Improved Water Solubility Research Articles

A Comprehensive Review on Solid Lipid Nanoparticles as a Carrier for Oral Absorption of Phyto-Bioactives.

Phyto-bioactive(PB) compounds are naturally occurring substances derived from plantsthat offer significant health benefits ranging from antioxidant and anti-inflammatory activities to potential cancer-fighting properties. However, their widespread application is limited by several inherent limitations, such as low bioavailability, poor biostability, limited aqueous solubility, and no site-specific target. Additionally, the necessity for high concentrations of effective PBs doses further restricts their use. Encapsulating PBs in suitable nanocarriers, particularly solid lipid nanoparticles (SLNs), can enhancetheir stability in biological environments, improvewater solubility, enablecontrolled release, and allowfor targeted delivery. This innovative approach increases bioavailability, reduces toxicity, and potentially lowers effective dosages. The current review examines the critical factors influencing oral PBs delivery, explores how biocompatible and biodegradable SLNs can be optimized to overcome these challenges, and discusses emerging techniques in nanoparticle design that could further enhance the efficacy of PBs delivery systems.

Carboxymethylation of paramylon derived from Euglena gracilis and its hypoglycemic mechanism in diabetic mice

Paramylon is a polysaccharide primarily composed of β-1,3-glucan, characterized by its high crystallinity and insolubility in water. Enhancing its water solubility through structural modifications presents an effective strategy to unlock its biological activity. In this study, carboxymethylation was employed to produce carboxymethylated paramylon (CEP) with varying carboxyl concentrations. The successful introduction of carboxyl groups led to a notable improvement in water solubility. In vivo experiments demonstrated that CEP reduced fasting blood glucose levels by 24.42 %, improved oral glucose tolerance, and enhanced insulin sensitivity in diabetic mice. Additionally, CEP regulated lipid homeostasis and ameliorated liver damage. Through modulation of the adenosine monophosphate-activated protein kinase/phosphoinositide 3-kinase/protein kinase B pathway and the glucose-6-phosphatase/phosphoenolpyruvate carboxykinase pathway, CEP effectively regulated hepatic glucose absorption and production. Furthermore, CEP mitigated diabetes-induced lipid metabolism disorders. These findings suggest that CEP holds significant promise in ameliorating glucose metabolism disorder, indicating its potential as a novel hypoglycemic functional food.

Improving Water Solubility and Skin Penetration of Ursolic Acid through a Nanofiber Process to Achieve Better In Vitro Anti-Breast Cancer Activity.

Woman's breast cancer has always been among the top ten causes of cancer death, and nearly 2% to 5% of locally advanced breast cancers develop a fungating breast wound. Fungal breast cancer leads to skin ulcers, wound ruptures, and other bacterial infections in patients. Ursolic acid (UA), a natural pentacyclic triterpene compound, is widely distributed in many fruits. Previous studies demonstrated that UA has anti-breast cancer, antifungal, and improved wound-healing effects. UA, however, had poor water solubility and low bioavailability, restricting its clinical application. Nanofibers have the advantages of rapid dissolution, improved stability, and bioavailability of active ingredients. We had successfully prepared ursolic acid nanofibers (UANFs) and effectively improved their water solubility and skin penetration. UANFs can increase water solubility by improving the physicochemical properties, including increased surface area, intermolecular bonding with excipients, and amorphous transformation. Furthermore, UANFs had better anti-breast cancer activity than raw UA. UANFs inhibited the expression of phospho-signal transducer and activator of transcription 3 (STAT3) and phospho-extracellular regulated protein kinases (ERK)1/2, and induced cleaved caspase-3 protein expression, but had no effect on the raw UA treatment. In summary, UANFs enhanced the skin absorption of UA and improved its anti-breast cancer efficacy. We expect that UANFs can be used as an anti-breast cancer treatment and reduce the discomfort of breast cancer patients during dressing changes, but more detailed efficacy and safety trials still need to be conducted in further studies.

