DATS (diallyl trisulfide), an anti-oxidant and cytotoxic chemical derived from the plant garlic, has been found to have potential therapeutic activity against triple-negative breast cancer (TNBC). Its hydrophobicity, short half-life, lack of target selectivity, and limited bioavailability at the tumor site limit its efficacy in treating TNBC. Overexpression of the Folate receptor on the surface of TNBC is a well-known target receptor for overcoming off-targeting, and lipid nanoparticles solve the limitations of limited bioavailability and short half-life. In order to overcome these constraints, we developed folic acid (FA)-conjugated DATS-SLNs in this research. The design of experiment (DoE) method was employed to optimize the FA-DATS-SLNs’ nanoformulation, which resulted in a particle size of 168.2 ± 3.78 nm and a DATS entrapment of 71.91 ± 6.27%. The similarity index between MCF-7 and MDA-MB-231 cell lines demonstrates that FA-DATS-SLNs are more therapeutically efficacious in the treatment of aggravating TNBC. Higher cellular internalization and efficient Bcl2 protein downregulation support the hypothesis that functionalization of the FA on the surface of DATS-SLNs improves anticancer efficacy when compared with DATS and DATS-SLNs. FA-functionalized DATS-SLNs have demonstrated to be a promising therapeutic strategy for TNBC management.

The “Warburg effect” provides a novel method for treating cancer cell metabolism. Overexpression of glucose transporter 1 (GLUT1), activation of AMP-activated protein kinase (AMPK), and downregulation of mammalian target of rapamycin (mTOR) have been identified as biomarkers of abnormal cancer cell metabolism. Metformin (MET) is an effective therapy for breast cancer (BC), but its efficacy is largely reliant on the concentration of glucose at the tumor site. We propose a WZB117 (a GLUT1 inhibitor)-OCMC (O-carboxymethyl-chitosan)-MET combo strategy for simultaneous GLUT1 and mTOR targeting for alteration of BC metabolism. WZB117 conjugated polymeric nanoparticles were 225.67 ± 11.5 nm in size, with a PDI of 0.113 ± 0.16, and an encapsulation of 72.78 6.4%. OCMC pH-dependently and selectively releases MET at the tumor site. MET targets the mTOR pathway in cancer cells, and WZB117 targets BCL2 to alter GLUT1 at the cancer site. WZB117-OCMC-MET overcomes the limitations of MET monotherapy by targeting mTOR and BCL2 synergistically. WZB117-OCMC-MET activates AMPK and suppresses mTOR in a Western blot experiment, indicating growth-inhibitory and apoptotic characteristics. AO/EB and the cell cycle enhance cellular internalization as compared to MET alone. WZB117-OCMC-MET affects cancer cells’ metabolism and is a promising BC therapeutic strategy.

Background: Ulcerative colitis (UC) is a chronic inflammatory condition associated with the colon and rectum, often predisposing individuals to inflammatory bowel disease-related colorectal cancer (IBD-CRC). Current therapeutic options for UC, including corticosteroids and immunosuppressive drugs, pose significant side effects. Punica granatum peel powder (PPPG), a traditional herbal remedy in Ayurveda medicine for colitis, exhibits promising therapeutic effects with a favorable safety profile. Objectives: This study aims to explore the therapeutic potential and mechanism of action of a modified PPPG formulation in UC treatment. Methods: Using NCM460 cells and an acetic acid-induced UC murine model, the efficacy of modified PPPG was evaluated. Results: Therapy with modified PPPG significantly improved UC-associated symptoms, such as improvements in body weight, colon length, and disease activity index, as validated by histological examination. Transcriptomic sequencing identified downregulation of the IL-6/STAT3 signaling pathway and reduced inflammatory markers like p-NF-κB, IL-1β, and NLRP3 on PPPG therapy. Conclusions: These findings suggest that modified PPPG holds promise as a novel therapeutic strategy for UC intervention, targeting key inflammatory pathways implicated in UC pathogenesis and potentially mitigating the risk of IBD-CRC.

TRAIL or tumor necrosis factor-related apoptosis-inducing ligand has been one of the major frontiers for the chemotherapeutic approach to treating carcinogenesis. Despite the emergence of TRAIL resistance cancer cell lines, it has been extensively studied for its unique property to induce apoptosis and provide specificity to any other conjugated chemotherapeutic agent. TRIAL highly reduces the dose and increases specific and targeted action against the cancer cells. It is a specific agonist for the death receptors DR4 and DR5 present on the cancer cell surface. Normal cells have more expression of decoy type of death receptors, which makes the use of TRAIL safer for regular cells. The TRAIL-drug conjugate systems have been under the radar due to their possible high synergistic potential and may open the door for the future cancer-specific targeted treatment frontier. This current study was conducted with a particular aim to provide a concise and simple amalgamation of current scenarios of different conjugations of this molecule along with various other molecules, RNAs, ligands, and anticancer drugs. Along with possible delivery systems of TRIAL that can have a significant future and the promise that is held by this particular way of cancer combinational chemotherapy with special interest in colorectal cancer.

Despite its advances in medicine, cancer still remains elusive for most of the conventional therapies because the medications are applied to healthy tissues as well; traditional procedures frequently result in significant adverse effects. This chapter provides a comprehensive overview of the role of nanotechnology in cancer diagnosis, imaging, and treatment. The chapter explores both passive and active targeting techniques as well as the mechanics behind medication delivery using nanoparticles. Therefore, the potential of nanotechnology to improve biomarker detection and cancer imaging is investigated. Furthermore, the prospect of nanotechnology for co-delivery of numerous therapeutic drugs into a single nanocarrier and combination therapy is investigated, emphasising the synergistic benefits and improved therapeutic results possible with this strategy. Overall, this chapter emphasises how much nanotechnology may do to enhance cancer outcomes by offering focused, effective, and least intrusive treatment options.