Low Water Solubility Research Articles

Nano-based Herbal Medicine: A New Candidate for Prostate Cancer Treatment?

Background: Prostate cancer (PCa) is known as the fifth reason for cancer-related deaths and involves a considerable population of men globally. In PCa, pluriform neoplasm with different cancer patterns is formed. Metastases have a substantial role in disease mortality, and lung, liver, and bone are among the common organs for metastasis. In spite of multiple attempts by researchers, it has not been recommended a safe and suitable approach against PCa so far. Results: Fortunately, herbal remedies have opened a novel window in order to treat several cancers, such as PCa; however, there are some barriers regarding this curative method, like low bioavailability and absorption and low water solubility. On the contrary, some nano-based formulations have revealed a potential ability to overcome these limitations, and it seems that the co-use of herbal products and nanoformulations provides a good opportunity for treating PCa. Conclusion: In this study, we argued about the therapeutic aspects of some nanoformulations of popular herbal products, such as curcumin, quercetin, and resveratrol, against PCa.

Preparation of disulfiram-Cu2+-polylactide nanofibrous membranes via electrostatic spinning and evaluation of their in vitro anticancer effects

The antitumor effects of disulfiram (DSF) —a conventional medication used to treat alcohol dependence—have been documented in numerous studies. However, because of its low water solubility and Cu2+-dependent anticancer effects, the application of DSF in cancer therapy has been limited. Nanofibrous membranes produced via electrospinning have large specific surface areas. Consequently, they have been extensively used in biomedical applications, such as tissue scaffolding, drug delivery. In this study, a polylactic acid nanofibrous membrane was designed to encapsulate Cu2+ and DSF. The encapsulated drug was released when the membranes came into contact with the tumor tissue. DSF functioned as a Cu-ion carrier and combined with Cu2+ to induce tumor-cell apoptosis. The anticancer properties of the drug-loaded nanofibrous membrane were verified at the cellular level using in vitro experiments with cells. The results indicated that DSF and Cu2+ were released from the fiber membrane, and the combination of DSF and Cu2+ exhibited a better of cancer are proposed.

Synthesis and characterization of clove residue-derived carbon quantum dots: Application in Pickering emulsion with enhanced antibacterial properties

Clove essential oil exhibits excellent antibacterial properties; however, its application is limited by low water solubility. To overcome this, solid particle-based Pickering emulsions have been explored. Carbon quantum dots (CQDs), which are promising solid particles for food applications, have not been studied regarding their synthesis from residual biomass for forming Pickering emulsions. This study aimed to synthesize CQDs from clove residue left over after the extraction of essential oil, assess their emulsifying efficacy, and compare their antibacterial properties with those of a traditional emulsion employing Polysorbate 80 as a surfactant. Four types of CQDs were synthesized using ultrapure distilled water and ethanol, with analyses such as 1H NMR, XPS, and interfacial tension confirming that CQDs synthesized with 40 % ethanol were the most effective as emulsifying agents. Additionally, the unique characteristics of CQDs rendered the Pickering emulsion’s surface relatively rough, which enhanced its interaction with bacteria and demonstrated potent antibacterial effects through disruption of the cell membrane. Consequently, this study suggests that the emulsifying efficiency and properties of Pickering emulsions can be tailored by controlling the surface properties of the solid particles.

Preparation and characterization of polyphenol–chitosan conjugate–eugenol essential oil microcapsule and its effect on storage behavior of cherry tomato

AbstractGiven the high volatility, low water solubility, and oxidative sensitivity of essential oils, this study synthesized microcapsules of essential oil (EEO) (quercetin–chitosan–EEO [QE–CS–EEO]) using a QE–CS graft copolymer as the wall material and EEO as the core material. Research findings indicate that QE–CS exhibits superior in vitro antioxidant activity, with scavenging abilities for 2,2‐diphenyl‐1‐picrylhydrazyl and 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid) ABTS+ radicals being 58.71% and 77.03% greater than those of CS, respectively, thereby providing more effective protection for the essential oil. In comparison to CS essential oil, microcapsules (CS–EEO), QE–CS–EEO demonstrated an 18.65% increase in EEO encapsulation efficiency, achieving a total encapsulation efficiency of 41.29%. Based on these results, various edible coating solutions were formulated, including Control, E1 (1% CS), E2 (0.5% CS + 0.5% CS–EEO), E3 (0.5% CS + 0.5% QE–CS–EEO), and E4 (1% EEO), to extend the shelf life of cherry tomatoes. Notably, cherry tomatoes treated with the E3 formulation maintained superior freshness indicators, exhibiting an extended shelf life of approximately 9–12 days compared to the control group. This study aims to explore a novel microcapsule wall material and provide a strategy for extending the shelf life of fruits and vegetables, thereby minimizing food waste.