Facile preparation of multi-functionalized zwitterionic surfactants for the separation of water in Arabian heavy crude oil emulsions

We report an easy process to prepare new anionic and zwitterionic surfactants to break water in Arabian heavy crude oil emulsions (W/O) with different compositions (10/90, 30/70 and 50/50 vol%). Surfactants were prepared in only two stages using simple methodology. Diethylenetriamine was interacted with three moles of glycidyl 4-nonyl ether followed by the interaction with 3 and 8 mol of 1,3-propanesultone to yield TNDTS-3 and TNDTS-8 respectively. FTIR and NMR spectroscopies were carried out to substantiate the chemical structures of surfactants. Relative solubility number (RSN), surface activity and solubility properties were determined. Demulsification efficiencies and interfacial tension (IFT) of the prepared surfactants were investigated. Our findings demonstrated that increasing propyl sulfonate groups in the surfactant structure improved water solubility, IFT activity and demulsification efficiency. TNDTS-8 achieved 100 % demulsification activities in all W/O emulsions (10/90, 30/70 and 50/50 vol%).

Environmentally Friendly UV Absorbers: Synthetic Characterization and Biosecurity Studies of the Host-Guest Supramolecular Complex.

Isoamyl 4-methoxycinnamate (IMC) is widely used in various fields because of its exceptional UV-filter properties. However, due to its cytotoxicity and anti-microbial degradability, the potential eco-environmental toxicity of IMC has become a focus of attention. In this study, we propose a host-guest supramolecule approach to enhance the functionality of IMC, resulting in a more environmentally friendly and high-performance materials. Sulfobutyl-β-cyclodextrin sodium salt (SBE-β-CD) was used as the host molecule. IMC-SBE-β-CD supramolecular substances were prepared through the "saturated solution method", and their properties and biosecurity were evaluated. Meanwhile, we conducted the AOS tree evaluation system that surpasses existing evaluation approaches based on apoptosis, oxidative stress system, and signaling pathways to investigate the toxicological mechanisms of IMC-SBE-β-CD within human hepatoma SMMC-7721 cells as model organisms. The AOS tree evaluation system aims to offer the comprehensive analysis of the cytotoxic effects of IMC-SBE-β-CD. Our findings showed that IMC-SBE-β-CD had an encapsulation rate of 84.45% and optimal stability at 30 °C. Further, IMC-SBE-β-CD promoted cell growth and reproduction without compromising the integrity of mitochondria and nucleus or disrupting oxidative stress and apoptosis-related pathways. Compared to IMC, IMC-SBE-β-CD is biologically safe and has improved water solubility with the UV absorption property maintained. Our study provides the foundation for the encapsulation of hydrophobic, low-toxicity organic compounds using cyclodextrins and offers valuable insights for future research in this field.

Insights into 5-fluorouracil anti–cancer drug encapsulation within the pristine and palladium-doped carbon, silicon-carbide, and germanium-carbide nanotubes: A DFT investigation for advanced nanomedicine applications

In this study, we investigated the interaction and binding properties of 5-Fluorouracil (5-FU), an anti-cancer drug, encapsulated within pristine and palladium-doped carbon, silicon-carbide, and germanium-carbide nanotubes (CNT, SiCNT, GeCNT). Using density functional theory (DFT), we conducted a comprehensive analysis at both aqueous and gas phases. This included geometrical, structural, electrical, bonding, and thermodynamic properties, optimized geometries, adsorption energies, quantum molecular descriptors, frontier molecular orbitals, and topological parameters at the M06-2X level of theory. Our findings indicate that Pd-doping enhances the encapsulation capabilities of nanotubes, strengthening interactions with 5-FU and improving water solubility. Calculations of recovery time required for drug release suggest that Pd-doped nanotubes effectively control the release of 5-FU. Notably, the decapsulation time of 5-FU from of Pd-doped nanotubes was longer in the gas phase than in aqueous conditions. Using the quantum theory of atoms in molecules (QTAIM) method, we investigated intermolecular interactions and critical bonding points. Natural bond orbital (NBO) analysis revealed enhanced stabilization of the 5-FU molecule post-encapsulation, with charge transfer primarily directed from nanotubes to the 5-FU. Hirshfeld surface analysis highlighted that hydrogen bonds between 5-FU active sites and nanotubes are crucial in encapsulation and fixation. Reduced Density Gradient (RDG) analysis confirmed Pd-doping as a primary source of strong attractive interactions in 5-FU/Pd-doped nanotube complexes compared to pristine nanotubes.

