Abstract Aim Using natural ingredients in cosmetics, such as sunscreen, offers a promising approach to creating more environmentally sustainable products. This study aimed to evaluate the feasibility of formulating a sunscreen body lotion containing tangerine oil by assessing its quality, stability, SPF value, and consumer acceptance. Materials and Methods The study involved phytochemical screening and chemical compound identification using gas chromatography-mass spectrometry (GC-MS). Antioxidant activity was measured using the DPPH method. Additional tests included organoleptic evaluation, homogeneity, pH, viscosity, spreadability, adhesion, emulsion type, particle size, functional group identification, SPF determination, accelerated stability testing (heating–cooling cycles), and hedonic testing. Results D-limonene was identified as the dominant compound in tangerine oil. It showed weak antioxidant activity, with an IC 50 value of 72,015.29 ppm and an antioxidant activity index (AAI) of 0.007. All five formulations met the required quality standards. The highest SPF value (13.59) was achieved by the formulation containing 3% TiO 2 and 9% tangerine oil, measured in vitro using a UV–Vis spectrophotometer. Stability testing over six heating–cooling cycles confirmed that all formulations remained stable. In hedonic testing, formula F4 (3% TiO 2 and 12% tangerine oil) was the most preferred by panelists. Conclusions Although tangerine oil exhibited negligible antioxidant activity, the study successfully developed stable body lotion formulations that met quality requirements, provided maximum sun protection, and were well accepted by users.
The present study aimed to develop and optimize posaconazole-conjugated graphene (PCZ-G) microgel for the treatment of cutaneous infections caused by fungus Aspergillus niger (A. niger). The Box–Behnken experimental design with three levels, three factors, and three center points was applied for optimization of PCZ-G microgel. Particle size (PS), polydispersity index (PDI), and entrapment efficiency were the three outputs utilized in the design matrix associated with Box–Behnken design (BBD), containing 17 runs. Three-dimensional response surface plots and contour plots have been generated using Stat Ease 360 software. On the optimized preparation, assessments were conducted on drug content, %CDR, PDI, PS, percentage entrapment efficiency (EE%), and in vitro antifungal activity. The optimized formulation of PCZ-G microgel showed a particle size of 1506 nm, an entrapment efficiency of 97.08±3.69%, a drug content of 94.43±1.09%, and other parameters all within the range of the model. In vitro release study showed prolonged drug release from the optimized formulation. Drugs and excipients were well integrated and physically stable in the designed microgel, which showed significant antifungal activity against A. niger.
Free radicals are important reactive species that perform both positive and negative functions within living organisms. Antioxidants play a significant part in preventing or managing diseases linked to oxidative stress, including cancer, cardiovascular disease, and neurodegenerative disorders. In the presented work, a two-step synthesis was used to prepare 15 phenolic compounds substituted with various N-heterocyclic moieties as potential antioxidants. The starting materials were 4-hydroxyphenylalkyl ketones, which were converted into 4-hydroxy-3-chloromethylphenylalkyl ketones via chloromethylation. These then reacted with various aliphatic amines (dimethylamine, diethylamine, isopropylamine, isobutylamine, and tertbutylamine) and heterocyclic amines (pyrrolidine, piperidine, morpholine, azepane, and 4-methylpiperazine). The purity of the products was confirmed by thin-layer chromatography, and their infrared (IR), ultraviolet (UV), and proton nuclear magnetic resonance (1H NMR) spectra were measured. Their antioxidant activity was determined using the DPPA and ABTS methods. The ABTS results show antioxidant activity values ranging from 85% to 95%, which are higher than the values for oxygen derivatives. Conformational analysis revealed a stronger hydrogen bond between OH and N than between OH and O. In the case of the compound containing isobutyl, the formation of an intramolecular hydrogen bond (NH⋯O) is considered more likely.
Chronic wounds are frequently complicated by bacterial biofilm formation, which significantly impairs healing and reduces the effectiveness of antimicrobial therapy. The aim of this study was to evaluate the efficacy of commonly used topical antimicrobial agents against multidrug-resistant wound pathogens in relation to the timing of their application and the stage of biofilm development.
