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首页> 外文OA文献 >Effect of liquid crystals with cyclodextrin on the bioavailability of a poorly water-soluble compound, diosgenin, after its oral administration to rats
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Effect of liquid crystals with cyclodextrin on the bioavailability of a poorly water-soluble compound, diosgenin, after its oral administration to rats

机译：液晶与环糊精对水溶性化合物，稻蛋白的生物利用度，其口服给予大鼠

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摘要

Diosgenin, found in wild yam (Dioscorea villosa), has been shown to ameliorate diabetes and hyperlipidemia, increase cell proliferation in a human 3D skin model, and inhibits melanin production in B16 melanoma cells. It is also an active element in cosmeceutical and dietary supplements. Although the bioavailability of diosgenin is low due to its poor solubility and intestinal permeability, it was subsequently improved using a β-cyclodextrin (β-CD) inclusion complex. Recently liquid crystals (LCs) were shown to enhance the bioavailability of poorly water-soluble drugs. The purpose in the present study was to prepare diosgenin LCs and investigate the interaction between LC and β-CD in order to improve its bioavailability of diosgenin. Crystallinity and particle diameters of LCs in water were determined by small angle X-ray scattering (SAXS) and Zetasizer. Pharmacokinetic parameters were calculated using the plasma content of diosgenin after its oral administration to Wistar rats. Regarding the formation of glyceryl monooleate (GMO) and phytantriol (PHY) LC, SAXS patterns showed the hexagonal and cubic phases, respectively. Bioavailability was significantly enhanced after oral administration of LCs prepared by GMO than after diosgenin alone. The bioavailability was further improved with the combination of LC and β-CD than LC and water.
机译：在野生山药（Dioscorea Villosa）中发现的Diosgenin已被证明是改善糖尿病和高脂血症，增加人3D皮肤模型中的细胞增殖，并抑制B16黑色素瘤细胞中的黑色素产生。它也是在化妆品和膳食补充剂中的活性元素。虽然诸如β-环糊精（β-CD）包合物的溶解度和肠道渗透性的溶解度和肠道渗透性的差，因此Diosgenin的生物利用度低。最近显示液晶（LCS）提高水溶性差的药物的生物利用度。本研究中的目的是制备二氧辛蛋白LCS，并研究LC和β-CD之间的相互作用，以提高其Diosgenin的生物利用度。通过小角度X射线散射（SAXS）和Zetasizer测定水中LCS中的结晶度和粒径。使用对Wistar大鼠的口服施用后，使用Diosgenin的血浆含量计算药代动力学参数。关于甘油单烯烃（GMO）和植物毒醇（PHY）LC的形成，SAXS图案分别显示六边形和立方相。在用基因GMO制备的LCS口服时显着提高生物利用度，而不是单独的二氧素蛋白。通过LC和β-Cd的组合进一步改善了生物利用度，而不是LC和水。

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