Enhancing Oral Bioavailability of Domperidone Maleate: Formulation, In vitro Permeability Evaluation In-caco-2 Cell Monolayers and In situ Rat Intestinal Permeability Studies.

The domperidone maleate, a lipophilic agent classified as a Biopharmaceutical Classification System Class II substance with weak water solubility. Self- Emulsifying Drug Delivery System is a novel approach to improve water solubility and, ultimately bioavailability of drugs. This study aimed to develop and characterize new domperidone-loaded self-emulsifying drug delivery systems as an alternative formulation and to evaluate the permeability of domperidone-loaded self-emulsifying drug delivery systems by using Caco-2 cells and via single-pass intestinal perfusion method. Three self-emulsifying drug delivery systems were prepared and characterized in terms of pH, viscosity, droplet size, zeta potential, polydispersity index, conductivity, etc. Each formulation underwent 10, 100, 200, and 500 times dilution in intestinal buffer pH 6.8 and stomach buffer pH 1.2, respectively. Female Sprague Dawley rats were employed for in situ single-pass intestinal perfusion investigations. Results of the study revealed that the ideal self-emulsifying drug delivery systems formulation showed narrow droplet size, ideal zeta potential, and no conductivity. Additionally, as compared to the control groups, the optimum formulation had better apparent permeability (12.74 ± 0.02×10-4) from Caco-2 cell monolayer permeability experiments. The study also revealed greater Peff values (2.122 ± 0.892×10-4 cm/s) for the optimal formulation from in situ intestinal perfusion analyses in comparison to control groups (Domperidone; 0.802 ± 0.418×10-4 cm/s). To conclude, prepared formulations can be a promising way of oral administration of Biopharmaceutical Classification System Class II drugs.

Multi-component Crystal Strategy for Improving Water Solubility and Antifungal Activity of Climbazole.

The primary problem with climbazole (CLB), a broad-spectrum imidazole antifungal drug, is its low water solubility. In order to increase its water solubility and antifungal activity, three new multi-component crystals were synthesized in this work, and the intermolecular interactions were systematically studied. This work helps to optimize the CLB product formulation and extend its application prospects. In this work, three novel multi-component crystals, CLB-malonic acid (CLB-MA) salt, CLB-succinic acid (CLB-SA) cocrystal and CLB-adipic acid (CLB-AA) cocrystal, were successfully synthesized. And the crystal structure, thermodynamic properties, solubility, dissolution, hygroscopicity, and antifungal activity of the three multi-component crystals were fully characterized by single-crystal X-ray diffraction (SCXRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), dynamic water vapor adsorption (DVS) and powder dissolution tests, etc. The molecular interactions and molecular stacking in multi-component crystals were studied by Hirshfeld surface (HS), molecular surface electrostatic potential (MEP), interaction region indication (IRI) and atom and molecule (AIM) techniques. The results show that the three multi-component crystals have good moisture resistance stability, and their water solubility is 6-22 times that of pure CLB. Meanwhile, the measurement of the minimum inhibitory concentration (MIC) proves that the cocrystal/salt has a stronger antifungal activity than climbazole. Quantum chemistry calculations of crystal structure visualized and quantified the interactions that exist in multi-component crystals, and explored the microscopic mechanisms underlying the different performance of multi-component crystals.

Enhancing the Biodegradability, Water Solubility, and Thermal Properties of Polyvinyl Alcohol through Natural Polymer Blending: An Approach toward Sustainable Polymer Applications.

