Abstract
6-shogaol is a promising anti-cancer and anti-inflammatory agent. However, the treatment effectiveness of 6-shogaol is limited by poor water solubility, poor oral absorption and rapid metabolism. Herein, 6-shogaol loaded in micelles (SMs) were designed to improve 6-shogaol’s solubility and bioavailability. The micelles of a PEG derivative of linoleic acid (mPEG2k-LA) were prepared by the nanoprecipitation method with a particle size of 76.8 nm, and entrapment of 81.6 %. Intriguingly, SMs showed a slower release in phosphate buffer saline (PBS) (pH = 7.4) compared to free 6-shogaol while its oral bioavailability increased by 3.2–fold in vivo. More importantly, the in vitro cytotoxic effect in HepG2 cells of SMs was significantly higher than free 6-shogaol. Furthermore, SMs could significantly improve the tissue distribution of 6-shogaol, especially liver and brain. Finally, SMs showed a better hepatoprotective effect against carbon tetrachloride (CCl4)-induced hepatic injury in vivo than free 6-shogaol. These results suggest that the novel micelles could potentiate the activities of 6-shogaol in cancer treatment and hepatoprotection.
Highlights
Ginger, the dried rhizome of Zingiber officinale, is a popular spice and seasoning, and a traditional Chinese medicine used to treat many diseases such as nausea, diarrhea and cold [1]
Gingerols, the main chemical components of ginger, have been found responsible for pharmacological effects including analgesic [2], antipyretic [3], cardiotonic [4], hypothermia inducing [5], and cancer prevention [6]. 6-shogaol is one of the shogaols obtained from Gingerols via dehydration during processing and storage. 6-shogaol exhibits significant antioxidant, anti-proliferative and anti-inflammation activity [7]. 6-shogaol is reported to induce cell cycle arrest coupled with autophagy and apoptosis in various cancer cells including hepatocellular carcinoma (HCC) cell, human non-small cell lung cancer A549 cells and human colon adenocarcinoma (HT-29) cells [8,9,10]. 6-shogaol has been previously reported to possess anti-inflammatory effects by downregulating nitric oxide synthase and COX-2 gene expression [11], while reducing the levels of β-glucuronidase and lactate dehydrogenase [12]
Nanotechnology have shown a huge advantage in enhancing the solubility of lipophilic compounds, oral absorption, bioavailability as well as reducing medicinal herb doses and toxicity, thereby improving the target ability and therapeutic effect compared with traditional Chinese herbal preparations [21,22]
Summary
The dried rhizome of Zingiber officinale, is a popular spice and seasoning, and a traditional Chinese medicine used to treat many diseases such as nausea, diarrhea and cold [1]. Nanotechnology (polymer nanoparticles or micelles, liposomes, inorganic nanoparticles and nano-emulsions) have shown a huge advantage in enhancing the solubility of lipophilic compounds, oral absorption, bioavailability as well as reducing medicinal herb doses and toxicity, thereby improving the target ability and therapeutic effect compared with traditional Chinese herbal preparations [21,22]. Micelles have already received a lot of attention due to their unique peculiarities like a hydrophilic outer shell coupled with a hydrophobic inner core These qualities impart on micelles’ water dissolvability, which result in the spontaneous production of micelles with the capability of encapsulating and solubilizing poorly aqueous-soluble drugs [23,24]. Self-assembled micelles could provide several advantages to drug delivery systems because of their high drug loading capacity, low dose of formulation required and long circulation time [25,26]. This study could provide an experimental basis for the further development and application of self-assembly nano drug delivery systems for enhancing the bioactivity of hydrophobic drugs
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