Synergetic effects of thymoquinone-loaded porous PVPylated Fe3O4nanostructures for efficient pH-dependent drug release and anticancer potential against triple-negative cancer cells
Abstract:Porous iron oxide nanostructures have attracted increasing attention due to their potential biomedical applications as nanocarriers for cancer and many other therapies as well as minimal toxicity.
“…Various TQ-loaded stimuli-responsive NPs with enhanced anticancer potentials have been discussed in the following sections. A TQ-loaded Fe 3 SO 4 NPs surface decorated with ethylene glycol and polyvinylpyrrolidone (PVP) pH-dependently delivered TQ in TNBC cells (MDA-MB-231) [ 201 ]. PVP surface decoration improved water solubility and delivered drugs in the acidic environment, which maximized tumoricidal efficiency.…”
Cancer causes a considerable amount of mortality in the world, while arthritis is an immunological dysregulation with multifactorial pathogenesis including genetic and environmental defects. Both conditions have inflammation as a part of their pathogenesis. Resistance to anticancer and disease-modifying antirheumatic drugs (DMARDs) happens frequently through the generation of energy-dependent transporters, which lead to the expulsion of cellular drug contents. Thymoquinone (TQ) is a bioactive molecule with anticancer as well as anti-inflammatory activities via the downregulation of several chemokines and cytokines. Nevertheless, the pharmacological importance and therapeutic feasibility of thymoquinone are underutilized due to intrinsic pharmacokinetics, including short half-life, inadequate biological stability, poor aqueous solubility, and low bioavailability. Owing to these pharmacokinetic limitations of TQ, nanoformulations have gained remarkable attention in recent years. Therefore, this compilation intends to critically analyze recent advancements in rheumatoid arthritis and cancer delivery of TQ. This literature search revealed that nanocarriers exhibit potential results in achieving targetability, maximizing drug internalization, as well as enhancing the anti-inflammatory and anticancer efficacy of TQ. Additionally, TQ-NPs (thymoquinone nanoparticles) as a therapeutic payload modulated autophagy as well as enhanced the potential of other drugs when given in combination. Moreover, nanoformulations improved pharmacokinetics, drug deposition, using EPR (enhanced permeability and retention) and receptor-mediated delivery, and enhanced anti-inflammatory and anticancer properties. TQ’s potential to reduce metal toxicity, its clinical trials and patents have also been discussed.
“…Various TQ-loaded stimuli-responsive NPs with enhanced anticancer potentials have been discussed in the following sections. A TQ-loaded Fe 3 SO 4 NPs surface decorated with ethylene glycol and polyvinylpyrrolidone (PVP) pH-dependently delivered TQ in TNBC cells (MDA-MB-231) [ 201 ]. PVP surface decoration improved water solubility and delivered drugs in the acidic environment, which maximized tumoricidal efficiency.…”
Cancer causes a considerable amount of mortality in the world, while arthritis is an immunological dysregulation with multifactorial pathogenesis including genetic and environmental defects. Both conditions have inflammation as a part of their pathogenesis. Resistance to anticancer and disease-modifying antirheumatic drugs (DMARDs) happens frequently through the generation of energy-dependent transporters, which lead to the expulsion of cellular drug contents. Thymoquinone (TQ) is a bioactive molecule with anticancer as well as anti-inflammatory activities via the downregulation of several chemokines and cytokines. Nevertheless, the pharmacological importance and therapeutic feasibility of thymoquinone are underutilized due to intrinsic pharmacokinetics, including short half-life, inadequate biological stability, poor aqueous solubility, and low bioavailability. Owing to these pharmacokinetic limitations of TQ, nanoformulations have gained remarkable attention in recent years. Therefore, this compilation intends to critically analyze recent advancements in rheumatoid arthritis and cancer delivery of TQ. This literature search revealed that nanocarriers exhibit potential results in achieving targetability, maximizing drug internalization, as well as enhancing the anti-inflammatory and anticancer efficacy of TQ. Additionally, TQ-NPs (thymoquinone nanoparticles) as a therapeutic payload modulated autophagy as well as enhanced the potential of other drugs when given in combination. Moreover, nanoformulations improved pharmacokinetics, drug deposition, using EPR (enhanced permeability and retention) and receptor-mediated delivery, and enhanced anti-inflammatory and anticancer properties. TQ’s potential to reduce metal toxicity, its clinical trials and patents have also been discussed.
“…100 A paper by Kumar et al studied the effect of herbal anti-cancer agent thymoquinone loaded in Fe3O4 nanoparticles against triple-negative breast cancer (TNBC) cells, and the DAPI observations confirm the cytotoxic behavior when treated with the formulations. 101 Figure 10 DAPI staining determining the number of nuclei of all samples in ( A ) MCF-7, ( B ) AGS, and ( C ) HepG2 cell lines. MCF-7, AGS, and HepG2 cells were plated onto a 24-well plate and exposed to the IC50 concentration of formulations for 48 hrs.…”
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.
“…20 The FTIR spectrum of PVP shows a characteristic absorption band at 1608 cm À1 corresponding to carbonyl (CQO) absorption, which was shifted to the spectra of NPs. 18,21 The O-H bending peak at 1027 cm À1 was in evidence, the infrared intensity of which reduced markedly after TA was coordinated with iron ions, indicating that iron ions were combined with the phenolic hydroxyl of TA. 22 Besides this, the peaks at 1716 cm À1 and 1612 cm À1 correspond to the CQO of the ester and aromatic CQC stretching bonds, respectively (Fig.…”
Section: Synthesis and Characterization Of Npsmentioning
Nanomedicine with immunotherapy will offer the opportunities to target cancer in an effective manner; however, remains challenging. We herein report a photothermal material loaded with immune-adjuvant combined immune checkpoint blockade...
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