Polyvinyl Alcohol (PVA)-Based Nanoniosome for Enhanced in vitro Delivery and Anticancer Activity of Thymol

Abstract

There is an unmet need to develop potent therapeutics against cancer with minimal side effects and systemic toxicity. Thymol (TH) is an herbal medicine with anti-cancer properties that has been investigated scientifically. This study shows that TH induces apoptosis in cancerous cell lines such as MCF-7, AGS, and HepG2. Furthermore, this study reveals that TH can be encapsulated in a Polyvinyl alcohol (PVA)-coated niosome (Nio-TH/PVA) to enhance its stability and enable its controlled release as a model drug in the cancerous region. Materials and Methods: TH-loaded niosome (Nio-TH) was fabricated and optimized using Box-Behnken method and the size, polydispersity index (PDI) and entrapment efficiency (EE) were characterized by employing DLS, TEM and SEM, respectively. Additionally, in vitro drug release and kinetic studies were performed. Cytotoxicity, antiproliferative activity, and the mechanism were assessed by MTT assay, quantitative real-time PCR, flow cytometry, cell cycle, caspase activity evaluation, reactive oxygen species investigation, and cell migration assays. Results: This study demonstrated the exceptional stability of Nio-TH/PVA at 4 °C for two months and its pH-dependent release profile. It also showed its high toxicity on cancerous cell lines and high compatibility with HFF cells. It revealed the modulation of Caspase-3/Caspase-9, MMP-2/MMP-9 and Cyclin D/ Cyclin E genes by Nio-TH/PVA on the studied cell lines. It confirmed the induction of apoptosis by Nio-TH/PVA in flow cytometry, caspase activity, ROS level, and DAPI staining assays. It also verified the inhibition of metastasis by Nio-TH/PVA in migration assays. Conclusion: Overall, the results of this study revealed that Nio-TH/PVA may effectively transport hydrophobic drugs to cancer cells with a controlled-release profile to induce apoptosis while exhibiting no detectable side effects due to their biocompatibility with normal cells.

Synthesis and Study Medical Application of Nanocomposites Based on grafted Chitosan /Polyvinyl alcohol

“…Increasing ROS levels and causing damage to the cellular components by intracellular oxidative stress and an increase in glutathione oxidation AgNPs and AuNPs could induce cytotoxicity [39]. Therefore, the anticancer activity of nanocomposites [XI] (AuNPs) showed significant effects at a concentration of 100 μg/mL against the A549 cell line and IC50=16.92 while IC50=82.68 for REF [40], as in Table 7 and Figure7-11.…”

Thymol as a Potential Neuroprotective Agent: Mechanisms, Efficacy, and Future Prospects

“…Thymol (2-isopropyl-5-methylphenol, Figure ), a naturally occurring monocyclic phenolic compound, is the major active component of the essential oils extracted from several thyme species, including Origanum vulgare , Coridothymus capitatus , and Thymus vulgaris . Many studies from in vitro and animal experiments have demonstrated that thymol possesses potent antioxidant, anti-inflammatory, antimicrobial, and immune-regulation functions. , On the basis of these pharmacological properties, thymol has been widely used in the pharmaceutical field for treating various diseases, including, chronic fibrosis, cancer, immune and inflammatory diseases, cardiovascular disease, infectious disease, and metabolic disease. − Recently, some studies showed that thymol exhibited potential therapeutic effects for several neurological diseases, such as Parkinson’s disease, Alzheimer’s disease, neuro-depression, aging-related learning, and memory impairment. − For example, Javed and colleagues reported that oral thymol supplementation (i.e., 50 mg/kg/day for 28 days) could significantly decrease the biomarkers of oxidative stress, inflammatory response in the brain tissues of rats, following to effectively attenuate neurotoxicity and neurodegeneration caused by rotenone, an inducer of Parkinson’s disease . Similarly, Abu-Elfotuh et al found that oral thymol administration at the final dose of 15 mg/kg/day for 5 weeks (i.e., 35 days) could effectively improve neuronal degeneration and behavioral impairments in rats via the inhibition of oxidative stress, apoptotic cell death, and neuroinflammatory response in the brain tissues of rats with Parkinson’s Disease .…”