黄芩素负载磷脂体的制备与表征:体外参数评估

K. Zade, A. Jain
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引用次数: 0

摘要

磷脂体是一种介于天然活性成分和磷脂之间的复合物。此外,磷脂体被应用于许多流行的草药提取物或活性分子中,以增加口服溶出度。因此,在目前的研究中,口服黄芩素是一种黄酮类化合物,吸收不良,溶出度不佳。采用反相蒸发法制备包封黄芩素的磷脂小体(1:1 Mm),并进行冷冻干燥。透射电子显微镜(TEM)分析显示,磷脂质体的形状接近球形,粒径小于100 nm。粉末x射线衍射(PXRD)和差示扫描量热法(DSC)表明,黄芩苷负载的磷脂质体是无定形的。治疗部分的非晶化导致溶解的改善。综上所述,表没食子儿茶素负载的磷脂小体显示出有希望的结果,并且需要在一系列严格的参数下进行进一步的体外和体内研究,以转化为临床可行的产品。
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Preparation and characterization of baicalein loaded phytosomes: Assessment of in vitro parameters
Phytosome is a complex between natural active ingredient and a phospholipid. Further, phytosomes been applied to many popular herbal extracts or active molecules for augmenting oral dissolution. Therefore, in present investigation, orally administered Baicalein, atype of flavanoids, is poorly absorbed, and shows suboptimal dissolution. The phytosomes encapsulating baicalein (1:1 Mm) were prepared by reverse phase evaporation method followed by lyophilization. Transmission electron microscopy (TEM) analysis revealed that phytosomes were almost spherical in shape with particle size below 100 nm. The Powder ex-ray diffraction (PXRD) and differential scanning calorimetry (DSC) demonstrated that Baicalein loaded phytosomes were amorphous in nature. Amorphization of therapeutic moiety leads to improvement in dissolution. In conclusion, epigallocatechin loaded phytosomes exhibited promising results and warrant further in vitro andin vivo investigations under a set of stringent parameters for transforming in to a clinically viable products.
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