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Assessment of a New Ginsenoside Rh2 Nanoniosomal Formulation for Enhanced Antitumor Efficacy on Prostate Cancer: An
Hadi Zare-Zardini1,2,3, Ashraf Alemi4, Asghar Taheri-Kafrani5
1Hematology and Oncology Research Center, Shahid Sadoughi University of Medical Sciences, Yazd, Iran.
Introduction:
Ginsenoside Rh2, purified from the Panax ginseng root, has been demonstrated to possess anticancer properties against various cancerous cells including colorectal, breast, skin, ovarian, prostate, and liver cancerous cells. However, the poor bioavailability, low stability on gastrointestinal systems, and fast plasma elimination limit further clinical applications of Ginsenoside Rh2 for cancer treatments. In this study, a novel formulation of niosomal Ginsenoside Rh2 was prepared using the thin film hydration technique.
Methods:
The niosomal formulation contained Span 60 and cholesterol, and cationic lipid DOTAP was evaluated by determining particle size distribution, encapsulation efficiency, the polydispersity index (PDI), and surface morphology. The cytotoxic effects of free Ginsenoside Rh2 and Ginsenoside Rh2-loaded niosomes were determined using the MTT method in the PC3 prostate cancer cell line. For the investigation of the in vitro cellular uptake of Ginsenoside Rh2-loaded niosome, two formulations were prepared: the Ginsenoside Rh2-loaded niosomal formula containing 5% DOTAP and the Ginsenoside Rh2-loaded niosomal formula without DOTAP.
Results:
The mean size, DPI, zeta potential, and encapsulation efficiency of the Ginsenoside Rh2-loaded nanoniosomal formulation containing DOTAP were 93.5±2.1 nm, 0.203±0.01, +4.65±0.65, and 98.32% ±2.4, respectively. The niosomal vesicles were found to be round and have a smooth surface. The release profile of Ginsenoside Rh2 from niosome was biphasic. Furthermore, a two-fold reduction in the Ginsenoside Rh2 concentration was measured when Ginsenoside Rh2 was administered in a nanoniosomal form compared to free Ginsenoside Rh2 solutions in the PC3 prostate cancer cell line. After storage for 90 days, the encapsulation efficiency, vesicle size, PDI, and zeta potential of the optimized formulation did not significantly change compared to the freshly prepared samples. The cellular uptake experiments of the niosomal formulation demonstrated that by adding DOTAP to the niosomal formulation, the cellular uptake was enhanced.
Discussion:
The enhanced cellular uptake and cytotoxic activity of the Ginsenoside Rh2 nanoniosomal formulation on the PC3 cell make it an attractive candidate for application as a nano-sized delivery vehicle to transfer Ginsenoside Rh2 to cancer cells.
Insights
This study developed a novel niosomal formulation of Ginsenoside Rh2, enhancing its delivery and effectiveness against prostate cancer cells. The nanoniosomal Ginsenoside Rh2 showed improved cellular uptake and cytotoxicity, making it a promising cancer treatment candidate.
Area of Science:
- Nanotechnology
- Pharmacology
- Biochemistry
Background:
- Ginsenoside Rh2 from Panax ginseng exhibits anticancer properties against various cancer types.
- Poor bioavailability and stability limit its clinical use.
- A novel niosomal formulation of Ginsenoside Rh2 was developed to overcome these limitations.
Purpose of the Study:
- To formulate and characterize niosomal Ginsenoside Rh2 for improved cancer treatment.
- To evaluate the in vitro cellular uptake and cytotoxic effects of the niosomal formulation.
Main Methods:
- Niosomal Ginsenoside Rh2 prepared using thin film hydration with Span 60, cholesterol, and DOTAP.
- Characterization included particle size, PDI, zeta potential, and encapsulation efficiency.
- Cytotoxicity assessed via MTT assay in PC3 prostate cancer cells; cellular uptake investigated.
Main Results:
- Nanosized vesicles (93.5 nm) with high encapsulation efficiency (98.32%) and positive zeta potential (+4.65 mV) were achieved.
- The formulation demonstrated biphasic release and enhanced cellular uptake, particularly with DOTAP.
- Nanosomal Ginsenoside Rh2 showed a two-fold increase in efficacy against PC3 cells compared to free Ginsenoside Rh2.
Conclusions:
- The developed nanoniosomal Ginsenoside Rh2 formulation is stable and exhibits enhanced cellular uptake and cytotoxicity.
- This formulation represents a promising nano-delivery system for Ginsenoside Rh2 in cancer therapy.
