Journal of Ginseng Research

The Korean Society of Ginseng (고려인삼학회)
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Preparation and evaluation of proliposomes formulation for enhancing the oral bioavailability of ginsenosides

  • Duy-Thuc Nguyen (College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University) ;
  • Min-Hwan Kim (College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University) ;
  • Min-Jun Baek (College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University) ;
  • Nae-Won Kang (College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University) ;
  • Dae-Duk Kim (College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University)
  • Received : 2023.01.12
  • Accepted : 2024.03.10
  • Published : 2024.07.01
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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 noncompartmental 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.

Keywords

Acknowledgement

This work was supported by the research grant of the Korean Society of Ginseng (2017) and the National Research Foundation of Korea (NRF) grant funded by the Ministry of Science and ICT (No. NRF-2018R1A5A2024425 and NRF-2020R1A2C2099983).

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