Browsing by Author "Gupta, Gaurav"
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- ItemAdvances in nanotechnology-based drug delivery in targeting PI3K signaling in respiratory diseases(FUTURE MEDICINE LTD, 2021) Chan, Yinghan; MacLoughlin, Ronan; Zacconi, Flavia C. M.; Tambuwala, Murtaza M.; Pabari, Ritesh M.; Singh, Sachin Kumar; Pinto Andreoli, Terezinha de Jesus; Gupta, Gaurav; Chellappan, Dinesh Kumar; Dua, Kamal
- ItemAlbumin Nano-Encapsulation of Piceatannol Enhances Its Anticancer Potential in Colon Cancer Via Downregulation of Nuclear p65 and HIF-1α(2020) Aljabali, Alaa A. A.; Bakshi, Hamid A.; Hakkim, Faruck L.; Haggag, Yusuf A.; Al-Batanyeh, Khalid M.; Al Zoubi, Mazhar S.; Al-Trad, Bahaa; Nasef, Mohamed M.; Satija, Saurabh; Mehta, Meenu; Pabreja, Kavita; Mishra, Vijay; Khan, Mohammed; Abobaker, Salem; Azzouz, Ibrahim M.; Dureja, Harish; Pabari, Ritesh M.; Dardouri, Ashref Ali K.; Kesharwani, Prashant; Gupta, Gaurav; Shukla, Shakti Dhar; Prasher, Parteek; Charbe, Nitin B.; Negi, Poonam; Kapoor, Deepak N.; Chellappan, Dinesh Kumar; da Silva, Mateus Webba; Thompson, Paul; Dua, Kamal; McCarron, Paul; Tambuwala, Murtaza M.Piceatannol (PIC) is known to have anticancer activity, which has been attributed to its ability to block the proliferation of cancer cells via suppression of the NF-kB signaling pathway. However, its effect on hypoxia-inducible factor (HIF) is not well known in cancer. In this study, PIC was loaded into bovine serum albumin (BSA) by desolvation method as PIC-BSA nanoparticles (NPs). These PIC-BSA nanoparticles were assessed for in vitro cytotoxicity, migration, invasion, and colony formation studies and levels of p65 and HIF-1 alpha. Our results indicate that PIC-BSA NPs were more effective in downregulating the expression of nuclear p65 and HIF-1 alpha in colon cancer cells as compared to free PIC. We also observed a significant reduction in inflammation induced by chemical colitis in mice by PIC-BSA NPs. Furthermore, a significant reduction in tumor size and number of colon tumors was also observed in the murine model of colitis-associated colorectal cancer, when treated with PIC-BSA NPs as compared to free PIC. The overall results indicate that PIC, when formulated as PIC-BSA NPs, enhances its therapeutic potential. Our work could prompt further research in using natural anticancer agents as nanoparticels with possible human clinical trails. This could lead to the development of a new line of safe and effective therapeutics for cancer patients.
- ItemAn overview of vaccine development for COVID-19(2021) Shahcheraghi, Seyed H.; Ayatollahi, Jamshid; Aljabali, Alaa A. A.; Shastri, Madhur D.; Shukla, Shakti D.; Chellappan, Dinesh K.; Jha, Niraj K.; Anand, Krishnan; Katari, Naresh K.; Mehta, Meenu; Satija, Saurabh; Dureja, Harish; Mishra, Vijay; Almutary, Abdulmajeed G.; Alnuqaydan, Abdullah M.; Charbe, Nitin; Prasher, Parteek; Gupta, Gaurav; Dua, Kamal; Lotfi, Marzieh; Bakshi, Hamid A.; Tambuwala, Murtaza M.The COVID-19 pandemic continues to endanger world health and the economy. The causative SARS-CoV-2 coronavirus has a unique replication system. The end point of the COVID-19 pandemic is either herd immunity or widespread availability of an effective vaccine. Multiple candidate vaccines - peptide, virus-like particle, viral vectors (replicating and nonreplicating), nucleic acids (DNA or RNA), live attenuated virus, recombinant designed proteins and inactivated virus - are presently under various stages of expansion, and a small number of vaccine candidates have progressed into clinical phases. At the time of writing, three major pharmaceutical companies, namely Pfizer and Moderna, have their vaccines under mass production and administered to the public. This review aims to investigate the most critical vaccines developed for COVID-19 to date.
