Antibacterial nanoparticles based on fluorescent 3-substituted uridine analogue

With a sudden and rapid increase in the spread of antimicrobial resistance, there is an urgent need for the development of novel antimicrobial therapies. Nanoparticles with antimicrobial activity provide advantages such as improved solubility, permeability, stability and selectivity. In this study, a uridine-scaffold was connected to a pyrene fluorescent unit to obtain novel compound UPy via an economical and straightforward route. Further, fluorescent organic nanoparticles (FONs) were prepared via self assembly of UPy and were found to have antibacterial activity towards Gram positive bacteria. The fluorescent nature of the FONs allowed us to identify a binding partner and propose mechanism of action in vivo. We believe that UPy can be an excellent starting point for the development of novel, potent and selective antimicrobial nanotherapeutics

Organic Nanovesicular Cargoes for Sustained Drug Delivery: Synthesis, Vesicle Formation, Controlling “Pearling” States, and Terfenadine Loading/Release Studies

“Sustained drug delivery systems” which are designed to accomplish long-lasting therapeutic effect are one of the challenging topics in the area of nanomedicine. We developed an innovative strategy to prepare nontoxic and polymer stabilized organic nanovesicles (diameter: 200 nm) from a novel bolaamphiphile, where two hydrogen bonding acetyl cytosine molecules connected to 4,4′′-positions of the 2,6-bispyrazolylpyridine through two flexible octyne chains. The nanovesicles behave like biological membrane by spontaneously self-assembling into “pearl-like” chains and subsequently forming long nanotubes (diameter: 150 nm), which further develop into various types of network-junctions through self-organization. For drug loading and delivery applications, the nanovesicles were externally protected with biocompatible poly(ethyleneglycol)-2000 to prevent them from fusion and ensuing tube formation. Nontoxic nature of the nanovesicles was demonstrated by zebrafish teratogenicity assay. Biocompatible nanovesicles were loaded with “terfenadine” drug and successfully utilized to transport and release drug in sustained manner (up to 72 h) in zebrafish larvae, which is recognized as an emerging in vivo model system