Are Nanostructured Lipid Carriers (NLC) better than Solid Lipid Nanoparticles (SLN) for delivering abiraterone acetate through the gastrointestinal tract?

Abiraterone acetate (AbA) is a progesterone derivative indicated for the treatment of metastatic prostate cancer. This BCS (Biopharmaceutics Classification System) Class IV molecule has an extremely poor oral bioavailability (<10 %), notably due to its very low water solubility and intestinal permeability. Among the few existing galenic strategies to improve AbA’s oral bioavailability, lipid nanoparticles such as Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) are relevant nanovectors. The objective of this study is to develop and compare SLN and NLC for oral delivery of abiraterone acetate. Both SLN and NLC are biocompatible, biodegradable and produced by high pressure homogenization (HPH), an ecological-friendly manufacturing process, organic solvent-free and easily scalable. The HPH process allowed the formation of AbA-loaded SLN and NLC with particle size lower than 160 nm and high encapsulation efficiencies. The addition of a liquid lipid significantly reduced the mean diameter of the nanoparticles, reflecting the greater benefit of the NLC formulation compared to SLN. Both SLN and NLC formulations offered an important protection of AbA in intestinal media, with a better stability for NLC. When encapsulated in SLN or NLC, the AbA is strongly retained by the nanoparticles, whatever the dissolution medium, which means that both formulas are able to protect and retain the drug in the intestinal tract, right up to its delivery to the enterocytes surface. High concentrations of nanoparticles were administered without cytotoxicity, especially for the NLC, which provides a real added value in terms of biocompatibility with Caco-2 cells. Finally, the nanoparticles were able to penetrate into enterocytes by the transcellular route, demonstrating an intense cellular internalization.

SUSTAINABLE AND SCALABLE ENZYMATIC PRODUCTION, STRUCTURAL ELUCIDATION, AND BIOLOGICAL EVALUATION OF NOVEL PHLORIZIN ANALOGUES.

It is not unusual for naturally occurring compounds to be limited for their use in cosmetics due to their low water solubility. Recently, aiming at accessing novel phlorizin analogues, we reported the synthesis of very promising - but low water-soluble - biomass-derived chalcones (CHs) and dihydrochalcones (DHCs) exhibiting antioxidant and anti-tyrosinase activities. Glycosylating bioactive compounds being one of the most common strategies to increase water solubility, herein we report the enzymatic glycosylation of the aforementioned CHs, as well as DHC, using cyclodextrin glycosyltransferases (CGTase), enzymes well-known for catalyzing the selective ⍺(1→4)transglycosylation. Indeed,while most natural glycosides areβ-glycosides (such as phlorizin), the selected enzyme produces selectively newα-glycosides, thus expanding their structural diversity. A first separation using Centrifugal Partition Chromatography (CPC) led to mono-, di- or triglycosides-enriched fractions, which were then submitted to a comprehensive purification strategy for an in-depth chemical profiling of the synthesizedα-glycosides, revealingas major compounds. Surprisingly, among the diglycosides characterized, besides the expected maltoside compounds, nigeroside derivatives were also identified in significant amounts, depending on the starting compound structure. Finally, evaluating the antiradical, anti-tyrosinase and antimicrobial activities of the major glycosides revealed them as potential sustainable alternatives to current petro-sourced cosmetic ingredients.