- ItemBiomedical Applications of polymeric micelles in the treatment of diabetes mellitus: Current success and future approaches(2022) Kaur, Jaskiran; Gulati, Monica; Zacconi, Flavia C. M.; Dureja, Harish; Loebenberg, Raimar; Ansari, Md Salahuddin; AlOmeir, Othman; Alam, Aftab; Chellappan, Dinesh Kumar; Gupta, Gaurav; Jha, Niraj Kumar; Pinto, Terezinha de Jesus Andreoli; Morris, Andrew; Choonara, Yahya E.; Adams, Jon; Dua, Kamal; Singh, Sachin KumarIntroduction Diabetes mellitus (DM) is the most common metabolic disease and multifactorial, harming patients worldwide. Extensive research has been carried out in the search for novel drug delivery systems offering reliable control of glucose levels for diabetics, aiming at efficient management of DM. Areas covered Polymeric micelles (PMs) as smart drug delivery nanocarriers are discussed, focusing on oral drug delivery applications for the management of hyperglycemia. The most recent approaches used for the preparation of smart PMs employ molecular features of amphiphilic block copolymers (ABCs), such as stimulus sensitivity, ligand conjugation, and as a more specific example the ability to inhibit islet amyloidosis. Expert opinion PMs provide a unique platform for self-regulated or spatiotemporal drug delivery, mimicking the working mode of pancreatic islets to maintain glucose homeostasis for prolonged periods. This unique characteristic is achieved by tailoring the functional chemistry of ABCs considering the physicochemical traits of PMs, including sensing capabilities, hydrophobicity, etc. In addition, the application of ABCs for the inhibition of conformational changes in islet amyloid polypeptide garnered attention as one of the root causes of DM. However, research in this field is limited and further studies at the clinical level are required.
- ItemDevelopment of mushroom polysaccharide and probiotics based solid self-nanoemulsifying drug delivery system loaded with curcumin and quercetin to improve their dissolution rate and permeability: State of the art(ELSEVIER, 2021) Khursheed, Rubiya; Singh, Sachin Kumar; Wadhwa, Sheetu; Gulati, Monica; Kapoor, Bhupinder; Jain, Subheet Kumar; Gowthamarajan, Kuppusamy; Zacconi, Flavia C. M.; Chellappan, Dinesh Kumar; Gupta, Gaurav; Jha, Niraj Kumar; Gupta, Piyush Kumar; Dua, KamalThe role of mushroom polysaccharides and probiotics as pharmaceutical excipients for development of nano-carriers has never been explored. In the present study an attempt has been made to explore Ganoderma lucidum extract powder (GLEP) containing polysaccharides and probiotics to convert liquid self nanoemulsifying drug delivery system (SNEDDS) into solid free flowing powder. Two lipophilic drugs, curcumin and quercetin were used in this study due to their dissolution rate limited oral bioavailability and poor permeability. These were loaded into liquid SNEDDS by dissolving them into isotropic mixture of Labrafill M1944CS, Capmul MCM, Tween-80 and Transcutol P. The liquid SNEDDS were solidified using probiotics and mushroom polysaccharides as carriers and Aerosil-200 as coating agent. The solidification was carried out using spray drying process. The process and formulation variables for spray drying process of liquid SNEDDS were optimized using Box Behnken Design to attain required powder properties. The release of both drugs from the optimized spray dried (SD) formulation was found to be more than 90%, whereas, it was less than 20% for unprocessed drugs. The results of DSC, PXRD and SEM, showed that the developed L-SNEDDS preconcentrate was successfully loaded onto the porous surface of probiotics, mushroom polysaccharides and Aerosil-200.