The escalating environmental crisis posed by single-use plastics underscores the urgent need for sustainable alternatives. This study provides an approach to introduce biodegradable polymer blends by blending synthetic polyvinyl alcohol (PVA) with natural polymers-corn starch (CS) and hydroxypropyl methylcellulose (HPMC)-to address this challenge. Through a comprehensive analysis, including of the structure, mechanical strength, water solubility, biodegradability, and thermal properties, we investigated the enhanced performance of PVA-CS and PVA-HPMC blends over conventional polymers. Scanning electron microscopy (SEM) findings of pure PVA and its blends were studied, and we found a complete homogeneity between the PVA and both types of natural polymers in the case of a high concentration of PVA, whereas at lower concentration of PVA, some granules of CS and HMPC appear in the SEM. Blending corn starch (CS) with PVA significantly boosts its biodegradability in soil environments, since adding starch of 50 w/w duplicates the rate of PVA biodegradation. Incorporating hydroxypropyl methylcellulose (HPMC) with PVA not only improves water solubility but also enhances biodegradation rates, as the addition of HPMC increases the biodegradation of pure PVA from 10 to 100% and raises the water solubility from 80 to 100%, highlighting the significant acceleration of the biodegradation process and water solubility caused by HPMC addition, making these blends suitable for a wide range of applications, from packaging and agricultural films to biomedical engineering. The thermal properties of pure PVA and its blends with natural were studied using diffraction scanning calorimetry (DSC). It is found that the glass transition temperature (Tg) increases after adding natural polymers to PVA, referring to an improvement in the molecular weight and intermolecular interactions between blend molecules. Moreover, the amorphous structure of natural polymers makes the melting temperature ™ lessen after adding natural polymer, so the blends require lower temperature to remelt and be recycled again. For the mechanical properties, both types of natural polymer decrease the tensile strength and elongation at break, which overall weakens the mechanical properties of PVA. Our findings offer a promising pathway for the development of environmentally friendly polymers that do not compromise on performance, marking a significant step forward in polymer science's contribution to sustainability. This work presents detailed experimental and theoretical insights into novel polymerization methods and the utilization of biological strategies for advanced material design.

Injectable Hydrogel of Chitosan-Octyl Itaconate Conjugate Modulates Inflammatory Response.

Itaconic acid and its derivative 4-octyl itaconate (OI) represent a novel anti-inflammatory medication that has demonstrated efficacy in multiple inflammation models because of its minimal side effects. Recently, natural polymers conjugated with small molecule drugs, known as polymer-drug conjugates (PDCs), have emerged as a promising approach to sustained drug release. In this work, we reported an approach to prepare a PDC containing an OI and make it into an injectable hydrogel. Chitosan (CS) was selected for PDC synthesis because of its abundant free amino groups that can be conjugated with molecules containing carboxyl groups by carbodiimide chemistry. We used an ethanol/water cosolvent system to synthesize a CS-OI conjugate via EDC/NHS catalysis. The CS-OI conjugate had improved water solubility and unique anti-inflammatory activity and did not show compromised antibacterial activity compared with unmodified CS. Beta-glycerophosphate (β-GP) cross-linked CS-OI hydrogel exhibited good injectability with sustainable OI release and effectively modulated inflammatory response in a rat model. Therefore, this study provides valuable insights into the design of PDC hydrogels with inflammatory modulatory properties.

GSH-responsive bithiophene Aza-BODIPY@HMON nanoplatform for achieving triple-synergistic photoimmunotherapy

Photoimmunotherapy represents an innovative approach to enhancing the efficiency of immunotherapy in cancer treatment. This approach involves the fusion of immunotherapy and phototherapy (encompassing techniques like photodynamic therapy (PDT) and photothermal therapy (PTT)). Boron-dipyrromethene (BODIPY) has the potential to trigger immunotherapy owing to its excellent PD and PT efficiency. However, the improvements in water solubility, bioavailability, PD/PT combined efficiency, and tumor tissue targeting of BODIPY require introduction of suitable carriers for potential practical application. Herein, a disulfide bond-based hollow mesoporous organosilica (HMON) with excellent biocompatibility and GSH-responsive degradation properties was used as a carrier to load a bithiophene Aza-BODIPY dye (B5), constructing a sample chemotherapy reagent-free B5@HMON nanoplatform achieving triple-synergistic photoimmunotherapy. HMON, involving disulfide bond, is utilized to improve water solubility, tumor tissue targeting, and PD efficiency by depleting GSH and enhancing host-guest interaction between B5 and HMO. The study reveals that HMON’s large specific surface area and porous properties significantly enhance the light collection and oxygen adsorption capacity. The HMON’s rich mesoporous structure and internal cavity achieved a loading rate of B5 at 11 %. It was found that the triple-synergistic nanoplatform triggered a stronger anti-tumor immune response, including tumor invasion, cytokine production, calreticulin translocation, and dendritic cell maturation, eliciting specific tumor-specific immunological responses in vivo and in vitro. The BALB/c mouse model with 4T1 tumors was used to assess tumor suppression efficiency in vivo, showing that almost all tumors in the B5@HMON group disappeared after 14 days. Such a simple chemotherapy reagent-free B5@HMON nanoplatform achieved triple-synergistic photoimmunotherapy.

