Nanoemulsion-Based System as a Novel and Promising Approach for Enhancing the Antimicrobial and Antitumoral Activity of Thymus vulgaris (L.) Oil in Human Hepatocellular Carcinoma Cells.

The utilisation of medicinal plants and their essential oils is receiving more attention due to the ineffectiveness of current therapeutic methods in the treatment of various cancers and the rising incidence of bacterial antibiotic resistance. Thymol, an active ingredient of Thymus vulgaris, is known to have hepatoprotective, antibacterial, and antioxidant properties. To overcome major obstacles to their usage, such as quick oxidation and high volatility, plant essential oils must be administered through a system to improve the delivery of their active pharmaceutical ingredient. The bioavailability of active substances may be enhanced by the colloidal dispersion nanoemulsion. Therefore, this study aims to derive a comparative evaluation of the thyme oil nanoemulsion formulation and the characterisation of its antibacterial and antitumorigenic activities. A nanoemulsion (NE) with a droplet size of 122.2 ± 1.079 nm was discovered to be stable and mono-dispersed for 4 months and inhibited the growth of B. subtilis, E. coli, P. aeruginosa, and S. aureus. It also displayed antitumorigenic capabilities in HepG2 cells by arresting the cell cycle in the G2/M phase and upregulating the gene expression levels of Bcl-2-associated X protein (Bax), Caspase 3, 8, and 9, as well as a concomitant concentration-dependent decrease in B-cell leukaemia/lymphoma 2 protein (BCL2). Along with an increase in inducible nitric oxide synthase (iNOS) levels, upregulation of the expression levels of the reactive oxygen species (ROS), mitogen-activated protein kinase (MAPK), and endoplasmic reticulum (ER) stress pathways was also seen, indicating of ROS formation in the cancer cells.

Fabrication, assessment, and potential anti-bacterial activity of sandalwood oil nanoemulsion and its hand rub sanitizer.

In the last decade, extensive research has been performed on developing hand sanitizers that can be used to eradicate the diseases that are caused due to poor hand hygiene. Essential oils possess antibacterial and antifungal properties and thus have great potential to replace the available antibacterial agents. In the present study, sandalwood oil-based nanoemulsion (NE) and sanitizer have been formulated and well characterized for their properties. Antibacterial activity was assessed using growth inhibition studies, agar cup, viability assay, etc. The sandalwood oil NE synthesized had oil to surfactant ratio of 1:0.5 (2.5% sandalwood oil and 0.5% Tween 80) and was observed to have a droplet diameter of 118.3 ± 0.92 nm, the zeta potential of - 18.8 ± 2.01 mV, and stability of 2 months. The antibacterial activity of sandalwood NE and sanitizer was evaluated against microorganisms. The antibacterial activity was assessed using the zone of inhibition value of sanitizer, which was in the range of 19 to 25 mm against all microorganisms. Morphological analysis showed distant changes in membrane shape and size and microorganisms' morphology. The synthesized NE was thermodynamically stable and efficient enough to be used in sanitizer, and the formulated sanitizer showed great antibacterial efficacy.

Development of food-grade antimicrobials of fenugreek oil nanoemulsion-bioactivity and toxicity analysis.

Antimicrobials of natural origin are proving to be an effective solution to emerging antimicrobial resistance and its physiological side effects. Recent studies have demonstrated that essential oils encapsulated in the form of nanoemulsions have better antimicrobial activity than the oil itself, possibly due to its high stability, solubility, sustained release, and increased bioavailability. In the present study, fenugreek oil-a well-known antimicrobial and antioxidant-has been used to fabricate nanoemulsion (NE), with an objective to meet potential alternative to synthesized antimicrobials. A combination of three different components, water, fenugreek oil, and Tween 80, has been used to prepare the nanoemulsions of different size and one of the most stable nanoemulsion with lowest concentration of surfactant Tween 80 was used to assess its bioactivity, antimicrobial properties, and toxicity against human hepatic cell line. Among all the formulations, nano-emulsion with 2.5% oil concentration, 30 min sonication (hydrodynamic size 135.2 nm, zeta potential 36.8 mV, PDI 0.135, and pH 5.12), was selected for all studies. The nanoemulsion showed potential antibacterial activity against all the microbial strains (Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa) used in this study. Interestingly, the nanoemulsion showed potential antibacterial activity against P. aeruginosa, known to show resistance against ampicillin. The toxicity evaluation in human hepatic cell line (WRL-68) indicated no significant toxicity of nanoemulsion up to the concentration of 800 µg/ml. The synthesized nanoemulsion thus has a translational potential as a food-grade non-toxic natural nanoantimicrobials.

MiR-206 conjugated gold nanoparticle based targeted therapy in breast cancer cells.

