Delivery of gefitinib in synergism with thymoquinone <i>via</i> transferrin-conjugated nanoparticle sensitizes gefitinib-resistant non-small cell lung carcinoma to control metastasis and stemness

Upadhyay, Priyanka; Ghosh, Avijit; Basu, Arijita; Pranati, P A; Gupta, P. C. Sen; Das, Shaswati; Sarker, Sushmita; Bhattacharjee, Mousumi; Bhattacharya, Saurav; Ghosh, Swatilekha; Chattopadhyay, Sreya; Adhikary, Arghya

doi:10.1039/d1bm01148k

Cited by 12 publications

(6 citation statements)

References 53 publications

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“…Natural phytochemicals have many outstanding and versatile bioactivities like anticancer or chemo sensitizing effect . Recent advances have witnessed the enhanced anticancer performances by EGFR-TKI combination with epigallocatechin-3-gallate, curcumin, , quercetin, , natural borneol, thymoquinone, resveratrol, artesunate (antimalaria drug), and capsaicin . In a recent study, Ganthala et al found that Erlo plus quercetin showed synergistic inhibition of lung cancer while the other combinations (fisetin, carnosic acid, or luteolin) of Erlo did not .…”

Section: Egfr-tki-based Combinational Cancer Therapymentioning

confidence: 99%

“…To improve the tumor-targeting delivery efficiency, nanoscale DDSs with passive (or enhanced permeability and retention effect; size less than 200 nm) , and active tumor targeting ability were designed. In these DDSs, active targeting moieties include peptides/proteins, − folic acid, , biotin, antibody, hyaluronic acid, , and aptamers, ,,,, which improve cancer cell targeting by their specific interactions with overexpressed receptors of cancer cells. Peng et al developed trastuzumab and mannose functionalized liposomes for dual-targeting HER2 positive NSCLC cells and mannose receptor-overexpressed tumor-associated macrophage M2 .…”

Section: Ddss For Enhanced Egfr-tki Deliverymentioning

confidence: 99%

“…Some small-molecular, nonchemotherapeutic drugs like clyclosporin A, schizandrin A, berbamine, and thymoquinone also exhibit great potency in reversing the resistance to TKIs. Han et al developed a PEG–PLA nanomedicine codelivering cyclosporin A (an immunosuppressant drug) and Gefi for inhibiting Gefi-resistant PC-9-GR tumor, where the anticancer mechanism revealed that STAT3/Bcl-2 inactivation was induced by this combination …”

Section: Reversing Drug Resistance In Cancer Treatmentmentioning

confidence: 99%

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Recent Advances in Boosting EGFR Tyrosine Kinase Inhibitors-Based Cancer Therapy

Pan

et al. 2023

Mol. Pharmaceutics

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Epidermal growth factor receptor (EGFR) plays a key role in signal transduction pathways associated with cell proliferation, growth, and survival. Its overexpression and aberrant activation in malignancy correlate with poor prognosis and short survival. Targeting inhibition of EGFR by small-molecular tyrosine kinase inhibitors (TKIs) is emerging as an important treatment model besides of chemotherapy, greatly reshaping the landscape of cancer therapy. However, they are still challenged by the offtargeted toxicity, relatively limited cancer types, and drug resistance after long-term therapy. In this review, we summarize the recent progress of oral, pulmonary, and injectable drug delivery systems for enhanced and targeting TKI delivery to tumors and reduced side effects. Importantly, EGFR-TKI-based combination therapies not only greatly broaden the applicable cancer types of EGFR-TKI but also significantly improve the anticancer effect. The mechanisms of TKI resistance are summarized, and current strategies to overcome TKI resistance as well as the application of TKI in reversing chemotherapy resistance are discussed. Finally, we provide a perspective on the future research of EGFR-TKI-based cancer therapy.

