Abstract

Resveratrol (RSV) and the ethanol extract of Angelica gigas Nakai (AGN Ex)-based nanoparticles (NPs) were prepared using the nanocrystal concept. AGN/RSV NPs with 224 nm hydrodynamic size, unimodal size distribution, and negative zeta potential values were developed with the emulsification and solvent evaporation techniques. The crystalline properties of AGN Ex and RSV were transformed during the emulsification and solvent evaporation processes, thus, AGN NPs and AGN/RSV NPs exhibited amorphous states. AGN/RSV NPs held up their initial hydrodynamic size after 24 h of incubation in serum-included media. Sustained release profiles (for 5 days) of decursin (D) and decursinol angelate (DA) (the representative markers of AGN Ex) and RSV were observed at normal physiological pH (pH 7.4). In ovarian cancer (SKOV-3) cells, although AGN/RSV NPs showed a lower cellular entry rate rather than AGN NPs, the cellular accumulated amount of AGN/RSV NPs was similar with that of AGN NPs after 4 h of incubation. The antiproliferation efficiency of AGN/RSV NPs group was significantly higher than the AGN Ex, AGN NPs, and AGN NPs + RSV groups in SKOV-3 cells. AGN/RSV NPs can be one of the promising candidates for therapeutic nanoplatforms against ovarian cancers.

Highlights

  • Many delivery approaches of drug cargos have been tried for cancer therapy [1,2,3,4,5]

  • Almost of NPs seemed to be located in the cytoplasm rather than the nucleus after their endocytosis (Figure 5B). All of these findings indicate that Angelica gigas Nakai (AGN)/RSV NPs can show an equivalent cellular accumulation efficiency and similar intracellular localization compared to AGN NPs

  • The RSV-incorporated AGN NPs were prepared by using emulsification and solvent evaporation methods

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Summary

Introduction

Many delivery approaches of drug cargos have been tried for cancer therapy [1,2,3,4,5]. Nanocarriers have been attracted for the precise delivery of drug cargos to the malignant tumor region via intravenous administration [6,7]. Due to the specialized anatomical structures of tumor tissue (for example, leaky vasculature and immature lymphatic system), the distribution of nanocarriers with certain properties (for example, particle size and surface charge) in tumor tissue may be improved via an enhanced permeability and retention (EPR) effect [8,9]. The EPR effect-related passive tumor targeting strategy has intrinsic limitations. Active tumor targeting strategies (that is, the attachment of targeting ligands onto nanocarriers) have been developed to improve tumor targeting efficiency [10,11,12]

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