Discovery of Biphenyl Derivatives to Target Hsp70-Bim Protein-Protein Interaction in Chronic Myeloid Leukemia by Scaffold Hopping Strategy.

Hsp70-Bim protein-protein interaction (PPI) is the most recently identified specific target in chronic myeloid leukemia (CML) therapy. Herein, we developed a new class of Hsp70-Bim PPI inhibitors via scaffold hopping of S1g-10, the most potent Hsp70-Bim PPI inhibitor thus far. Through structure-activity relationship (SAR) study, we obtained a biphenyl scaffold compound JL-15 with a 5.6-fold improvement in Hsp70-Bim PPI suppression (Kd = 123 vs 688 nM) and a 4-fold improvement in water solubility (29.42 vs 7.19 μg/mL) compared to S1g-10. It maintains comparable apoptosis induction capability with S1g-10 against both TKI-sensitive and TKI-resistant CML cell lines in an Hsp70-Bim-dependent manner. Additionally, through SAR, 1H-15N TRSOY-NMR, and molecular docking, we revealed that Lys319 is a "hot spot" in the Hsp70-Bim PPI interface. Collectively, these results provide a novel chemical scaffold and structural insights for the rational design of Hsp70-Bim PPI inhibitors.

Preparation and characterization of nano-emulsion formulations of Asparagus densiflorus root and aerial parts extracts: evaluation of in-vitro antibacterial and anticancer activities of nano-emulsion versus pure plant extract

Objective Preparation and characterization of nano-emulsion formulations for Asparagus densiflorus aerial and root parts extracts. Significance Genus Asparagus is known for its antimicrobial and anticancer activities, however, freeze dried powder of aqueous – alcoholic extract prepared in this study, exhibited a limited water solubility, limiting its therapeutic application. Thus, encapsulation of its phytochemicals into nano-emulsion is proposed as a solution to improve water solubility, and facilitate its clinical translation. Methods the composition of extracts for both aerial and root parts of Asparagus densiflorus was identified by HPLC and LC-MS analysis. Nano-emulsion was prepared via homogenization where a mixture of Castor oil: phosphate buffered saline (10 mM, pH 7.4): Tween 80: PEG 600 in a ratio of 10: 5: 2.5: 2.5, respectively. Nano-emulsion formulations were characterized for particle size, polydispersity index (PDI), zeta potential, TEM, viscosity and pH. Then, the antibacterial and anticancer activities of nano-emulsion formulations versus their pure plant counterparts was assessed. Results The analysis of extracts identified several flavonoids, phenolics, and saponins which were reported to have antimicrobial and anticancer activities. Nano-emulsion formulations were monodispersed with droplet sizes ranging from 80.27 ± 2.05 to 111.16 ± 1.97 nm, and polydispersity index ≤0.3. Nano-emulsion formulations enhanced significantly the antibacterial (multidrug resistant bacteria causing skin and dental soft tissues infections) and anticancer (HuH7, HEPG2, H460 and HCT116) activities compared to their pure plant extract counterparts. Conclusion Employing a nano-delivery system as a carrier for phytochemicals might be an effective strategy to enhance their pharmacological activity, overcome their limitations, and ultimately increase their potential for clinical applications.

Preparation, Characterization, and Oral Bioavailability of Solid Dispersions of Cryptosporidium parvum Alternative Oxidase Inhibitors.

The phenylpyrazole derivative 5-amino-3-[1-cyano-2-(3-phenyl-1H-pyrazol-4-yl) vinyl]-1-phenyl-1H-pyrazole-4-carbonitrile (LN002), which was screened out through high-throughput molecular docking for the AOX target, exhibits promising efficacy against Cryptosporidium. However, its poor water solubility limits its oral bioavailability and therapeutic utility. In this study, solid dispersion agents were prepared by using HP-β-CD and Soluplus® and characterized through differential scanning calorimetry, Fourier transform infrared, powder X-ray diffraction, and scanning electron microscopy. Physical and chemical characterization showed that the crystal morphology of LN002 transformed into an amorphous state, thus forming a solid dispersion of LN002. The solid dispersion prepared with an LN002/HP-β-CD/Soluplus® mass ratio of 1:3:9 (w/w/w) exhibited significantly increased solubility and cumulative dissolution. Meanwhile, LN002 SDs showed good preservation stability under accelerated conditions of 25 °C and 75% relative humidity. The complexation of LN002 with HP-β-CD and Soluplus® significantly improved water solubility, pharmacological properties, absorption, and bioavailability.