Enhancing the solubility and antibacterial activity of novel molecular salts of enrofloxacin drug with isomeric pyridinedicarboxylic acids

Enrofloxacin (EFX) is a third-generation synthetic fluoroquinolone with a broad spectrum of antibacterial activity but suffers from low water solubility, affecting its bioavailability. This study attempts to enhance the physicochemical and biological properties of enrofloxacin by converting it into multicomponent forms using crystal engineering concepts. Cocrystallization of enrofloxacin with isomeric pyridine-2,n-dicarboxylic acids (n = 3,4,5,6) resulted in four new crystalline salts (1:1): EFX·Py2,3DCA, EFX·Py2,4DCA, EFX·Py2,5DCA·H2O and EFX·Py2,6DCA·H2O; two of these are monohydrates. The protonation of the nitrogen atom of the piperazine moiety and the presence of crystallization water molecules were confirmed by single-crystal X-ray diffraction and Fourier transform infrared spectroscopy. Thermogravimetric analysis provided information on the thermal behaviour of multicomponent forms. The biological studies showed that the obtained salts are characterized by high antibacterial activity against Gram-positive and Gram-negative bacteria, and their haemolytic activity is low. The new salts demonstrate significantly greater solubility in water compared to the parent drug, along with enhanced antibacterial activity; hence, pyridinedicarboxylic acids appear to be efficient cocrystallizing agents for improving the efficacy of pharmaceutical ingredients.

A Comprehensive Review on the Impact of Hesperidin and Its Aglycone Hesperetin on Metabolic Dysfunction-Associated Steatotic Liver Disease and Other Liver Disorders.

The purpose of this review is to examine the effects of hesperidin and hesperetin on liver disorders. Metabolic dysfunction-associated steatotic liver disease is a complicated disorder influenced by many factors such as inflammation, diabetes, and obesity. Currently, the most prominent treatment method is lifestyle changes. If left untreated, it can progress to cirrhosis, liver fibrosis, and liver cancer. Hesperidin, which is a flavanone glycoside polyphenolic plant compound, belongs to the flavanone class and was first isolated from citrus peel. Hesperidin includes aglycone hesperetin and rutinoside sugar. It is the most dominant form of flavonoid in citrus fruits. In our review, we discussed the effects of these phytochemicals on liver diseases, focusing on their relationship with inflammation, blood sugar regulation, and blood lipids. Hesperidin and hesperetin are seen as promising agents for many diseases. Their antioxidant and anti-inflammatory properties support this view. Although their low water solubility limits their potential effects, many studies have demonstrated their benefits. They are thought to play an effective role in inflammatory processes, particularly in liver diseases ore studies are required to find the optimum dosage and to use them as a therapeutic agent for the liver.

High cell density cultivation by anaerobic respiration

BackgroundOxygen provision is a bottleneck in conventional aerobic high cell density culturing (HCDC) of bacteria due to the low O2 solubility in water. An alternative could be denitrification: anaerobic respiration using nitrogen oxides as terminal electron acceptors. Denitrification is attractive because NO3− is soluble in water, the end-product (N2) is harmless, and denitrification is widespread among bacteria, hence suitable organisms for most purposes can be found. The pH must be controlled by injection of an inorganic acid to compensate for the pH increase by NO3−-consumption, resulting in salt accumulation if feeding the bioreactor with NO3− salt. We avoid this with our novel pH–stat approach, where the reactor is supplied with 5 M HNO3 to compensate for the alkalization, thus sustaining NO3−-concentration at a level determined by the pH setpoint. Here we present the first feasibility study of this method, growing the model strain Paracoccus denitrificans anaerobically to high densities with glucose as the sole C-source and NO3− as the N-source and electron acceptor.ResultsOur fed-batch culture reached 20 g cell dry weight L−1, albeit with slower growth rates than observed in low cell density batch cultures. We explored reasons for slow growth, and the measured trace element uptake indicates it is not a limiting factor. Bioassays with spent medium excluded accumulation of inhibitory compounds at high cell density as the reason for the slow growth. The most plausible reason is that high metabolic activity led to CO2/H2CO3 accumulation, thus suppressing pH, leading to a paucity in HNO3-feeding until N2-sparging had removed sufficient CO2. The three free intermediates in the denitrification pathway (NO3− → NO2− → NO → N2O → N2) can all reach toxic concentrations if the electron flow is unbalanced, and this did occur if cells were glucose-limited. On the other hand, accumulation of polyhydroxyalkanoates occurred if the cells were NO3−-limited. Carefully balancing glucose provision according to the HNO3 injected is thus crucial.ConclusionsThis work provides a proof of concept, while also identifying CO2/H2CO3 accumulation as a hurdle that must be overcome for further development and optimization of the method.

