Enhancing Flucytosine Anticandidal Activity Using PEGylated Squalene Nanocarrier.

There is an emerging necessity for improved therapies against Candida-related infections, with significant implications for global healthcare. Current antifungal agents, limited in number, target specific pathways, but resistance remains a concern. Flucytosine (5FC) exhibits antifungal activity, particularly against Candida.

Novel Nanotherapeutic Systems Based on PEGylated Squalene Micelles for Enhanced In Vitro Activity of Methotrexate and Cytarabine.

Nanomedicine has garnered significant attention due to the advantages it offers in the treatment of cancer-related disorders, some of the deadliest diseases affecting human lives. Conventional medication formulations often encounter issues of instability or insolubility in biological environments, resulting in low bioavailability. Nanocarriers play a crucial role in transporting and safeguarding drugs at specific sites of action, enabling gradual release under particular conditions.

Mucoadhesive Mesoporous Silica Particles as Versatile Carriers for Doxorubicin Delivery in Cancer Therapy.

Due to their structural, morphological, and behavioral characteristics (e.g., large volume and adjustable pore size, wide functionalization possibilities, excellent biocompatibility, stability, and controlled biodegradation, the ability to protect cargoes against premature release and unwanted degradation), mesoporous silica particles (MSPs) are emerging as a promising diagnostic and delivery platform with a key role in the development of next-generation theranostics, nanovaccines, and formulations.

Towards Regenerative Audiology: Immune Modulation of Adipose-Derived Mesenchymal Cells Preconditioned with Citric Acid-Coated Antioxidant-Functionalized Magnetic Nanoparticles.

: Based on stem cells, bioactive molecules and supportive structures, regenerative medicine (RM) is promising for its potential impact on field of hearing loss by offering innovative solutions for hair cell rescue. Nanotechnology has recently been regarded as a powerful tool for accelerating the efficiency of RM therapeutic solutions. Adipose-derived mesenchymal cells (ADSCs) have already been tested in clinical trials for their regenerative and immunomodulatory potential in various medical fields; however, the advancement to bedside treatment has proven to be tedious.

Chemical Attachment of 5-Nitrosalicylaldimine Motif to Silatrane Resulting in an Organic-Inorganic Structure with High Medicinal Significance.

Two chemical motifs of interest for medicinal chemistry, silatrane as 1-(3-aminopropyl) silatrane (SIL M), and nitro group attached in position 5 to salicylaldehyde, are coupled in a new structure, 1-(3-{[(2-hydroxy-5-nitrophenyl)methylidene]amino}propyl)silatrane (SIL-BS), through an azomethine moiety, also known as a versatile pharmacophore. The high purity isolated compound was structurally characterized by an elemental, spectral, and single crystal X-ray diffraction analysis. Given the structural premises for being a biologically active compound, different specific techniques and protocols have been used to evaluate their in vitro hydrolytic stability in simulated physiological conditions, the cytotoxicity on two cancer cell lines (HepG2 and MCF7), and protein binding ability-with a major role in drug ADME (Absorption, Distribution, Metabolism and Excretion), in parallel with those of the SIL M.

Multilayer gold nanoparticles as non-viral vectors for targeting MCF-7 cancer cells.

Cargocomplexes play a vital role in non-viral delivery methods due to their capacity to target certain cells (or cells through the cell-division cycle) and inject their (macro)molecular "cargo" into them. The development of gene carriers that can efficiently transport and deliver genetic material into human-targeted cells with minimal toxicity is an important challenge in the field. The present study reports the straightforward preparation and testing of a modular non-viral gene carrier based on AuNPs.

Biocompatible Self-Assembled Hydrogen-Bonded Gels Based on Natural Deep Eutectic Solvents and Hydroxypropyl Cellulose with Strong Antimicrobial Activity.