- ItemDietary Crocin is Protective in Pancreatic Cancer while Reducing Radiation-Induced Hepatic Oxidative Damage(2020) Bakshi, Hamid A.; Al Zoubi, Mazhar S.; Faruck, Hakkim L.; Aljabali, Alaa A. A.; Rabi, Firas A.; Hafiz, Amin A.; Al-Batanyeh, Khalid M.; Al-Trad, Bahaa; Ansari, Prawej; Nasef, Mohamed M.; Charbe, Nitin B.; Satija, Saurabh; Mehta, Meenu; Mishra, Vijay; Gupta, Gaurav; Abobaker, Salem; Negi, Poonam; Azzouz, Ibrahim M.; Dardouri, Ashref Ali K.; Dureja, Harish; Prasher, Parteek; Chellappan, Dinesh K.; Dua, Kamal; Da Silva, Mateus Webba; El Tanani, Mohamed; McCarron, Paul A.; Tambuwala, Murtaza M.Pancreatic cancer is one of the fatal causes of global cancer-related deaths. Although surgery and chemotherapy are standard treatment options, post-treatment outcomes often end in a poor prognosis. In the present study, we investigated anti-pancreatic cancer and amelioration of radiation-induced oxidative damage by crocin. Crocin is a carotenoid isolated from the dietary herb saffron, a prospect for novel leads as an anti-cancer agent. Crocin significantly reduced cell viability of BXPC3 and Capan-2 by triggering caspase signaling via the downregulation of Bcl-2. It modulated the expression of cell cycle signaling proteins P53, P21, P27, CDK2, c-MYC, Cyt-c and P38. Concomitantly, crocin treatment-induced apoptosis by inducing the release of cytochrome c from mitochondria to cytosol. Microarray analysis of the expression signature of genes induced by crocin showed a substantial number of genes involved in cell signaling pathways and checkpoints (723) are significantly affected by crocin. In mice bearing pancreatic tumors, crocin significantly reduced tumor burden without a change in body weight. Additionally, it showed significant protection against radiation-induced hepatic oxidative damage, reduced the levels of hepatic toxicity and preserved liver morphology. These findings indicate that crocin has a potential role in the treatment, prevention and management of pancreatic cancer.
- ItemHypoxia-Inducible Factor (HIF): Fuel for Cancer Progression(Bentham Science Publ. LTD, 2021) Satija, Saurabh; Kaur, Harpreet; Tambuwala, Murtaza M.; Sharma, Prabal; Vyas, Manish; Khurana, Navneet; Sharma, Neha; Bakshi, Hamid A.; Charbe, Nitin B.; Zacconi, Flavia C. M.; Aljabali, Alaa A.; Nammi, Srinivas; Dureja, Harish; Singh, Thakur G.; Gupta, Gaurav; Dhanjal, Daljeet S.; Dua, Kamal; Chellappan, Dinesh K.; Mehta, MeenuHypoxia is an integral part of the tumor microenvironment, caused primarily due to rapidly multiplying tumor cells and a lack of proper blood supply. Among the major hypoxic pathways, HIF-1 transcription factor activation is one of the widely investigated pathways in the hypoxic tumor microenvironment (TME). HIF-1 is known to activate several adaptive reactions in response to oxygen deficiency in tumor cells. HIF-1 has two subunits, HIF-1 beta (constitutive) and HIF-1 alpha (inducible). The HIF-1 alpha expression is largely regulated via various cytokines (through PI3K-ACT-mTOR signals), which involves the cascading of several growth factors and oncogenic cascades. These events lead to the loss of cellular tumor suppressant activity through changes in the level of oxygen via oxygen-dependent and oxygen-independent pathways. The significant and crucial role of HIF in cancer progression and its underlying mechanisms have gained much attention lately among the translational researchers in the fields of cancer and biological sciences, which have enabled them to correlate these mechanisms with various other disease modalities. In the present review, we have summarized the key findings related to the role of HIF in the progression of tumors.
- ItemLuteolin: a favonoid with a multifaceted anticancer potential(2022) Prasher, Parteek; Sharma, Mousmee; Singh, Sachin K.; Gulati, Monica; Chellappan, Dinesh K.; Zacconi, Flavia C. M.; De Rubis, Gabriele; Gupta, Gaurav; Sharifi-Rad, Javad; Cho, William C.; Dua, KamalTherapeutic effect of phytochemicals has been emphasized in the traditional medicine owing to the presence of bioactive molecules, such as polyphenols. Luteolin is a flavone belonging to the flavonoid class of polyphenolic phytochemicals with healing effect on hypertension, inflammatory disorders, and cancer due to its action as pro-oxidants and antioxidants. The anticancer profile of luteolin is of interest due to the toxic effect of contemporary chemotherapy paradigm, leading to the pressing need for the development and identification of physiologically benevolent anticancer agents and molecules. Luteolin exerts anticancer activity by downregulation of key regulatory pathways associated with oncogenesis, in addition to the induction of oxidative stress, cell cycle arrest, upregulation of apoptotic genes, and inhibition of cell proliferation and angiogenesis in cancer cells. In this review, we discuss about the anticancer profile of luteolin.