The Development and Performance of a Gemini Viscoelastic Surfactant with Tricationic Groups Applied in Unconventional Oil and Gas Reservoir Stimulation

AbstractTo improve water solubility and salt tolerance of viscoelstic surfactants (VESs), modifying the spacer of Gemini VES was adopted and a novel Gemini VES nominated TC‐2OH, with tri‐cationic groups and double hydroxyls on the spacer, was developed. The basic surface activity properties of TC‐2OH and the molecular aggregate behavior stimulated by NaCl or NaSal were measured and analyzed to investigate the mechanism of viscoelastic fluid forming by TC‐2OH solution, and it proved that TC‐2OH is more sensitive to NaSal, compared with NaCl, due to the embedded structure of salicylate. The molecular structure of TC‐2OH imparts excellent solubility to itself, and with the assistance of ethanol, the dissolution time in water can be shortened to within 45 seconds. In addition, oscillation experiments, heat and shear resistant experiments, and drag reduction tests were conducted to study the advantage of NaSal for stimulating the formation of the slickwater compared with NaCl. The slickwater stimulated by NaSal indeed exhibit superior drag reduction and proppant carrying capacity. To effectively disassemble the wormlike micelles for gel breaking, ethylene glycol butyl ether performs better than the hydrocarbons because of its high polarity and water solubility. The gel breaking fluids of slickwater caused extremely low damage to the tight sandstone cores. The successful development of TC‐2OH enables instant preparation of slickwater and variable‐viscosity for fracturing in unconventional reservoirs, which also realizes convenient switching between the slickwater with different viscosity.

Exploring the binding process of lutein with hydroxypropyl-β-cyclodextrin: Multispectral and molecular simulation study

Lutein possesses various biological activities, including antioxidant and benefits for eye health, but its application is hindered by poor water solubility and chemical instability. The study utilized hydroxypropyl-β-cyclodextrin (HP-β-CD) in complexation with lutein to enhance stability. The preparation conditions of the inclusion complex (IC) were optimized using Box-Behnken design (BBD), and the IC binding mechanism was investigated and studied by multispectral and molecular docking techniques. The results indicated that the maximum encapsulation efficiency of 84.92% was obtained when shell-to-core ratio was 1:11 (g: g), stirring speed was 420 rpm, and time was 15 h. Moreover, the microstructure characterization and multispectral analysis indicate the formation of IC, with lutein exhibiting an amorphous structure. The results of molecular docking and molecular dynamics (MD) simulations further demonstrate that lutein and HP-β-CD are bound through electrostatic and hydrophobic interactions. IC exhibits higher stability compared to free lutein under varying temperatures and simulated digestive conditions, and enhance antioxidant activity. IC changes the original crystal form of lutein and improves water solubility, which may be more favorable for human absorption and utilization. Hence, encapsulating lutein with HP-β-CD may offer a promising strategy to enhance its applications in pharmaceuticals and food applications.

In Silico Structural Modeling and Analysis of Physicochemical Properties of Antitumoral QS‐13 Peptide and Its Derivatives in Water and Dimethyl Sulfoxide

ABSTRACTThe NC1 domain of the alpha 4 chain of type IV collagen was previously reported to exert anti‐tumor properties in a melanoma model and to inhibit angiogenesis. The minimal active sequence identified to date comprises 13 amino acids: QKISRCQVCVKYS. Unfortunately, this sequence is not soluble in aqueous media and requires prior dissolution in DMSO. The disulfide bridge (DB) that spontaneously forms in solution between two cysteine residues is crucial for its biological activity. The aim of this article was to study the impact of DMSO on the physicochemical properties of the QS‐13 peptide and to replace hydrophobic amino acids to enhance its water solubility. Using bioinformatics (GROMACS, VMD, and ProtParam) and programming (Python and RStudio) software programs, we demonstrated that DMSO could promote the formation of DBs, but it is not strictly necessary. Among the QS‐13 substituted peptides, some were demonstrated to display similar characteristics to the original peptide. Improved water solubility will make the peptide easier to use in biological studies and facilitate its administration for potential therapeutic applications.