Natural borneol improves cellular uptake of curcumin to enhance its photodynamic bactericidal activity against Escherichia coli ATCC 8739

Photodynamic inactivation (PDI), a non-thermal sterilization method, has attracted considerable attention due to its broad-spectrum antimicrobial activity, environmental friendliness and cost-effectiveness. Curcumin (Cur), a food-grade photosensitizer, exhibits photodynamic antimicrobial activity based primarily on its efficiency in intracellular accumulation. However, Cur's low water solubility and the barriers presented by the outer membrane of Gram-negative bacteria challenge its ability to penetrate the cytoplasm. Natural borneol (NB), a monoterpene food flavoring agent, has also been shown to improve the efficiency of drug absorption. In this study, we demonstrated that NB significantly improved the cellular uptake of Cur, thereby enhancing its photodynamic bactericidal activity against Gram-negative Escherichia coli (E. coli) ATCC 8739, a potential alternative to enterohemorrhagic E. coli O157:H7. This effect was attributed to NB's ability to disrupt the integrity of the E. coli bacterial membrane, thereby increasing cellular permeability. Transcriptomic analysis further confirmed that NB dysregulated the expression of genes associated with bacterial membrane structure and function in E. coli. Consequently, the increased accumulation of Cur in E. coli led to excessive production of intracellular reactive oxygen species (ROS) upon exposure to 6.5 J/cm2 blue light (BL). These ROS, analyzed biochemically and transcriptionally, primarily disrupted bacterial membrane structure and function, the antioxidant system, and ultimately caused bacterial death. Remarkably, this combined strategy not only reduced E. coli contamination in the tested orange juice, but also preserved its nutritional quality. In conclusion, this research provides an innovative and effective approach to maintaining food safety.

Structural, DFT, Molecular Docking and Biological Activity of New Albendazole-Norfloxacin Mixed-Ligand Complexes: Promising Metal Complexes for Combating Microbial Resistance and Inflammation.

This study presents a comprehensive characterization of the Fe(III) (C1) and Co(II) (C2) complexes that were synthesized from the Albendazole (Alb) and Norfloxacin (Nor) ligands. The complexes exhibit remarkable thermal stability, low water solubility, and a non-electrolytic nature, characteristics that enhance their suitability for diverse applications. Conductivity measurements indicate molar conductivities of 9.85 and 8.59 Ω-1cm2mol-1, confirming their status as neutral molecules. Fourier Transform Infrared (FTIR) spectroscopy reveals significant ligand-metal interactions, marked by shifts in vibrational frequencies that confirm chelation, while Ultraviolet-Visible (UV-Vis) spectroscopy supports the identification of octahedral geometries for both complexes. Magnetic moment assessments align with their electronic configurations, and stoichiometric analysis consistently shows a 1:1:1 ratio, further validated by mass spectrometry. Thermal stability studies highlight anhydrous characteristics and distinct thermal decomposition behaviors, underscoring their structural integrity. Employing Density Functional Theory (DFT) calculations using the B3LYP functional, we evaluate the electronic properties of the ligands and their metal complexes, revealing reduced energy gaps (ΔE) of 2.29eV for C1 and 2.15eV for C2, significantly lower than those of the ligands (Alb: 4.61eV, Nor: 4.17eV), indicating enhanced reactivity and potential biological activity. Additionally, molecular electrostatic potential (MEP) maps provide insights into charge distributions, suggesting critical regions for interactions with biomolecules. Notably, the results demonstrate that metal coordination significantly enhances antibacterial/anti-fungal activity surpassing both the free ligands and the standard antibiotic Ofloxacin/Fluconazole. Furthermore, the complexes show significant improvement in anti-inflammatory activity by inhibiting protein denaturation more effectively than their ligand counterparts. Molecular docking studies reveal stronger binding affinities and interactions with antimicrobial target proteins 1HNJ and 5IKT, attributed to enhanced hydrophobic interactions and hydrogen bonding. These findings position C1 and C2 as promising candidates for developing effective antimicrobial therapies, highlighting the crucial role of metal ions in enhancing biological reactivity and addressing resistant strains of pathogens.

