PDF(Pubmed)
Abstract：
UNASSIGNED: This research main objective was to evaluate a proliposomes (PLs) formulation for the enhancement of oral bioavailability of ginsenosides, using ginsenoside Rg3 (Rg3) as a marker.
UNASSIGNED: A novel PLs formulation was prepared using a modified evaporation-on-matrix method. Soy phosphatidylcholine, Rg3-enriched extract, poloxamer 188 (Lutrol® F 68) and sorbitol were mixed and dissolved using a aqueous ethanolic solution, followed by the removal of ethanol and lyophilization. The characterization of Rg3-PLs formulations was performed by powder X-ray diffractometry (PXRD), transmission electron microscopy (TEM) and in vitro release. The enhancement of oral bioavailability was investigated and analyzed by non-compartmental parameters after oral administration of the formulations.
UNASSIGNED: PXRD of Rg3-PLs indicated that Rg3 was transformed from crystalline into its amorphous form during the preparation process. The Rg3-encapsulated liposomes with vesicular-shaped morphology were generated after the reconstitution by gentle hand-shaking in water; they had a mean diameter of approximately 350 nm, a negative zeta potential (-28.6 mV) and a high entrapment efficiency (97.3%). The results of the in vitro release study exhibited that significantly more amount of Rg3 was released from the PLs formulation in comparison with that from the suspension of Rg3-enriched extract (control group). The pharmacokinetic parameters after oral administration of PLs formulation in rats showed an approximately 11.8-fold increase in the bioavailability of Rg3, compared to that of the control group.
UNASSIGNED: The developed PLs formulation could be a favorable delivery system to improve the oral bioavailability of ginsenosides, including Rg3.
UNASSIGNED: A novel PLs formulation was prepared using a modified evaporation-on-matrix method. Soy phosphatidylcholine, Rg3-enriched extract, poloxamer 188 (Lutrol® F 68) and sorbitol were mixed and dissolved using a aqueous ethanolic solution, followed by the removal of ethanol and lyophilization. The characterization of Rg3-PLs formulations was performed by powder X-ray diffractometry (PXRD), transmission electron microscopy (TEM) and in vitro release. The enhancement of oral bioavailability was investigated and analyzed by non-compartmental parameters after oral administration of the formulations.
UNASSIGNED: PXRD of Rg3-PLs indicated that Rg3 was transformed from crystalline into its amorphous form during the preparation process. The Rg3-encapsulated liposomes with vesicular-shaped morphology were generated after the reconstitution by gentle hand-shaking in water; they had a mean diameter of approximately 350 nm, a negative zeta potential (-28.6 mV) and a high entrapment efficiency (97.3%). The results of the in vitro release study exhibited that significantly more amount of Rg3 was released from the PLs formulation in comparison with that from the suspension of Rg3-enriched extract (control group). The pharmacokinetic parameters after oral administration of PLs formulation in rats showed an approximately 11.8-fold increase in the bioavailability of Rg3, compared to that of the control group.
UNASSIGNED: The developed PLs formulation could be a favorable delivery system to improve the oral bioavailability of ginsenosides, including Rg3.
摘要：
■这项研究的主要目的是评估前体脂质体（PLs）制剂，以提高人参皂苷的口服生物利用度，以人参皂苷Rg3(Rg3)为标志。
■使用改进的基质蒸发方法制备新型PLs制剂。大豆磷脂酰胆碱,富含Rg3的提取物，将泊洛沙姆188(Lutrol®F68)和山梨糖醇混合并使用乙醇水溶液溶解,然后除去乙醇并冻干。Rg3-PLs制剂的表征通过粉末X射线衍射(PXRD)进行,透射电镜(TEM)和体外释放。通过口服施用制剂后的非房室参数来研究和分析口服生物利用度的增强。
■Rg3-PLs的PXRD表明Rg3在制备过程中从结晶转变为其无定形形式。Rg3包封的脂质体具有囊泡状形态是通过在水中轻轻手摇重建后产生的；它们的平均直径约为350nm，负ζ电位（-28.6mV）和高包封效率（97.3%）。体外释放研究的结果表明，与富含Rg3的提取物的悬浮液（对照组）相比，从PLs制剂中释放的Rg3量明显更多。与对照组相比，大鼠口服PLs制剂后的药代动力学参数显示Rg3的生物利用度增加了约11.8倍。
■开发的PLs制剂可能是改善人参皂苷口服生物利用度的有利递送系统，包括Rg3。
■使用改进的基质蒸发方法制备新型PLs制剂。大豆磷脂酰胆碱,富含Rg3的提取物，将泊洛沙姆188(Lutrol®F68)和山梨糖醇混合并使用乙醇水溶液溶解,然后除去乙醇并冻干。Rg3-PLs制剂的表征通过粉末X射线衍射(PXRD)进行,透射电镜(TEM)和体外释放。通过口服施用制剂后的非房室参数来研究和分析口服生物利用度的增强。
■Rg3-PLs的PXRD表明Rg3在制备过程中从结晶转变为其无定形形式。Rg3包封的脂质体具有囊泡状形态是通过在水中轻轻手摇重建后产生的；它们的平均直径约为350nm，负ζ电位（-28.6mV）和高包封效率（97.3%）。体外释放研究的结果表明，与富含Rg3的提取物的悬浮液（对照组）相比，从PLs制剂中释放的Rg3量明显更多。与对照组相比，大鼠口服PLs制剂后的药代动力学参数显示Rg3的生物利用度增加了约11.8倍。
■开发的PLs制剂可能是改善人参皂苷口服生物利用度的有利递送系统，包括Rg3。
