Nguyen Duy-Thuc, Kim Min-Hwan, Baek Min-Jun, Kang Nae-Won, Kim Dae-Duk
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Republic of Korea.
Natural Products Research Institute, Seoul National University, Seoul, Republic of Korea.
J Ginseng Res. 2024 Jul;48(4):417-424. doi: 10.1016/j.jgr.2024.03.004. Epub 2024 Mar 21.
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.
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 release. The enhancement of oral bioavailability was investigated and analyzed by non-compartmental parameters after oral administration of the formulations.
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 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.
The developed PLs formulation could be a favorable delivery system to improve the oral bioavailability of ginsenosides, including Rg3.
本研究的主要目的是以人参皂苷Rg3（Rg3）为指标，评估一种用于提高人参皂苷口服生物利用度的前体脂质体（PLs）制剂。
采用改良的基质蒸发法制备了一种新型PLs制剂。将大豆磷脂酰胆碱、富含Rg3的提取物、泊洛沙姆188（聚氧乙烯氢化蓖麻油F 68）和山梨醇用乙醇水溶液混合溶解，然后除去乙醇并冻干。通过粉末X射线衍射（PXRD）、透射电子显微镜（TEM）和释放度对Rg3-PLs制剂进行表征。口服给药后，通过非房室参数研究和分析口服生物利用度的提高情况。
Rg3-PLs的PXRD表明，Rg3在制备过程中从结晶态转变为无定形态。在水中轻轻振摇复溶后，形成了具有囊泡状形态的包封Rg3的脂质体；它们的平均直径约为350nm，ζ电位为负（-28.6mV），包封率高（97.3%）。释放度研究结果表明，与富含Rg3的提取物悬浮液（对照组）相比，PLs制剂释放出的Rg3量显著更多。大鼠口服PLs制剂后的药代动力学参数显示，与对照组相比，Rg3的生物利用度提高了约11.8倍。
所开发的PLs制剂可能是一种有利于提高包括Rg3在内的人参皂苷口服生物利用度的给药系统。