- ItemProbing 3CL protease: Rationally designed chemical moieties for COVID-19(2020) Sharma, Mousmee; Prasher, Parteek; Mehta, Meenu; Zacconi, Flavia C.; Singh, Yogendra; Kapoor, Deepak N.; Dureja, Harish; Pardhi, Dinesh M.; Tambuwala, Murtaza M.; Gupta, Gaurav; Chellappan, Dinesh K.; Dua, Kamal; Satija, Saurabh
- ItemProtein and peptide delivery to lungs by using advanced targeted drug delivery(2022) Chellappan, Dinesh Kumar; Prasher, Parteek; Saravanan, Vilashini; Yee, Vanessa See Vern; Chi, Wendy Chai Wen; Wong, Jia Wei; Wong, Joon Kang; Wong, Jing Tong; Wan, Wai; Chellian, Jestin; Molugulu, Nagashekhara; Prabu, Sakthivel Lakshmana; Ibrahim, Rania; Darmarajan, Thiviya; Candasamy, Mayuren; Singh, Pankaj Kumar; Mishra, Vijay; Shastri, Madhur D.; Zacconi, Flavia C. M.; Chakraborty, Amlan; Mehta, Meenu; Gupta, Piyush Kumar; Dureja, Harish; Gulati, Monica; Singh, Sachin Kumar; Gupta, Gaurav; Jha, Niraj Kumar; Oliver, Brian Gregory George; Dua, KamalThe challenges and difficulties associated with conventional drug delivery systems have led to the emergence of novel, advanced targeted drug delivery systems. Therapeutic drug delivery of proteins and peptides to the lungs is complicated owing to the large size and polar characteristics of the latter. Nevertheless, the pulmonary route has attracted great interest today among formulation scientists, as it has evolved into one of the important targeted drug delivery platforms for the delivery of peptides, and related compounds effectively to the lungs, primarily for the management and treatment of chronic lung diseases. In this review, we have discussed and summarized the current scenario and recent developments in targeted delivery of proteins and peptide-based drugs to the lungs. Moreover, we have also highlighted the advantages of pulmonary drug delivery over conventional drug delivery approaches for peptide-based drugs, in terms of efficacy, retention time and other important pharmacokinetic parameters. The review also highlights the future perspectives and the impact of targeted drug delivery on peptide-based drugs in the coming decade.
- ItemSmall interfering RNA for cancer treatment: overcoming hurdles in delivery(2020) Zacconi, Flavia C. M.; Aljabali, Alaa A.A.; Chellappan, D.K.; Shrivastava, Garima; Gupta, Gaurav; Bakshi, Hamid A.; Dua, Kamal; Metha, Meenu; Tambuwala, Murtaza M.; Amnerkar, Nikhil D.; Charbe, Nitin Bharat; Negi, Poonam; Satheeshkumar, Rajendran; Khadse, Saurabh C.; Satija, SaurabhIn many ways, cancer cells are different from healthy cells. A lot of tactical nano-based drug delivery systems are based on the difference between cancer and healthy cells. Currently, nanotechnology-based delivery systems are the most promising tool to deliver DNA-based products to cancer cells. This review aims to highlight the latest development in the lipids and polymeric nanocarrier for siRNA delivery to the cancer cells. It also provides the necessary information about siRNA development and its mechanism of action. Overall, this review gives us a clear picture of lipid and polymer-based drug delivery systems, which in the future could form the base to translate the basic siRNA biology into siRNA-based cancer therapies. (C) 2020 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
- ItemTargeting LIN28: a new hope in prostate cancer theranostics(2021) Shrivastava, Garima; Aljabali, Alaa A. A.; Shahcheraghi, Seyed Hossein; Lotfi, Marzieh; Shastri, Madhur D.; Shukla, Shakti D.; Chellappan, Dinesh K.; Jha, Niraj Kumar; Anand, Krishnan; Dureja, Harish; Pabari, Ritesh M.; Mishra, Vijay; Almutary, Abdulmajeed G.; Alnuqaydan, Abdullah M.; Charbe, Nitin; Prasher, Parteek; Negi, Poonam; Goyal, Rohit; Dua, Kamal; Gupta, Gaurav; Serrano-Aroca, Angel; Bahar, Bojlul; Barh, Debmalya; Panda, Pritam Kumar; Takayama, Kazuo; Lundstorm, Kenneth; McCarron, Paul; Bakshi, Hamid; Tambuwala, Murtaza M.The mortality and morbidity rates for prostate cancer have recently increased to alarming levels, rising higher than lung cancer. Due to a lack of drug targets and molecular probes, existing theranostic techniques are limited. Human LIN28A and its paralog LIN28B overexpression are associated with a number of tumors resulting in a remarkable increase in cancer aggression and poor prognoses. The current review aims to highlight recent work identifying the key roles of LIN28A and LIN28B in prostate cancer, and to instigate further preclinical and clinical research in this important area.