MicroRNAs (miRNAs) are single-stranded, non-coding, 19-25 nucleotide RNA molecules that have been observed to be dysregulated in many diseases including cancer. miRNAs have been known to play an important role in cellular proliferation, differentiation, migration, apoptosis, survival, and morphogenesis. Breast cancer is heterogeneous in nature and contributed extensively to the increased mortality rate. miRNA can either be tumor-suppressive or oncogenic in nature. The level of expression of miRNA changes according to the subtypes of cancer and the mutation responsible for different cancers. miRNA mimicry or inhibition are emerging possible therapies to maintain the level of miRNA inside the cells. In order to have proper miRNA mimicry, the major hurdle is to deliver the miRNA mimics at the site of tumor. Metallic nanoparticles with modified surface can be used to solve the problem of miRNA delivery. MiR-206 is reported to be down-regulated in Luminal-A type of breast cancer. In the current manuscript, we aim to modify the surface of gold-nanoparticles (AuNPs) with PEG moiety and allow miRNA to attach to it. The fabricated nano-complex, not only delivered miR-206 but also caused cell death in MCF-7 by arresting cells in the G0-G1 phase and inducing apoptosis by downregulating NOTCH 3.

Fabrication of methotrexate-loaded gold nanoconjugates and its enhanced anticancer activity in breast cancer.

Methotrexate (MTX) is known antagonist of folic acid and widely used as an anti-cancer drug. The folate receptor (FR) and reduced folate carrier are mostly responsible for internalization of methotrexate in tumor cells. Mutation in reduced folate carrier (RFC) leads to resistance against MTX in various tumor cell lines including MDA-MB-231 breast cancer cells. To overcome the resistance of MTX, folate receptor targeted nanoparticles have been commonly used for targeting breast tumors. The aim of the study is to determine the ability of methotrexate gold nanoparticles (MTX-GNPs) in the induction of apoptosis and to explore the molecular changes at genomics and proteomics level. Different assays like cell viability assay, cell cycle analysis, apoptosis, real-time PCR and western blot were carried out to evaluate the anti-cancer effect of MTX-Gold NPs on MCF-7 and MDA-MB-231 cells. Our observations demonstrated the decrease in the percent viable cells after the treatment of MTX-GNPs, with an arrest in cell cycle at G0/G1 phase and a significant increase in apoptotic cell population and loss of mitochondrial membrane potential in MCF-7 and MDA-MB-231 cells. Folate receptor targeted MTX-GNPs showed significant cellular uptake in breast cancer cells along with significant down-regulation in expression of anti-apoptotic gene (Bcl-2) and up-regulation in expression of pro-apoptotic genes (Bax, Caspase-3, Caspase-9, APAF-1, p53). These results unveil the increased anti-cancer effect of MTX-GNPs in cancer cells. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s13205-021-02718-7.

Nanotherapeutics for the Treatment of Cancer and Arthritis.

BACKGROUND: Nanotechnology is gaining significant attention worldwide for the treatment of complex diseases such as AIDS (acquired immune deficiency syndrome), cancer and rheumatoid arthritis. Nanomedicine is the application of nanotechnology used for diagnosis and treatment for the disease that includes the preservation and improvement of human health by covering an area such as drug delivery using nanocarriers, nanotheranostics and nanovaccinology. The present article provides an insight into several aspects of nanomedicine such as usages of multiple types of nanocarriers, their status, advantages and disadvantages with reference to cancer and rheumatoid arthritis. METHODS: An extensive search was performed on the bibliographic database for research article on nanotechnology and nanomedicine along with looking deeply into the aspects of these diseases, and how all of them are co-related. We further combined all the necessary information from various published articles and briefed to provide the current status. RESULTS: Nanomedicine confers a unique technology against complex diseases which includes early diagnosis, prevention, and personalized therapy. The most common nanocarriers used globally are liposomes, polymeric nanoparticles, dendrimers, metallic nanoparticles, magnetic nanoparticles, solid lipid nanoparticles, polymeric micelles and nanotubes among others. CONCLUSION: Nanocarriers are used to deliver drugs and biomolecules like proteins, antibody fragments, DNA fragments, and RNA fragments as the base of cancer biomarkers.

Formulation of vitamin D encapsulated cinnamon oil nanoemulsion: Its potential anti-cancerous activity in human alveolar carcinoma cells.

Cinnamon oil is used for medicinal purpose since ancient time because of its antioxidant activity. Oil-in-water nanoemulsion (NE) of cinnamon oil was formulated using cinnamon oil, nonionic surfactant Tween 80 and water by ultrasonication technique. Phase diagram was constructed to investigate the influence of oil, water and surfactant concentration. Vitamin D encapsulated cinnamon oil NE was fabricated by wash out method followed by ultrasonication in similar fashion. The hydrodynamic size of cinnamon oil NE and vitamin D encapsulated cinnamon oil NE was observed as 40.52 and 48.96 nm in complete DMEM F12 media respectively. We focused on the cytotoxic and genotoxic responses of NEs in A549 cells in concentration dependent manner. We observed that both NEs induce DNA damage along with corresponding increase in micronucleus frequency that is evident from the comet and CBMN assay. Both the NEs arrested the cell cycle progression in G0/G1 phase, showed increased expression of Bax, capase-3 and caspase-9 and decrease expression of BcL2 proteins along with significant (p < 0.05) increase in apoptotic cell population and loss of mitochondrial membrane potential. NEs were also evaluated for bactericidal efficacy against E. coli. Thus, both NEs have cytotoxic, genotoxic and antibacterial potential and hence can also be used in food industry with cinnamon oil as carrier for lipophilic nutraceutical like vitamin D.