化来制备SLN分散体。通过透射电子显微镜（TEM）检查粒度和形态，并通过电视微电泳仪测量ζ电位。已经根据包封效率研究和优化了工艺和配方变量。进行差示扫描量热法（DSC）和粉末X射线衍射（PXRD）研究以表征药物状态。在磷酸盐缓冲溶液（PBS）（pH 7.4）中进行了体外释放研究。研究了小鼠体内的组织分布和兔的药代动力学，以评估SLNs的组织靶向特性。开发了具有平均尺寸范围为15-35nm和平均ζ电位为-45.07mV的冬凌草甲素的稳定的SLN制剂。前哨淋巴结中夹带了40％以上的冬凌草甲素。 DSC和PXRD分析表明，冬凌草甲素以无定形状态分散在SLN中。分析了该药物的释放模式，发现其遵循了Higuchi方程。体内研究表明，添加冬凌草甲素的SLNs明显增加了肝脏，肺和脾脏中冬凌草甲素的浓度，而其在心脏和肾脏中的分布却减少了。

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