- ItemTargeting mucus barrier in respiratory diseases by chemically modified advanced delivery systems(ELSEVIER IRELAND LTD, 2022) Prasher, Parteek; Sharma, Mousmee; Singh, Sachin Kumar; Gulati, Monica; Jha, Niraj Kumar; Gupta, Piyush Kumar; Gupta, Gaurav; Chellappan, Dinesh Kumar; Zacconi, Flavia C. M.; Pinto, Terezinha de Jesus Andreoli; Chan, Yinghan; Liu, Gang; Paudel, Keshav Raj; Hansbro, Philip M.; Oliver, Brian Gregory George; Dua, KamalMucus gel constitutes of heavily cross-linked mucin fibers forming a viscoelastic, dense porous network that coats all the exposed epithelia not covered with the skin. The layer provides protection to the underlying gastrointestinal, respiratory, and female reproductive tracts, in addition to the organs such as the surface of eye by trapping the pathogens, irritants, environmental fine particles, and potentially hazardous foreign matter. However, this property of mucus gel poses a substantial challenge for realizing the localized and sustained drug delivery across the mucosal surfaces. The mucus permeating particles that spare the protective properties of mucus gel improve the therapeutic potency of the drugs aimed at the management of diseases, including sexually transmitted infections, lung cancer, irritable bowel disease, degenerative eye diseases and infections, and cystic fibrosis. As such, the mucoadhesive materials conjugated with drug molecules display a prolonged retention time in the mucosal gel that imparts a sustained release of the deliberated drug molecules across the mucosa. The contemporarily developed mucus penetrating materials for drug delivery applications comprise of a finer size, appreciable hydrophilicity, and a neutral surface to escape the entrapment within the cross-inked mucus fibers. Pertaining to the mucus secretion as a first line of defence in respiratory tract in response to the invading physical, chemical, and biological pathogens, the development of mucus penetrating materials hold promise as a stalwart approach for revolutionizing the respiratory drug delivery paradigm. The present review provides an epigrammatic collation of the mucus penetrating/mucoadhesive materials for achieving a controlled/sustained release of the cargo pharmaceutics and drug molecules across the respiratory mucus barrier.
- ItemVitamin D-A prominent immunomodulator to prevent COVID-19 infection(WILEY, 2023) Ashique, Sumel; Gupta, Kirti; Gupta, Gaurav; Mishra, Neeraj; Singh, Sachin Kumar; Wadhwa, Sheetu; Gulati, Monica; Dureja, Harish; Zacconi, Flavia C. M.; Oliver, Brian G.; Paudel, Keshav Raj; Hansbro, Philip M.; Chellappan, Dinesh Kumar; Dua, KamalCOVID-19 remains a life-threatening infectious disease worldwide. Several bio-active agents have been tested and evaluated in an effort to contain this disease. Unfortunately, none of the therapies have been successful, owing to their safety concerns and the presence of various adverse effects. Various countries have developed vaccines as a preventive measure; however, they have not been widely accepted as effective strategies. The virus has proven to be exceedingly contagious and lethal, so finding an effective treatment strategy has been a top priority in medical research. The significance of vitamin D in influencing many components of the innate and adaptive immune systems is examined in this study. This review aims to summarize the research on the use of vitamin D for COVID-19 treatment and prevention. Vitamin D supplementation has now become an efficient option to boost the immune response for all ages in preventing the spread of infection. Vitamin D is an immunomodulator that treats infected lung tissue by improving innate and adaptive immune responses and downregulating the inflammatory cascades. The preventive action exerted by vitamin D supplementation (at a specific dose) has been accepted by several observational research investigations and clinical trials on the avoidance of viral and acute respiratory dysfunctions. To assess the existing consensus about vitamin D supplementation as a strategy to treat and prevent the development and progression of COVID-19 disease, this review intends to synthesize the evidence around vitamin D in relation to COVID-19 infection.