Natural deep eutectic solvents (NADES)-hydroxypropyl cellulose (HPC) self-assembled gels with potential for pharmaceutical applications are prepared. FT-IR, 1HNMR, DSC, TGA and rheology measurements revealed that hydrogen bond acceptor−hydrogen bond donor interactions, concentration of NADES and the water content influence significantly the physico-chemical characteristics of the studied gel systems. HPC-NADES gel compositions have thermal stabilities lower than HPC and higher than NADES components.

Hydroxypropyl Cellulose/Pluronic-Based Composite Hydrogels as Biodegradable Mucoadhesive Scaffolds for Tissue Engineering.

Recently, the development of new materials with the desired characteristics for functional tissue engineering, ensuring tissue architecture and supporting cellular growth, has gained significant attention. Hydrogels, which possess similar properties to natural cellular matrixes, being able to repair or replace biological tissues and support the healing process through cellular proliferation and viability, are a challenge when designing tissue scaffolds. This paper provides new insights into hydrogel-based polymeric blends (hydroxypropyl cellulose/Pluronic F68), aiming to evaluate the contributions of both components in the development of new tissue scaffolds.

Functionalized Mesoporous Silica as Doxorubicin Carriers and Cytotoxicity Boosters.

Mesoporous silica nanoparticles (MSNs) bearing methyl, thiol or glucose groups were synthesized, and their encapsulation and release behaviors for the anticancer drug Doxorubicin (Dox) were investigated in comparison with nonporous homologous materials. The chemical modification of thiol-functional silica with a double bond glucoside was completed for the first time, by green thiol-ene photoaddition. The MSNs were characterized in terms of structure (FT-IR, Raman), morphology (TEM), porosity (nitrogen sorption-desorption) and Zeta potential measurements.

Biocompatible Chitosan-Based Hydrogels for Bioabsorbable Wound Dressings.

Supramolecular hydrogels based on chitosan and monoaldehydes are biomaterials with high potential for a multitude of bioapplications. This is due to the proper choice of the monoaldehyde that can tune the hydrogel properties for specific practices. In this conceptual framework, the present paper deals with the investigation of a hydrogel as bioabsorbable wound dressing.

Hydrophobic Composites Designed by a Nonwoven Cellulose-Based Material and Polymer/CaCO Patterns with Biomedical Applications.

Herein, we report a simple method to obtain hydrophobic surfaces by surface modification with calcium carbonate via diffusion-controlled crystallization using a cheap, versatile, and super-hydrophilic cellulose-based nonwoven material (NWM) as the substrate. To control the CaCO crystal growth, the ammonium carbonate diffusion method was applied in the presence of polyanions [poly(acid acrylic), poly(2-acrylamido-2-methylpropanesulfonic acid), and a copolymer which contains 55 mol % 2-acrylamido-2-methylpropanesulfonic acid and 45 mol % acrylic acid] or nonstoichiometric polyelectrolyte complexes with polycations [poly(allylamine hydrochloride) and chitosan] on a pristine NWM and on polycation-treated surfaces. The surface morphology obtained by calcite growth under surface or environmental functional groups' influence and the hydrophilic/hydrophobic character of the composite materials were followed and compared to that of the starting material.

Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors.

A potential microtubule destabilising series of new indolizine derivatives was synthesised and tested for their anticancer activity against a panel of 60 human cancer cell lines. Compounds , , , and showed a broad spectrum of growth inhibitory activity against cancer cell lines representing leukaemia, melanoma and cancer of lung, colon, central nervous system, ovary, kidney, breast, and prostate. Among them, compound was distinguishable by its excellent cytostatic activity, showing GI values in the range of 10-100 nM on 43 cell lines.

In Vitro and In Vivo Antioxidant Activity of the New Magnetic-Cerium Oxide Nanoconjugates.

Background: Cerium oxide nanoparticles present the mimetic activity of superoxide dismutase, being able to inactivate the excess of reactive oxygen species (ROS) correlated with a large number of pathologies, such as stents restenosis and the occurrence of genetic mutations that can cause cancer. This study presents the synthesis and biological characterisation of nanoconjugates based on nanoparticles of iron oxide interconnected with cerium oxide conjugates.