Although flucytosine is a powerful antifungal drug, formulation-related issues frequently restrict its clinical usage, and the growing prevalence of invasive fungal infections caused by Candida and Cryptococcus species poses a serious public health problem. This work designed, optimized, and assessed a flucytosine-loaded nanoemulsion using a Box–Behnken experimental design to improve physicochemical stability and antifungal activity. Pre-formulation studies confirmed the purity, crystallinity, and compatibility of flucytosine with selected excipients. A total of 17 nanoemulsion formulations were prepared by varying the oil concentration, surfactant–co-surfactant (Smix) ratio, and homogenization time, with particle size, polydispersity index (PDI), and entrapment efficiency (%EE) as key responses. The optimized formulation (F7) exhibited a small droplet size (~104 nm), low PDI (<0.3), high entrapment efficiency (~95%), suitable pH, and a stable negative zeta potential, indicating excellent physical stability. Transmission electron microscopy confirmed spherical and uniformly dispersed droplets. In vitro drug release studies demonstrated a sustained release profile over 24 hours, with the optimized formulation showing significantly higher cumulative drug release compared to other batches. Antifungal evaluation against Candida albicans revealed a markedly larger zone of inhibition for the nanoemulsion compared to plain drug solution, indicating enhanced antifungal efficacy. Stability studies conducted under International Council for Harmonisation (ICH) conditions confirmed the formulation's stability over 3 months. Overall, the proposed flucytosine nanoemulsion demonstrated higher antifungal activity, prolonged drug release, better physicochemical features, and good stability, suggesting its potential as a successful antifungal therapeutic delivery method.
This study investigated the chemical diversity of essential oils (EOs) extracted from eight Mentha spicata samples collected across different regions of Iran.
Silver nanoparticles (AgNPs) were synthesized via a green chemistry approach using Melissa officinalis aqueous extract as both a reducing and stabilizing agent. The formation of AgNPs was confirmed visually by a color change from light yellow to dark brown and spectroscopically by a distinct surface plasmon resonance band between 350 and 500 nm. The formulation containing 2 mM AgNO3 and 4% (v/v) extract at pH 8 and 37 °C exhibited optimal nanoparticle formation. Fourier transform infrared (FTIR) analysis revealed the presence of hydroxyl, carbonyl, and amine functional groups, indicating that phenolic and flavonoid compounds acted as reducing and capping agents. Dynamic light scattering (DLS) showed a broad hydrodynamic distribution, while scanning electron microscopy (SEM) confirmed that the primary nanoparticles were spherical with an average diameter of approximately 60 nm. X-ray diffraction (XRD) patterns indicated a face-centered cubic crystalline structure. Phytochemical analysis revealed a significant decrease in total phenolic and flavonoid contents following nanoparticle synthesis, confirming their involvement in the reduction and stabilization processes. Antioxidant assays (FRAP and DPPH) demonstrated that AgNPs retained or slightly enhanced activity compared to the crude extract, with FRAP values of 2.23 vs. 1.93 Eq/mg and DPPH inhibition of 86.72% vs. 78.31% at a concentration of 1 mg/mL. Antibacterial testing revealed selective activity against Staphylococcus aureus, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 8 µg/mL and 16 µg/mL, respectively. In contrast, only weak or no activity was observed against Escherichia coli and Proteus mirabilis. Cytotoxicity assays (MTT) on MCF-7 breast cancer cells showed that the M. officinalis extract exhibited greater anticancer activity (IC50 = 32 µg/mL) than the synthesized AgNPs, suggesting reduced bioavailability due to nanoparticle aggregation and lower cellular uptake. Overall, these findings demonstrate that M. officinalis-mediated AgNPs are spherical nanoscale particles (∼60 nm) with confirmed crystallinity, moderate stability, enhanced antioxidant activity, and selective antibacterial effects. Optimization of synthesis parameters could further improve their biomedical potential.
