Increased antitumor efficacy of ginsenoside Rh ₂ via mixed micelles: in vivo and in vitro evaluation

Abstract

The aim of this work is to apply Solutol ® HS15 and TPGS to prepare self-assembled micelles loading with ginsenoside Rh 2 to increase the solubility of ginsenoside Rh 2 , hence, improving the antitumor efficacy. Ginsenoside Rh 2 -mixed micelles (Rh 2 -M) were prepared by thin film dispersion method. The optimal Rh 2 -M was characterized by particle size, morphology, and drug encapsulation efficiency. The enhancement of in vivo anti-tumor efficacy of Rh 2 -M was evaluated by nude mice bearing tumor model. The solubility of Rh 2 in self-assembled micelles was increased approximately 150-folds compared to free Rh 2 . In vitro results demonstrated that the particle size of Rh 2 -M is 74.72 ± 2.63 nm(PDI = 0.147 ± 0.15), and the morphology of Rh 2 -M is spherical or spheroid, and the EE% and LE% are 95.27 ± 1.26% and 7.68 ± 1.34%, respectively. The results of in vitro cell uptake and in vivo imaging showed that Rh 2 -M could not only increase the cell uptake of drugs, but also transport drug to tumor sites, prolonging the retention time. In vitro cytotoxicity and in vivo antitumor results showed that the anti-tumor effect of Rh 2 can be effectively improved by Rh 2 -M. Therefore, Solutol ® HS15 and TPGS could be used to entrapping Rh 2 into micelles, enhancing solubility and antitumor efficacy.

A comprehensive and systemic review of ginseng‐based nanomaterials: Synthesis, targeted delivery, and biomedical applications

“…Ginsenoside Rh2‐mixed micelles also increased the solubility of ginsenoside Rh2 up to 150‐folds compared to free Rh2, hence, improving the antitumor efficacy 99 . Rh2 liposome also prolonged the blood circulation and stabilized the structure of liposomes, while the paclitaxel‐loaded Rh2 liposome realized the efficient tumor growth suppression 118 …”

“…Solutol HS15 and TPGS forming a block copolymer micelle that were applied by thin film dispersion method to prepare self‐assembled micelles loaded with ginsenoside Rh2. The prepared micelles enhanced antitumor efficacy and solubility of Rh2 99 …”

“…The prepared micelles enhanced antitumor efficacy and solubility of Rh2. 99 Liposomes are also considered as the useful carriers for the drug delivery. Methyl ether poly(ethylene glycol)poly(lactide-co-glycolide) (mPEG-PLGA) nanoparticles loaded with Panax notoginsenoside were prepared using a water-in-oil-in-water double emulsion solvent evaporation method.…”

Ginsenosides emerging as both bifunctional drugs and nanocarriers for enhanced antitumor therapies

“…Amphiphilic PEG micelles modified by celastrol and ginsenoside Rh2 (CG-M) have shown a stronger cell uptake ability, apoptosis induction ability and antiproliferation activity to A549 cells, where the internalization of CG-M to A549 cells was 1.8× stronger than that of free Rh2 [ 113 ]. In addition, Solutol® and TPGS have been used to fabricate Rh2-micelles, with an increasing solubility ~ 150-fold greater than that for Rh2, substantially enhancing the antitumor effect [ 112 ].…”

EGFR-Targeted Liposomes Combined with Ginsenoside Rh2 Inhibit Triple-Negative Breast Cancer Growth and Metastasis

“…However, ginsenoside Rh2 and luteolin are less effective and bioavailable than expected because of their poor water solubility and the barrier function of the body. , To solve these problems, nanoparticles have been constructed as a delivery system to carry these active substances. , Currently, liposomes are widely used to deliver active substances because they are more biocompatible and commercially available than other nano-delivery systems. In addition, their core-shell structure allows them to encapsulate multiple substances simultaneously .…”