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Published in Valerio Voliani, Nanomaterials and Neoplasms, 2021
Eun-Kyung Lim, Taekhoon Kim, Soonmyung Paik, Seungjoo Haam, Yong-Min Huh, Kwangyeol Lee
Tyrosine kinases that are responsible for activation of signal transduction cascades can be inhibited by tyrosine kinase inhibitors. These are used as anticancer drugs by competing with ATP [211]. About 15%–20% of patients with early-stage breast cancer have tumors that overexpress or amplify HER2 genes, which is associated with increased proliferation of cancer cells and poor prognosis [390–394]. When HER2 binds to the ligands (preferably forming dimers), the HER2 pathway can initiate the mitogen-activated protein kinase pathway as well as the PI3K/Akt pathway, which in turn activates the nuclear factor kappa B pathway. When growth factors bind to their receptors on the cell surface, the receptors give a signal causing cell division. However, if growth factor receptor inhibitors bind to their receptors, the receptors no longer cause uncontrolled cell proliferation. Trastuzumab (Herceptin) is a HER2-specific mAb and the only approved HER2-targeted drug. Cells targeted with trastuzumab experience cell cycle arrest in the G phase; thus, cell proliferation is reduced by downregulation of HER2/neu [383, 384]. When cancer develops it requires generation of neovasculature for nutrient and oxygen supply. Trastuzumab suppresses angiogenesis, formation of new blood vessels, by both induction of antiangiogenic factors and repression of proangiogenic factors. Cetuximab (Erbitux), an EGFR inhibitor, binds to EGFR and inhibits uncontrolled growth of cancers with EGFR mutations [215, 216, 395–400].
Genotoxicity and in vitro investigation of Gefitinib-loaded polycaprolactone fabricated nanoparticles for anticancer activity against NCI-H460 cell lines
Published in Journal of Experimental Nanoscience, 2022
Gefitinib, a BCS class II drug used to treat non-small cell lung cancer (NSCLC) [1–5]. It works as both an EGFR inhibitor and a tyrosine kinase inhibitor (TKIs) [6]. According to new research, Gefitinib has a lower solubility and a slower onset of action in the gastric environment at pH 4–6. Gefitinib was found to have a log-P value of 4.15, indicating that it has a higher hydrophobic property [7]. Furthermore, hepatic elevations of alanine aminotransferase, anorexia, stomatitis, vomiting, diarrhea, and nausea were reported to occur with the 250 mg marketed Gefitinib tablets, which had only 44% bioavailability [8]. Moreover, despite their lack of understanding of new polymers, the effects of critical attributes and critical process parameters, and the basic criteria for polymeric nanoformulations such as smaller particle sizes, entrapment efficacy percentage, and polydispersity index, modern scientists are turning to polymeric nanotechnological approaches to tackle these issues [9, 10]. As a result, one of the goals of this study is to create a Gefitinib control release formulation that uses a quality by design approach, which could have rapid onset of action, increased drug solubility profile, and better drug entrapment efficacy [11].
The emergence of nanoporous materials in lung cancer therapy
Published in Science and Technology of Advanced Materials, 2022
Deepika Radhakrishnan, Shan Mohanan, Goeun Choi, Jin-Ho Choy, Steffi Tiburcius, Hoang Trung Trinh, Shankar Bolan, Nikki Verrills, Pradeep Tanwar, Ajay Karakoti, Ajayan Vinu
Surface modification of MSNs is used for attaching targeting agents for the targeted delivery of drugs to drug-resistant or mutant lung cancer cells. A typical study targeting EGFR (Epidermal Growth Factor Receptor) mutant lung cancer cells with MSNs has been conducted. The surface of MSN was modified and functionalised with the targeting drug cetuximab (CET), a tyrosine kinase inhibitor specifically targeting the EGFR, and the MSN pores were loaded with DOX and gefitinib for giving a dual therapy (Figure 2C) [179]. The surface of the MSN with a specific surface area of 887.9 m2/g was functionalised with 3-mercaptopropyltriethoxysilane to introduce mercapto group. The MSN was loaded with DOX and gefitinib and was further conjugated with CET by cross-linking of disulfide bonds. The drug release occurred with the cleavage of sulfur bond due to the presence of abundant glutathione enzyme (GSH) within the tumour cells followed by the release of chemo drugs (Figure 2CII, 2CIII). CET capped MSNs in the EGFR resistant PC9 cells showed higher endocytosis than in low EGFR expressed BEAS-2B cell lines, ascertaining the effect of CET functionalisation in improving the endocytosis.
Recapitulate genistein for topical applications including nanotechnology delivery
Published in Inorganic and Nano-Metal Chemistry, 2022
Afroz Jahan, Juber Akhtar, Neha Jaiswal, Asad Ali, Usama Ahmad
Genistein is a strong protein tyrosine kinase inhibitor with excellent topical permeability. Genistein shows radical scavenging action by lowering H2O2 levels in the skin. Genistein constituted polyphenols. It has one H-atom to the oxygen radical, that ensuing less reactive phenoxy radicals. Since daidzein has one fewer OH group than genistein because of which it was expected to have a lower anti-skin oxidation effect.[43] The Pka of daidzein was 7.2, indicating that it has a higher water solubility and lower skin permeability. Because of its lipophilicity, genistein has a longer retention period than daidzein. The log K’ of genistein and daidzein were 0.23 and 0.05, respectively, suggesting that daidzein is more hydrophilic. For genistein and daidzein, the subcutaneous layer functions as a significant barrier, whereas -terpineol and oleic acid act as penetration enhancers. The melting points of genistein, daidzein, and aglycones were 305°, 338°, and 238 °C, respectively, but when they were combined, the melting points decreased, indicating a eutectic effect. Because chemicals in the eutectic state had a high solubility subcutaneously, this helped to enhance skin permeability.