Methods: The synthesis of magnetite-nanoceria nanoconjugates has been done in several stages, where the key to the process is the coating of nanoparticles with polyethyleneimine and its chemical activation-reticulation with glutaraldehyde.

The Cytotoxic Properties of Some Tricyclic 1,3-Dithiolium Flavonoids.

Background: Due to the emergence of multidrug resistant microorganisms, new classes of antibiotics are needed. In this paper, we present the cytotoxic effects of five tricyclic flavonoids, one of which was previously identified as a potent antimicrobial agent.

Methods: All five derivatives were tested against human HOS and MCF7 cancer cell lines using a wound scratch assay.

Synergistic Effect of Low Molecular Weight Polyethylenimine and Polyethylene Glycol Components in Dynamic Nonviral Vector Structure, Toxicity, and Transfection Efficiency.

When studying polyethylenimine derivatives as nonviral vectors for gene delivery, among the important issues to be addressed are high toxicity, low transfection efficiency, and nucleic acid polyplex condensation. The molecular weight of polyethylenimine, PEGylation, biocompatibility and, also, supramolecular structure of potential carrier can all influence the nucleic acid condensation behavior, polyplex size, and transfection efficiency. The main challenge in building an efficient carrier is to find a correlation between the constituent components, as well as the synergy between them, to transport and to release, in a specific manner, different molecules of interest.

Dynamic constitutional chemistry towards efficient nonviral vectors.

Dynamic constitutional chemistry has been used to design nonviral vectors for gene transfection. Their design has been thought in order to fulfill ab initio the main requirements for gene therapy. As building blocks were used hyperbranched PEI as hydrophilic part and benzentrialdehyde and a diamine linear siloxane as hydrophobic part, connected through reversible imine linkages.

Flexible cyclic siloxane core enhances the transfection efficiency of polyethylenimine-based non-viral gene vectors.

Transfection of nucleic acid molecules, large enough to interfere with the genetic mechanisms of active cells, can be performed by means of small carriers, able to collectively collaborate in generating cargocomplexes that could be involved in passive mechanisms of cellular uptake. The present work describes the synthesis, characterization, and evaluation of transfection efficacy of a conjugate molecule, which comprises a cyclic siloxane ring (2,4,6,8-tetramethylcyclotetrasiloxane, cD ) as the core, and, on average, 3.76 molecules of 2 kDa polyethyleneimine (PEI) as cationic branches, with an average molecular mass of 7.

DyNAvectors: dynamic constitutional vectors for adaptive DNA transfection.

Dynamic constitutional frameworks, based on squalene, PEG and PEI components, reversibly connected to core centers, allow the efficient identification of adaptive vectors for good DNA transfection efficiency and are well tolerated by mammalian cells.

Dynamic constitutional frameworks (DCFs) as nanovectors for cellular delivery of DNA.

We introduce Dynamic Constitutional Frameworks (DCFs), macromolecular structures that efficiently bind and transfect double stranded DNA. DCFs are easily synthesizable adaptive 3D networks consisting of core connection centres reversibly linked via labile imine bonds both to linear polyethyleneglycol (PEG, ∼1500 Da) and to branched polyethyleneimine (bPEI, ∼800 Da). DCFs bind linear and plasmid DNA, forming particulate polyplexes of 40-200 nm in diameter.

Hybrid fullerene conjugates as vectors for DNA cell-delivery.

The present study reports fullerene conjugates that act as efficient binders of double stranded DNA (dsDNA) into cytofriendly polyplexes. The conjugates are designed to generate dendrimeric structures, having C60 as the core and bearing linear or branched PEI and polyethyleneglycol (PEG) arms (∼2 kDa). Simple and reproducible synthesis pathways provided C60-PEI and C60-PEG-PEI conjugates.