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Section: Egfr-tki-based Combinational Cancer Therapymentioning

confidence: 99%

Section: Ddss For Enhanced Egfr-tki Deliverymentioning

confidence: 99%

Section: Reversing Drug Resistance In Cancer Treatmentmentioning

confidence: 99%

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Recent Advances in Boosting EGFR Tyrosine Kinase Inhibitors-Based Cancer Therapy

Pan

et al. 2023

Mol. Pharmaceutics

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“…Compared to EGFR-TKIs alone, NPs loaded with EGFR TKI not only reduce systemic toxicity but also improve intracellular delivery and increase bioavailability ( Ahlawat et al, 2022 ). Upadhyay et al demonstrated the efficiency of transferrin-modified PLGA thymoquinone NPs combined with gefitinib (NP-DUAL-3) in treating resistant NSCLC cells for the first time ( Upadhyay et al, 2021 ). The results indicated that NP-DUAL-3 may restore the MET phenomenon, thereby making drug-resistant NSCLC cells re-sensitive to gefitinib.…”

Section: Nanodrug Targeted Epidermal Growth Factor Receptor In Nsclcmentioning

confidence: 99%

Advancement of regulating cellular signaling pathways in NSCLC target therapy via nanodrug

Li,

Huang

et al. 2023

Front. Chem.

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Lung cancer (LC) is one of the leading causes of high cancer-associated mortality worldwide. Non-small cell lung cancer (NSCLC) is the most common type of LC. The mechanisms of NSCLC evolution involve the alterations of multiple complex signaling pathways. Even with advances in biological understanding, early diagnosis, therapy, and mechanisms of drug resistance, many dilemmas still need to face in NSCLC treatments. However, many efforts have been made to explore the pathological changes of tumor cells based on specific molecular signals for drug therapy and targeted delivery. Nano-delivery has great potential in the diagnosis and treatment of tumors. In recent years, many studies have focused on different combinations of drugs and nanoparticles (NPs) to constitute nano-based drug delivery systems (NDDS), which deliver drugs regulating specific molecular signaling pathways in tumor cells, and most of them have positive implications. This review summarized the recent advances of therapeutic targets discovered in signaling pathways in NSCLC as well as the related NDDS, and presented the future prospects and challenges.

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“…Combining TQ nanoparticles with the TKI gefitinib may provide an effective platform for treating non-small cell lung cancer (NSCLC). Nanoparticles containing TQ showed better anti-lung cancer activity and induced therapeutic effects of epithelial-to-mesenchymal transition (EMT) in NSCLC by regulating the STAT3/PTEN/AKT/miR-21 axis [ 41 ]. These studies indicate an important role of TQ in lung cancer treatment.…”

Section: Anti-inflammatory Effects Of Tq In Tumorsmentioning

confidence: 99%

The Role of Thymoquinone in Inflammatory Response in Chronic Diseases

Liu

Huang

Kim

et al. 2022

IJMS

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Anti-inflammatory therapies have been shown to be effective in the prevention of various cardiovascular diseases, tumors, and cancer complications. Thymoquinone (TQ), the main active constituent of Nigella sativa, has shown promising therapeutic properties in many in vivo and in vitro models. However, TQ has poor bioavailability and is hydrophobic, prohibiting clinical trials with TQ alone. Studies have explored the combination of TQ with biological nanomaterials to improve its bioavailability. The TQ nanoparticle formulation shows better bioavailability than free TQ, and these formulations are ready for clinical trials to determine their potential as therapeutic agents. In this paper, we review current knowledge about the interaction between TQ and the inflammatory response and summarize the research prospects in Korea and abroad. We discuss the different biological activities of TQ and various combination therapies of TQ and nanomaterials in clinical trials.

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Delivery of gefitinib in synergism with thymoquinone via transferrin-conjugated nanoparticle sensitizes gefitinib-resistant non-small cell lung carcinoma to control metastasis and stemness

Abstract: Epidermal growth factor receptor (EGFR) normally over-express in non-small cell lung cancer (NSCLC) and its mutations act as oncogenic drivers in the cellular signal transduction pathway and induce downstream activation...

Cited by 12 publications

References 53 publications

Recent Advances in Boosting EGFR Tyrosine Kinase Inhibitors-Based Cancer Therapy

Recent Advances in Boosting EGFR Tyrosine Kinase Inhibitors-Based Cancer Therapy

Advancement of regulating cellular signaling pathways in NSCLC target therapy via nanodrug

The Role of Thymoquinone in Inflammatory Response in Chronic Diseases

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