Natural compounds in the fight against Staphylococcus aureus biofilms: a review of antibiofilm strategies.

Staphylococcus aureus is an important pathogen due to its ability to form strong biofilms and antibiotic resistance. Biofilms play an important role in bacterial survival against the host immune system and antibiotics. Natural compounds (NCs) have diverse bioactive properties with a low probability of resistance, making them promising candidates for biofilm control. NC such as curcumin, cinnamaldehyde, carvacrol, eugenol, thymol, citral, linalool, 1,8-cineole, pinene, cymene, terpineol, quercetin, and limonene have been widely utilized for the inhibition and destruction of S. aureus biofilms. NCs influence biofilm formation through several procedures. Some of the antibiofilm mechanisms of NCs are direct bactericidal effect, disrupting the quorum sensing system, preventing bacteria from aggregation and attachment to surfaces, reducing the microbial surface components recognizing adhesive matrix molecules (MSCRAMMs), interfering with sortase A enzyme, and altering the expression of biofilm-associated genes such as icaADBC, agr, and sarA. Furthermore, these compounds affect extracellular polymeric substances (EPS) and their components, such as polysaccharide intercellular adhesin (PIA) and eDNA. However, some disadvantages, such as low water solubility and bioavailability, limit their clinical usage. Therefore, scientists have considered using nanotechnology and drug platforms to improve NC's efficacy. Some NC, such as thymol and curcumin, can also enhance photodynamic therapy against S. aurous biofilm community. This article evaluates the anti-biofilm potential of NC, their mechanisms of action against S. aureus biofilms, and various aspects of their application.

Boosting Tumor Accumulation of Phthalocyanine through Sialylation Engineering for Superior Cancer Phototherapy

AbstractPhthalocyanines (Pcs) are widely developed in cancer phototherapy due to their definite chemical structure and tunable photosensitivity. However, their in vivo application is hampered by low water solubility and non‐specific biodistribution. Here,a strategy of sialylation‐modulation is developed for the first time to highly improve the bioavailability of Pcs. The sialylated Pcs (ZnPc‐4SA) not only has good hydrophilicity, but also can self‐assemble into nanoparticles (ZnPc‐4SA NPs). These nanoformulations retain the excellent photophysical properties of Pcs, which in turn reflects excellent optoacoustic and phototherapeutic properties. Importantly, ZnPc‐4SA NPs exhibit boosted tumor accumulation due to the passive targeting and sialic acid‐mediated E‐selectin targeting. Besides, the phototoxicity of ZnPc‐4SA NPs can effectively trigger cell apoptosis and tumor elimination upon laser irradiation. Therefore, sialylation engineering strategy provides a new option for hydrophobic drugs modification with enhanced tumor theranostics.

Development of a Water-Soluble Nanomicellar Formulation Loaded with Trans-Resveratrol Using Polyethylene Glycol Monostearate for the Treatment of Intracerebral Hemorrhage.

Background/Objectives: Trans-resveratrol (Res) has been reported to possess many biological activities, including neuroprotective effects, owing to its anti-inflammatory and antioxidant properties. However, Res has very low water solubility, which limits its therapeutic application. In this work, we formulated water-soluble micellar formulations incorporating Res using polyethylene glycol monostearate (stPEG). Methods: These formulations (stPEG/Res) were developed using five types of stPEG containing 10, 25, 40, 55 and 140 PEG repeat units. The formulations were characterized for Res content, water solubility, particle size, zeta potential, precipitation, biodistribution, and efficacy against neuronal and motor dysfunction in intracerebral hemorrhage (ICH). Results: Intravenous administration of stPEG40/Res, which demonstrated particle size, water solubility, and biodistribution properties suitable for intravenous administration, suppressed neurological and motor dysfunction following in a collagenase-induced ICH mouse model. These effects were inhibited by zinc protoporphyrin-9, an inhibitor of the antioxidant enzyme heme oxygenase-1, suggesting that Res contributes to antioxidant enzyme expression and anti-inflammatory activity. Conclusions: The stPEG/Res micellar formulation developed in this study may offer a promising therapeutic approach for ICH treatment.

