Preparation and evaluation of proliposomes formulation for enhancing the oral bioavailability of ginsenosides

IF 6.8 2区 医学 Q1 CHEMISTRY, MEDICINAL
Duy-Thuc Nguyen , Min-Hwan Kim , Min-Jun Baek , Nae-Won Kang , Dae-Duk Kim
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引用次数: 0

Abstract

Background

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.

Methods

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.

Results

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.

Conclusion

The developed PLs formulation could be a favorable delivery system to improve the oral bioavailability of ginsenosides, including Rg3.

Abstract Image

Abstract Image

制备和评估用于提高人参皂苷口服生物利用度的脂质体制剂
背景本研究的主要目的是以人参皂苷 Rg3(Rg3)为标记物,评估一种能提高人参皂苷口服生物利用度的脂质体(PLs)制剂。将大豆磷脂酰胆碱、富含 Rg3 的提取物、poloxamer 188(Lutrol® F 68)和山梨醇混合并用乙醇水溶液溶解,然后去除乙醇并冻干。通过粉末 X 射线衍射仪(PXRD)、透射电子显微镜(TEM)和体外释放法对 Rg3-PLs 制剂进行了表征。结果 Rg3-PLs 的 X 射线衍射表明,在制备过程中,Rg3 由晶体转变为无定形形式。在水中用手轻轻振荡重组后,Rg3包囊脂质体呈囊泡状,其平均直径约为350 nm,zeta电位为负(-28.6 mV),包封效率高(97.3%)。体外释放研究结果表明,与富含 Rg3 的提取物悬浮液(对照组)相比,PLs 制剂释放的 Rg3 量明显更多。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。
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来源期刊
Journal of Ginseng Research
Journal of Ginseng Research CHEMISTRY, MEDICINAL-INTEGRATIVE & COMPLEMENTARY MEDICINE
CiteScore
11.40
自引率
9.50%
发文量
111
审稿时长
6-12 weeks
期刊介绍: Journal of Ginseng Research (JGR) is an official, open access journal of the Korean Society of Ginseng and is the only international journal publishing scholarly reports on ginseng research in the world. The journal is a bimonthly peer-reviewed publication featuring high-quality studies related to basic, pre-clinical, and clinical researches on ginseng to reflect recent progresses in ginseng research. JGR publishes papers, either experimental or theoretical, that advance our understanding of ginseng science, including plant sciences, biology, chemistry, pharmacology, toxicology, pharmacokinetics, veterinary medicine, biochemistry, manufacture, and clinical study of ginseng since 1976. It also includes the new paradigm of integrative research, covering alternative medicinal approaches. Article types considered for publication include review articles, original research articles, and brief reports. JGR helps researchers to understand mechanisms for traditional efficacy of ginseng and to put their clinical evidence together. It provides balanced information on basic science and clinical applications to researchers, manufacturers, practitioners, teachers, scholars, and medical doctors.
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