This study focuses on the development and characterization of microemulsion gel systems incorporating the model drug lidocaine. Microemulsions were prepared via the standard phase titration method using various oil phases, surfactants, and co-surfactants, with demineralized water as the aqueous component. The primary objective was to assess the physical properties of the resulting gels and compare their drug release profiles to conventional gel formulations. The study examined the impact of varying surfactant and co-surfactant types, as well as the presence of the active pharmaceutical ingredient, on gel characteristics. Physical properties were evaluated through texture analysis and rheological measurements, while drug release was determined using Franz diffusion cells. Results showed that while the physical properties of microemulsion gels remained largely consistent across formulations, significant differences were observed in lidocaine liberation, highlighting the potential of microemulsion gels to modulate drug release behavior.
Carboxymethyl tamarind gum (CMTG) is an anionic polymer gaining attention for its potential in drug delivery applications. In the present study, composite hydrogel films composed of CMTG and flaxseed mucilage (FSM) were developed for wound dressing applications. According to previous reports, hydrogel films prepared using CMTG alone exhibited poor matrix integrity and limited swelling capacity. To overcome these limitations, FSM was incorporated due to its highly hydrophilic nature, excellent water-holding capacity, and superior swelling characteristics, which are expected to enhance the overall performance of the composite hydrogel films. The composite hydrogel films were prepared by using solvent casting method. The developed hydrogel films were evaluated for weight loss, thickness, carboxyl content, contact angle, and swelling. The hydrogel films were characterized by attenuated total reflectance–Fourier transform infrared (ATR–FTIR) and thermal analysis. The drug loading was initiated by using diffusion mechanism. The drug release was studied in Tris HCl buffer pH 7.4. The physicochemical properties of the hydrogel films, including weight loss, thickness, carboxyl content, and contact angle, were influenced by the concentrations of citric acid and FSM. The optimized films showed enhanced swelling capacity (up to 37.83 g/g), superior to CMTG-alone films. The films were hemocompatible and exhibited minimal protein adsorption (<0.5 %). In addition, they demonstrated favorable water vapor permeability and effectively resisted microbial penetration. Drug release studies with metronidazole revealed a non-Fickian diffusion mechanism. ATR–FTIR and thermogravimetric analyses confirmed crosslinking between CMTG and citric acid, along with entanglement of FSM polymeric chains within the hydrogel matrix. The CMTG–FSM composite hydrogel films offer enhanced performance and biocompatibility, making them promising candidates for wound dressing applications.
Prostate cancer is a disease characterized by unusual uncontrolled growth and proliferation of prostate cells. Docetaxel (DTX) has been associated with reduction in tumor growth, progression, and metastasis. The purpose of this research is to develop nanomedicines of DTX and rubone with effective antitumor activity against prostate cancer cells.
The use of stimuli-responsive gels is increasingly widespread and includes almost all routes of administration. Their main property is the phase transition from sol to gel under the influence of physiological stimuli such as temperature, pH, ion presence, or enzymes. The aim of this formulation study was to prepare oral in situ gel containing silver complex with nicotinamide. We prepared formulations based on the thermosensitive polymer Pluronic® F-127 (15% w/w), methylcellulose (0.25% w/w), and various concentrations of the ion-sensitive polymer sodium alginate (0.2%–4% w/w). Various properties were evaluated, such as pH, injectability, critical sol–gel transition temperature of sols, gelation capacity, as well as dissolution profile and antimicrobial activity. We found that sodium alginate affects the critical sol–gel transition temperature of sols, and with higher concentrations, the sol–gel transition temperature decreases. At a 4% w/w sodium alginate concentration, the presence of calcium cations was necessary for gel formation. Sodium alginate also significantly influenced the viscosity of sols; higher concentrations led to more viscous sols. The most suitable formulation contained 4% sodium alginate and was used to incorporate silver complex with nicotinamide, a new potential antimicrobial agent. The drug release kinetics most closely correlated with the first-order kinetics, and the drug was released via Fickian diffusion. During antimicrobial activity testing, the formulation demonstrated higher efficacy against Pseudomonas aeruginosa compared to a commercial dental gel containing chlorhexidine gluconate, although this difference was not statistically significant. Overall, the chlorhexidine gel showed greater efficacy against most of the tested bacteria, while the antimicrobial in situ gel maintained a consistent moderate level of antimicrobial activity.