Preparation, Characterization, and Cytotoxicity Study of Nitrogen-Doped Graphene Quantum Dots Functionalized Hyaluronic Acid Loaded with Docetaxel-Catalyzed Nanoparticles for Breast Cancer Imaging and Targeting In Vitro

Many women worldwide are impacted by breast cancer that also claims many lives every year. Docetaxel (DOC) is the natural chemotherapeutic agent used most commonly for the treatment of breast cancer. However, it has some drawbacks including low water solubility, a long half-life, an unregulated rate of discharge from the target site, etc. The objective of our present research reported here was to formulate DOC-loaded hyaluronic acid (HA)-functionalized nitrogen-doped graphene quantum dots (N-GQDs) nanoconjugate (DOC@HA-SDH-NGQDs) by using the adhesive properties of succinic acid dihydrazide (SDH) as a hopeful nanocarrier system for potential breast cancer imaging and targeting. The prepared DOC@HA-SDH-NGQDs nanoparticles (NPs) demonstrated 87.58 % drug loading, 97 % drug release, and −14.5 zeta potential indicating excellent stability. The outcomes of our MTT assay showed the full biocompatibility of the produced nanoconjugate and the significant reduction in MCF7 breast cancer cell viability observed in samples of DOC-loaded HA-SDH-NGQDs NP when we compared to other formulations. The MCF7 cancer cell line was found to respond better to the DOC@HA-SDH-NGQDs nanocomposite than to the standard drug, according to the cellular uptake studies. Conclusively, our described study, we believe, is the first to describe HA-NGQDs nanotherapeutics (NTCs) with the added adhesive qualities of SDH for breast cancer imaging and treatment via pH-triggered targeted anticancer drug delivery.

Mechanistic characterization of fast dissolving PVP-I powder with multipolymer approaches and investigation on their molecular interaction

Povidone-iodine (PVP-I) is widely used as an antiseptic in medical applications. However, its effectiveness is limited by certain drawbacks, such as low solubility in water and high volatility. Therefore, a formulation of a stable solid PVP-I is desirable. In this study, complexes of molecular PVP-I with polyethylene glycol-polyvinyl alcohol copolymer (PEG-PVA copolymer) were considered water-soluble iodophors. Two different methods were used to prepare the solids: physical mixtures and kneading. The physical characteristics of the obtained solids were evaluated using several spectroscopic methods. The presence of iodine was confirmed by a potentiometric titration and antimicrobial activity was tested. The results showed that the PEG-PVA copolymer interacted with povidone primarily through hydrogen bonding between the hydroxyl part of the PEG-PVA copolymer and the amide part of povidone with an estimated binding energy of 3.2 kcal/mol. The amide groups polarity in povidone made them more likely to form hydrogen bonds with the PEG-PVA copolymer. Also, the protonated pyrrolidone bonded to the triiodide anions by intermolecular hydrogen bonds, which increased PVP-I solubility in water. The kneading method provided a faster dissolution rate than physical mixing and pure PVP-I. The iodine contents were within an acceptable range (10-12%), and the antimicrobial activity proved effective against Staphylococcus aureus, Staphylococcus epidermidis, and Streptococcus mutans.

Outer-surface adduct formation and selective separation of cis-type gallated and cis-type non-gallated catechins using cucurbit[7]uril.

We found that cis-type gallated and non-gallated catechins form low water solubility outer-surface adducts with cucurbit[7]uril in aqueous solution, with cis-type gallated catechins showing a higher tendency to precipitate as outer-surface adducts. By exploiting this phenomenon, we achieved the selective separation of cis-type gallated and non-gallated catechins in solution.

