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Scientific community has made a lot of efforts to combat the infectious diseases using antimicrobial agents, but these are associated with problems of development of multi-drug resistance and their adverse side effects. To tackle these challenges, nanocarrier-based drug delivery system using polysaccharides has received enormous attention in the past few years. These antimicrobial agents can become more efficacious when adsorbed, entrapped, or linked to polysaccharides. In addition, these nanocarrier-based systems provide an increase in the surface area of the drug and are able to achieve the targeted drug delivery as well as used for the synthesis of packaging materials with improved mechanical strength, barrier, and antimicrobial properties. This review focuses on potential therapeutic applications of nanocarrier-based drug delivery systems using polysaccharides for antimicrobial applications.

A series of 30 non-covalent imidazo[1,2-a]quinoxaline-based inhibitors of epidermal growth factor receptor (EGFR) were designed and synthesized. EGFR inhibitory assessment (against wild type) data of compounds revealed 6b, 7h, 7j, 9a and 9c as potent EGFRWT inhibitors with IC50 values of 211.22, 222.21, 193.18, 223.32 and 221.53 nM, respectively, which were comparable to erlotinib (221.03 nM), a positive control. Furthermore, compounds exhibited excellent antiproliferative activity when tested against cancer cell lines harboring EGFRWT; A549, a non-small cell lung cancer (NSCLC), HCT-116 (colon), MDA-MB-231 (breast) and gefitinib-resistant NSCLC cell line H1975 harboring EGFRL858R/T790M. In particular, compound 6b demonstrated significant inhibitory potential against gefitinib-resistant H1975 cells (IC50 = 3.65 μM) as compared to gefitinib (IC50 > 20 μM). Moreover, molecular docking disclosed the binding mode of the 6b to the domain of EGFR (wild type and mutant type), indicating the basis of inhibition. Furthermore, its effects on redox modulation, mitochondrial membrane potential, cell cycle analysis and cell death mode in A549 lung cancer cells were also reported.

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Here, a targeted NMR experiment is introduced which selectively detects the formation of 13C–12C bonds in mixtures.

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