Dipsacus fullonum L. (teasel) is a traditional medicinal plant, known to be a supplement in the treatment of Lyme disease. However, its scientific evaluation remains limited. This study investigates the phytochemical composition, antioxidant capacity and antibacterial properties of D. fullonum leaf and root ethanolic extracts. Ultrasound-assisted extraction with 70% ethanol was performed, and the extracts were analysed for total polyphenols, tannins and hydroxycinnamic acids. Antioxidant activity was assessed using the DPPH radical scavenging method, while antibacterial activity was evaluated via the broth microdilution method against various bacterial reference strains. Results indicate that leaf extract contains higher levels of bioactive compounds and exhibits stronger antioxidant activity than root extract. A combination of both extracts showed an additive effect. The leaf extract displayed weak antibacterial activity against selected Gram-positive and Gram-negative bacteria, whereas the root extract demonstrated no antibacterial effects.
Type 2 diabetes mellitus (T2DM), a degenerative disease characterized by insulin resistance, has been reported as a serious healthcare problem, especially in low-to-middle-income countries. Dipeptidyl peptidase IV (DPP4) inhibition is a potential solution to overcome T2DM-related problems. Liberica coffee (Coffea liberica) was reported to have several health benefits due to the bioactive compounds it contains, such as phenolics, flavonoids, and alkaloids. This study aimed to provide a comprehensive evaluation of ground-roasted coffee beans (GRCB) from C. liberica, including in vitro evaluation, metabolite fingerprinting using LC-HRMS, and authentication analysis using Fourier transform infrared (FTIR) spectroscopy combined with chemometric techniques. In vitro evaluation proved the inhibitory activity of GRCB solution (with a percentage inhibition of 92.09%), which was comparable to sitagliptin used as a positive control. Metabolite identification revealed the presence of caffeine and chlorogenic acid isomers, namely cryptochlorogenic acid and isochlorogenic acid, as potential markers for further investigation. Chemometric techniques, namely principal component analysis (PCA) and partial least squares-discriminant analysis (PLS-DA), were used to perform exploratory data analysis and authentication study, respectively. The PCA results generated the plot observation, capturing 99.4% of the total variance within the first two components. It also facilitated the functional group identification by evaluating wavenumbers as the variables in the model construction. An authentication study using PLS-DA was also carried out, and it successfully differentiated GRCB with the presence of starch as an adulterant with the area under the curve-receiver operating characteristic (AUC-ROC) outcome of 1.
The eye is a highly sensitive organ with multiple physiological barriers that limit drug bioavailability and reduce patient compliance. Research studies are still going on to discover a novel drug delivery system for ocular delivery. The current research aims to develop and compare the PLGA ocuserts of brimonidine tartrate (BT) by different methods. These BT-loaded PLGA ocuserts offer a promising alternative to commercially available BT eye drops. Ocuserts could significantly minimize the challenges encountered with eye drops like lacrimation, blinking-induced washout, dosing frequency, penetration, stability, and controlled release issues. The BT-loaded PLGA ocuserts were prepared using two methods: solvent casting method (SCM) and glass substrate method (GSM). Both SCM and GSM formulations exhibited smooth texture, pH levels within the range of 6.88±0.24 to 6.90±0.28, uniform thickness (SCM: 0.47±0.10 mm; GSM: 0.29±0.03 mm), minimal weight variation (SCM: 7.83±0.38 mg; GSM: 6.55±0.76 mg), sterility, and appropriate swelling indices (SCM: 6.69±0.33%; GSM: 5.40±0.27%). The evaluation results of SCM and GSM ocuserts revealed positive attributes for ophthalmic use. Noteworthy distinctions emerged in folding endurance, with SCM ocuserts demonstrating significantly higher endurance (87.17±4.34 folds) than GSM ocuserts (71.33±4.82 folds). Moreover, SCM ocuserts exhibited superior drug entrapment efficiency (88.26±3.33 %) to GSM ocuserts (74.91±4.39 %). Stability studies confirmed good stability over a 6-month period, while in vitro (italics) drug release study indicated better controlled release properties for SCM than GSM. Findings demonstrate that SCM emerged as an effective method for preparation of polymeric films in various pharmaceutical industries, including transdermal patches, scaffolds in tissue engineering, flexible wound healing films, biodegradable drug delivery systems, and pharmaceutical packaging as well.