Fabrication of verrucarin-a-loaded zinc oxide nanocomposite for inducing apoptosis in triple-negative breast cancer cells

Due to its low bioavailability and insolubility in water, little is known about the biological effects of Verrucarin-A. Chitosan-coated zinc oxide (ZnO) nanoparticles were employed as a potential nanocarrier to transport Verrucarin-A to its target cells to enhance its bioavailability. Results showed improved water solubility, entrapment, drug release, and loading efficiencies for the fabricated Verrucarin-A clocked ZnO- nanocomposite (Ver-A@ZnNCs). Comparing Ver-A@ZnNCs to both non-cancerous epithelial (MCF-10A) cells and triple-negative breast cancer (MDA-MB-231) cells in an in vitro cell viability test (MTT), the latter showed greater biocompatibility. According to observations, verrucarin-A release from Ver-A@ZnNCs at cancer cell sites may be caused by the acidic tumor microenvironment. Apoptosis occurred in the cancer cells after increased nanoparticle uptake, which may have stimulated ROS generation. Further evidence of Ver-A@ZnNCs' in vitro anticancer activity was obtained through apoptosis investigations. After performing significant in vitro studies, it has been shown that Ver-A@ZnNCs is compatible with humanity and shows promise as an anticancer drug for triple-negative breast cancer patients.

A biologically inspired fluorescent probe with enhanced sensing performance for detection of Al3+ based on metal replacement strategy

Salicylaldehyde acyl-hydrazone derivatives have been widely applied to design fluorescent probe for Al3+ detection, but they are always restricted to detect Al3+ in water and actual samples by their poor solubility, low sensitivity, and long response time. Biologically inspired, four salicylaldehyde acyl-hydrazone compounds were designed and synthesized and H4L1 as one of them was selected for in-situ assembly of the ytterbium complex (FP-Al), which has been developed to be a new fluorescent probe for Al3+ detection by the central mental displacement process. The in-situ structure transformation from FP-Al to Al-L was fully characterized by X-ray crystal structure analysis, 1H NMR, FT-IR, and spectral analysis. The intrinsic driving force was explained and elaborated by theoretical calculation. FP-Al showed a significant visible fluorescence enhancement and near-infrared luminescence decreased upon the addition of Al3+. Compared with the ligand H4L1, FP-Al showed enhanced sensing performance during Al3+ detection, especially in improving water solubility and selectivity to Al3+, promoting response speed, reducing background fluorescence and increase cell-membrane permeability. The application of spontaneous metal replacement reaction might be able to provide a new strategy to develop high-performance optical chemo-sensors.

Immobilization of Horseradish Peroxidase onto Montmorillonite/Glucosamine-Chitosan Composite for Electrochemical Biosensing of Polyphenols.

Glucosamine-chitosan synthesized by the Maillard reaction was combined with montmorillonite to obtain a nanohybrid composite to immobilize horseradish peroxidase. The material combines the advantageous properties of clay with those of the chitosan derivative; has improved water solubility and reduced molecular weight and viscosity; involves an eco-friendly synthesis; and exhibits ion exchange capacity, good adhesiveness, and a large specific surface area for enzyme adsorption. The physicochemical characteristics of the composite were analyzed by infrared spectroscopy and X-ray diffraction to determine clay-polycation interactions. The electrochemical response of the different polyphenols to glassy carbon electrodes modified with the composite was evaluated by cyclic voltammetry. The sensitivity and detection limit values obtained with the biosensor toward hydroquinone, chlorogenic acid, catechol, and resorcinol are (1.6 ± 0.2) × 102 µA mM-1 and (74 ± 8) nM; (1.2 ± 0.1) × 102 µA mM-1 and (26 ± 3) nM; (16 ± 2) µA mM-1 and (0.74 ± 0.09) μM; and (3.7± 0.3) µA mM-1 and (3.3 ± 0.2) μM, respectively. The biosensor was applied to quantify polyphenols in pennyroyal and lemon verbena extracts.