Biotinylated polyaminoacid-based nanoparticles for the targeted delivery of lenvatinib towards hepatocarcinoma.

In this work, we describe the development of targeted polymeric nanoparticles loaded with lenvatinib for the treatment of hepatocellular carcinoma (HCC). A synthetic brush copolymer (PHEA-g-BIB-pButMA-g-PEG-biotin) was synthesized from α-poly(N-2-hydroxyethyl)-D,L-aspartamide (PHEA) by a three-step reaction involving atom transfer radical polymerisation (ATRP) to graft hydrophobic polybutylmethacrylate pendant groups and further conjugation with biotinylated polyethylene glycol via carbonate ester. Subsequently, lenvatinib-loaded nanoparticles were obtained and characterized demonstrating colloidal size, negative zeta potential, biotin exposure on the surface and the ability to release lenvatinib in a sustained manner. Lenvatinib-loaded nanoparticles were tested in vitro on HCC cells to evaluate their anticancer efficacy compared to free drug. Furthermore, the enhanced in vivo efficacy of lenvatinib-loaded nanoparticles on nude mice HCC xenograft models was demonstrated by evaluating tumor burdens, apoptotic markers and histological scores after administration of lenvatinib-nanoparticles via intraperitoneal or oral route. Finally, in vivo biodistribution studies were performed, demonstrating the ability of the prepared drug delivery systems to significantly accumulate in the solid tumor by active targeting, due to the presence of biotin on the nanoparticle surface.

Synthesis of Bodipy-Tagged Galactoconjugates and Evaluation of Their Antibacterial Properties.

As a development of our research on biocompatible glycoconjugate probes and specifically multi-chromophoric systems, herein, we report the synthesis and early bactericidal tests of two luminescent glycoconjugates whose basic structure is characterized by two boron dipyrromethene difluoride (BODIPY) moieties and three galactoside rings mounted on an oligophenylene ethynylene (OPE) skeleton. BODIPY fluorophores have found widespread application in many branches of biology in the last few decades. In particular, molecular platforms showing two different BODIPY groups have unique photophysical behavior useful in fluorescence imaging. Construction of the complex architecture of the new probes is accomplished through a convergent route that exploits a series of copper-free Heck-Cassar-Sonogashira cross-couplings. The great emergency due to the proliferation of bacterial infections, in conjunction with growing antibiotic resistance, requires the production of new multifunctional drugs and efficient methods for their targeted delivery to control bacteria-associated diseases. Preliminary studies of the glycoconjugate properties as antibacterial agents against representatives of Gram-negative (P. aeruginosa) and Gram-positive (S. aureus) pathogens, which are associated with chronic infections, indicated significant bactericidal activity ascribable to their structural features.

Anti-Biofilm Strategies: A Focused Review on Innovative Approaches.

Biofilm (BF) can give rise to systemic infections, prolonged hospitalization times, and, in the worst case, death. This review aims to provide an overview of recent strategies for the prevention and destruction of pathogenic BFs. First, the main phases of the life cycle of BF and maturation will be described to identify potential targets for anti-BF approaches. Then, an approach acting on bacterial adhesion, quorum sensing (QS), and the extracellular polymeric substance (EPS) matrix will be introduced and discussed. Finally, bacteriophage-mediated strategies will be presented as innovative approaches against BF inhibition/destruction.

Photochemical synthesis, characterization, and electrochemical sensing properties of CD-AuNP nanohybrids.

Among the existing nanosystems used in electrochemical sensing, gold nanoparticles (AuNPs) have attracted considerable attention owing to their intriguing chemical and physical properties such as good electrical conductivity, high electrocatalytic activity, and high surface-to-volume ratio. However, despite these useful characteristics, there are some issues due to their instability in solution that can give rise to aggregation phenomena and the use of hazardous chemicals in the most common synthetic procedures. With an aim to find a solution to these issues, recently, we prepared and characterized carbon dots (CDs), from olive solid wastes, and employed them as reducing and capping agents in photo-activated AuNP synthesis, thus creating CD-Au nanohybrids. These nanomaterials appear extremely stable in aqueous solutions at room temperature, are contemporary, and have been obtained using CDs, which are exclusively based on non-toxic elements, with an additional advantage of being generated from an otherwise waste material. In this paper, the synthesis and characterization of CD-Au nanohybrids are described, and the electrochemical experiments for hydroquinone detection are discussed. The results indicate that CD-Au acts as an efficient material for sensing hydroquinone, matching a wide range of interests in science from industrial processes to environmental pollution.