Aminated Polysaccharide-Based Nanoassemblies as Stable Biocompatible Vehicles Enabling Crossing of Biological Barriers: An Effective Transdermal Delivery of Diclofenac Medicine.

A series of stable polysaccharide derivatives that spontaneously self-assemble into nanocarriers was synthesized by applying a reductive amination on chitosan. The prepared nanocarriers were comprehensively studied and found to allow encapsulation of molecular cargo in both aqueous and lipidic media and deliver this cargo across biological barriers. The nanocarriers have demonstrated effective transdermal delivery of diclofenac (Voltaren), a nonsteroidal anti-inflammatory drug, by increasing its skin permeation up to 100 vs the tested control. The modified polysaccharides were studied with a panel of three types of bioreporter bacteria sensitive to genotoxic and cytotoxic stresses. These studies showed the general safety of the prepared nanocarriers and provided insights concerning their activity in collaboration with the aliphatic side chain length. The described nanocarriers could be applied as tunable biocompatible vehicles for the delivery of medicines, cosmetic agents, and in other applications.

Omniphilic Polysaccharide-Based Nanocarriers for Modular Molecular Delivery in a Broad Range of Biosystems.

Self-adjusting omniphilic nanocarriers (OPNs) with a multisolvent aptitude were prepared via a Schiff base reaction between chitosan, a natural polysaccharide, and bioactive aldehydes. Experimental studies supported by atomistic molecular dynamics simulations revealed these OPNs can encapsulate insoluble molecular cargo, transport them in aqueous or lipid environments, and deliver them through cross-phase barriers. N-imine dynamic covalent bonds have been incorporated to endow the OPNs with pH responsiveness, also allowing the amplification of their bioactivity, as demonstrated in vitro with the ability to delay fungal proliferation in wheat grains. The reported OPNs hold remarkable potential as biocompatible nanocarriers for the effective delivery of active agents in agriculture, medicine, and cosmetics.

Eliminating the Need for Biocidal Agents in Anti-Biofouling Polymers by Applying Grafted Nanosilica Instead.

A nondestructive one-step approach was applied for grafting biocide-free monodispersed silica nanoparticles (SNPs) with a diameter of 30 ± 10 nm on polystyrene, polyethylene, and polyvinyl chloride surfaces. The prepared surfaces were comprehensively characterized using spectroscopic (Fourier transform infrared attenuated total reflection, ultraviolet-visible, and X-ray photoelectron spectroscopy) and microscopic (high-resolution scanning electron microscopy and atomic force microscopy) methods. The modified polymers were found to maintain their original mechanical and physical properties, while their nanoroughness on the other hand had risen by 1.6-2.7 times because of SNP grafting. The SNP-grafted surfaces displayed anti-biofouling properties, resulting in a significant reduction in the attached Gram-positive Bacillus licheniformis or Gram-negative Pseudomonas aeruginosa bacteria compared to their nongrafted counterparts. Confocal laser scanning microscopy and scanning electron microscopy studies have confirmed that bacterial cells could not successfully adhere onto the SNP-grafted polymer films regardless of the polymer type, and their biofilm formation was therefore damaged. The presented facile and straightforward protocol allows eliminating the need for biocidal agents and resorts to grafted nanosilica instead. This strategy may serve as a feasible and safe platform for the development of sustainable anti-biofouling surfaces in biomedical devices; food, water, and air treatment systems; and industrial equipment.

Investigation of Substituent Effect in Modified Nature-Sourced Polymers: Rational Side Chain Engineering to Control Yield, Design, and Properties.

"Side chain engineering" research has yielded many promising and beneficial results, with applications in various fields. However, this research did not receive sufficient focus when nature-sourced polymers are concerned. In this study, we have performed side chain engineering on chitosan, a nature-sourced polysaccharide, by coupling it with a number of aliphatic aldehydes of varying chain lengths. The side chains' length and the pursuing effect on the modified products' properties were studied in great detail. In terms of coupling yields, it was found that some substituents have displayed more favorable results than others by a factor of over 35 times. When studying the modified polymers' physical and mechanical properties, some of them were found to exhibit more rigid mechanical properties by a factor of 3.5 times than others. The effect was also expressed through self-assembly concentrations and encapsulation capabilities of the modified polymers. Remarkably, the combined experimental and calculated kinetic studies showed the results do not necessarily follow a linear progression relating to substituent chain length, but rather a parabolic pattern with a specific extremum point. This study has assisted in shedding light on the inspected phenomenon, explaining that not only steric and electronic factors but also interfacial solubility related factors govern the coupling reaction and the resulting modified polymers' properties. As chemical protocols in various academic, clinical, and industrial studies around the world slowly shift their norms toward finding safer ways for the production of novel materials and technologies, nature-sourced polymers hold great promise as virtually inexhaustible raw materials. The perfection of their chemical modification is therefore relevant now more than ever, with far-reaching and diverse applicative prospects.

Antimicrobial films based on cellulose-derived hydrocolloids. A synergetic effect of host-guest interactions on quality and functionality.

A series of active films based on biodegradable cellulose-derived hydrocolloids capable of controlled release of antimicrobial propionic acid (PA) was prepared. ß-Cyclodextrin (ß-CD), usually used for encapsulation of lipophilic compounds, was utilized in this research to host the hydrophilic PA. It was found that addition of ß-CD to the film forming solutions notably enhanced the hydrocolloid matrix capacity and resulted in up to a ten-fold increase in the amount of uploaded PA. In addition, ß-CD resulted in a two-fold prolongation of the effective PA release duration. ß-CD alone caused undesired effects on the physical, mechanical and morphological properties of the hydrocolloid films. Interestingly, when ß-CD was combined with PA in the film formulation, its undesired effects were significantly subdued. The antifungal activity of the films was demonstrated on fresh harvested wheat grains. Films containing ß-CD and PA were found to be effective in preventing fungal growth on wheat grains. Thus, incorporation of ß-CD and PA in hydrocolloids matrices demonstrated a synergetic effect and resulted in the formation of biodegradable active films that benefit good physical and mechanical properties, high active agent content, prolonged release ability and effective antimicrobial properties.

Assessment of 6'- and 6'''-N-acylation of aminoglycosides as a strategy to overcome bacterial resistance.

Amongst the many synthetic aminoglycoside analogues that were developed to regain the efficacy of this class of antibiotics against resistant bacterial strains, the 1-N-acylated analogues are the most clinically used. In this study we demonstrate that 6'-N-acylation of the clinically used compound tobramycin and 6'''-N-acylation of paromomycin result in derivatives resistant to deactivation by 6'-aminoglycoside acetyltransferase (AAC(6')) which is widely found in aminoglycoside resistant bacteria. When tested against AAC(6')- or AAC(3)-expressing bacteria as well as pathogenic bacterial strains, some of the analogues demonstrated improved antibacterial activity compared to their parent antibiotics. Improvement of the biological performance of the N-acylated analogues was found to be highly dependent on the specific aminoglycoside and acyl group. Our study indicates that as for 1-N-acylation, 6'- and 6'''-N-acylation of aminoglycosides offer an additional promising direction in the search for aminoglycosides capable of overcoming infections by resistant bacteria.