Enhanced chemiluminescence with sub-1 nanometer CuO-PMA nanosheets for the sensitive detection of quercetin

BackgroundChemiluminescence (CL) analysis, characterized by its simple instrumentation, high signal-to-noise ratio, wide linear range, and minimal background interference, has garnered increasing attention from researchers. Nanomaterials (NMs) have been explored to enhance CL intensity. Notably, sub-1 nanometer scale NMs are considered to hold significant untapped potential due to their size effects. The application of these sub-1 nanometer NMs in enhancing CL is anticipated to yield favorable results. Additionally, the low water solubility and bioavailability of quercetin glycosides lead to their presence in bodily fluids at only trace levels, highlighting the urgent need for efficient and rapid detection methods. ResultsIn this work, phosphomolybdic acid (PMA) was incorporated into CuO to synthesize sub-1 nanometer CuO-PMA nanosheets (SNSs) using a cluster-core co-assembly strategy. Conformational and structural characterization confirmed the successful synthesis of these nanosheets. The CuO-PMA SNSs were employed to enhance the CL emission of the luminol-H2O2 system, resulting in an increase of over 1000 times. The catalytic properties of CuO-PMA SNSs significantly facilitated the decomposition of H2O2, leading to an enhanced production of reactive oxygen species, which in turn induced the CL enhancement. Given that the antioxidant effect of quercetin would consume the reactive oxygen species generated during the catalysis, a decrease in CL intensity was anticipated. A CL sensor for quercetin detection was developed based on the CuO-PMA SNSs-luminol-H2O2 system, demonstrating a strong linear relationship (R2 = 0.9969) and a low detection limit of 0.31 nM. SignificanceThis research provides a strategy to enhance the CL intensity of the luminol-H2O2 system by using CuO-PMA SNSs, offering a highly sensitive assay for detecting quercetin concentrations. The method is characterized as a simple and cost-effective analytical strategy making CL analysis very attractive for chemical analysts.

Biocompatible Naringin loaded low molecular peptide Nanogels are effective against human melanoma cells.

Melanoma, a type of cancer, has the ability to metastasize and can be fatal. The lack of success in the treatment of melanoma with chemotherapeutic agents and the side effects have led to the search for new agents. Moreover, developing systems that will provide reduce side effects by using biocompatible carriers, may be beneficial. Naringin (NAR), from Citrus plants, has anticancer and anti-inflammatory properties. NAR is useful in formulations where it is used with a carrier due to its low water solubility and bioavailability with few toxicity. This study aimed to evaluate the effects of NAR-loaded peptide based Fmoc-FF nanogels on human melanoma (SK-MEL-30) cells. Characterization of NAR-loaded Fmoc-FF nanogels was carried out. The biocompatibility properties of Fmoc-FF and NAR-loaded nanogels were evaluated in mouse fibroblast (L929) cells, and their cytotoxic effects were evaluated in human melanoma (SK-MEL-30) cells by the MTT method. While the DCF-DA method was used to measure the effects on reactive oxygen species (ROS) release, the changes in oxidative stress biomarkers were examined by spectrophotometric analysis, tyrosinase enzyme activity and inflammation biomarkers were investigated by ELISA method. Comet method was used to evaluate antigenotoxic effects. It has been observed that loading NAR into Fmoc peptide gels may be effective in causing cytotoxic, genotoxic, anti-inflammatory and anti-tyrosinase effects and an increase in ROS release in melanoma cells. These results indicate that NAR-loaded Fmoc-FF gels, which have the feature of easy application to the skin, may be effective in the treatment of melanoma without causing toxic effects.

The Application and Pharmaceutical Development of Etomidate: Challenges and Strategies.

Etomidate is a synthetic imidazole anesthetic that exerts hypnotic effects by potentiating the action of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) or directly activating the anionic GABA (GABAA) receptor. It stands out among many anesthetics because of its multiple advantages, such as good hemodynamic stability and minimal inhibition of spontaneous respiration. However, its low water solubility and side effects, such as adrenal cortex inhibition and myoclonus, have limited the clinical application of this drug. To address these issues, extensive research has been conducted on the drug delivery of etomidate in recent decades, which has led to the emergence of different etomidate preparations. Despite so many etomidate preparations, so far some of the toxic side effects have not yet been effectively addressed. Herein we discuss the pharmaceutical design of etomidate that may resolve the above problem. We also propose targeted strategies for future research on etomidate preparations and discuss the feasibility of different administration routes and dosage forms to expand the application of this drug. Through this review, we hope to draw more attention to the potential of etomidate and its application challenges and provide valuable insights into the development of new etomidate preparations.