- ItemZerumbone liquid crystalline nanoparticles protect against oxidative stress, inflammation and senescence induced by cigarette smoke extract in vitro(2024) Paudel, Keshav Raj; Clarence, Dvya Delilaa; Panth, Nisha; Manandhar, Bikash; De Rubis, Gabriele; Devkota, Hari Prasad; Gupta, Gaurav; Zacconi, Flavia C.; Williams, Kylie A.; Pont, Lisa G.; Singh, Sachin Kumar; Warkiani, Majid Ebrahimi; Adams, Jon; Macloughlin, Ronan; Oliver, Brian G.; Chellappan, Dinesh Kumar; Hansbro, Philip Michael; Dua, KamalThe purpose of this study was to evaluate the potential of zerumbone-loaded liquid crystalline nanoparticles (ZER-LCNs) in the protection of broncho-epithelial cells and alveolar macrophages against oxidative stress, inflammation and senescence induced by cigarette smoke extract in vitro. The effect of the treatment of ZER-LCNs on in vitro cell models of cigarette smoke extract (CSE)-treated mouse RAW264.7 and human BCi-NS1.1 basal epithelial cell lines was evaluated for their anti-inflammatory, antioxidant and anti-senescence activities using colorimetric and fluorescence-based assays, fluorescence imaging, RT-qPCR and proteome profiler kit. The ZER-LCNs successfully reduced the expression of pro-inflammatory markers including Il-6, Il-1 beta and Tnf-alpha, as well as the production of nitric oxide in RAW 264.7 cells. Additionally, ZER-LCNs successfully inhibited oxidative stress through reduction of reactive oxygen species (ROS) levels and regulation of genes, namely GPX2 and GCLC in BCi-NS1.1 cells. Anti-senescence activity of ZER-LCNs was also observed in BCi-NS1.1 cells, with significant reductions in the expression of SIRT1, CDKN1A and CDKN2A. This study demonstrates strong in vitro anti-inflammatory, antioxidative and anti-senescence activities of ZER-LCNs paving the path for this formulation to be translated into a promising therapeutic agent for chronic respiratory inflammatory conditions including COPD and asthma.
- ItemZerumbone-incorporated liquid crystalline nanoparticles inhibit proliferation and migration of non-small-cell lung cancer in vitro(2024) Manandhar, Bikash; Paudel, Keshav Raj; Clarence, Dvya Delilaa; De Rubis, Gabriele; Madheswaran, Thiagarajan; Panneerselvam, Jithendra; Zacconi, Flavia C.; Williams, Kylie A.; Pont, Lisa G.; Warkiani, Majid Ebrahimi; MacLoughlin, Ronan; Oliver, Brian Gregory; Gupta, Gaurav; Singh, Sachin Kumar; Chellappan, Dinesh Kumar; Hansbro, Philip M.; Dua, KamalLung cancer is the second most prevalent type of cancer and is responsible for the highest number of cancer-related deaths worldwide. Non-small-cell lung cancer (NSCLC) makes up the majority of lung cancer cases. Zerumbone (ZER) is natural compound commonly found in the roots of Zingiber zerumbet which has recently demonstrated anti-cancer activity in both in vitro and in vivo studies. Despite their medical benefits, ZER has low aqueous solubility, poor GI absorption and oral bioavailability that hinders its effectiveness. Liquid crystalline nanoparticles (LCNs) are novel drug delivery carrier that have tuneable characteristics to enhance and ease the delivery of bioactive compounds. This study aimed to formulate ZER-loaded LCNs and investigate their effectiveness against NSCLC in vitro using A549 lung cancer cells. ZER-LCNs, prepared in the study, inhibited the proliferation and migration of A549 cells. These inhibitory effects were superior to the effects of ZER alone at a concentration 10 times lower than that of free ZER, demonstrating a potent anti-cancer activity of ZER-LCNs. The underlying mechanisms of the anti-cancer effects by ZER-LCNs were associated with the transcriptional regulation of tumor suppressor genes P53 and PTEN, and metastasis-associated gene KRT18. The protein array data showed downregulation of several proliferation associated proteins such as AXL, HER1, PGRN, and BIRC5 and metastasis-associated proteins such as DKK1, CAPG, CTSS, CTSB, CTSD, and PLAU. This study provides evidence of potential for increasing the potency and effectiveness of ZER with LCN formulation and developing ZER-LCNs as a treatment strategy for mitigation and treatment of NSCLC.