The effect of ionic strength and surface charge density of the lipoplexes formed from the cationic surfactant octadecyltrimethylammonium bromide (OTAB) and the neutral phospholipid 1,2-dioleoyl- sn -glycero-3-phosphocholine (DOPC) on DNA condensation was studied using fluorescence spectroscopy. The structure of lipoplexes was examined by small- and wide-angle X-ray scattering (SAXS/WAXS). The efficiency of DNA condensation was monitored by relative changes in the intensity of the emission of the fluorescence probe ethidium bromide (EtBr). A high OTAB/DNA charge ratio of 10:1 is required for efficient condensation at all ionic strengths. The increasing mole ratio of OTAB/DOPC supports DNA condensation, while the process is significantly hindered by a high ionic strength. Only ~55% of DNA was found to be condensed by OTAB/DOPC = 1 mol mol −1 complexes in 150 mmol l −1 of NaCl. A condensed fluid lamellar phase (L α c ) was detected in the DOPC + OTAB + DNA complexes. The SAXS patterns show regular DNA–DNA packing only in complexes prepared in a medium of low ionic strength (<50 mmol l −1 ). Interestingly, free DNA in the supernatant of DOPC + OTAB + DNA complexes was not detected by UV/Vis spectrometry, indicating its trapping in the lipoplexes.
Enterococcus faecalis is a significant pathogen in endodontic infections, often leading to treatment failure in root canal therapy and contributing to chronic infections. The growing concern over antimicrobial resistance highlights the need for alternative treatment approaches. This study aims to evaluate the antibacterial properties of aqueous green tea (Camellia sinensis) and peppermint (Mentha × piperita) extracts, focusing on their phytochemical profiles and antibacterial activity against E. faecalis, a major pathogen in endodontic infections.
The aim of the study was to investigate the effects of chondroitin sulfate (CS) and fucoidan (F), as well as their combination (CS + F) on the growth and viability of spheroids derived from the non-tumor cell line NIH3T3 and the tumor cell line Hepa1c1c7 using a three-dimensional (3D) cell culture model. Spheroids were formed using the liquid overlay method and treated with different concentrations of substances. Flow cytometry was used to quantitatively assess the representation of live, apoptotic, necrotic, and dead cells in the spheroids after treatment. Spheroids from the non-tumor cell line NIH3T3 after treatment with CS and fucoidan were nontoxic to the cells. By light microscopy, we observed a significant proliferative effect in the case of CS and combination of fucoidan and CS (F + CS). On the contrary, in spheroids from the Hepa1c1c7 tumor cell line, after treatment with our compounds, the compounds, especially fucoidan and a combination of CS and fucoidan, showed antiproliferative effects, which confirms their synergistic antiproliferative effect. According to flow cytometry in non-tumor NIH3T3 spheroids, CS had the most significant effect on the proportion of viable cells, which confirmed its proliferative effect (66.43 ± 4.43%). In spheroids derived from the Hepa1c1c7 tumor cell line, flow cytometry revealed the highest number of dead cells in spheroids after treatment with a combination of CS and fucoidan (19.84 ± 5.80%). Based on our results, we can conclude that a combination of CS and fucoidan showed a synergistic antiproliferative effect on Hepa1c1c7 cell cultures. The 3D cell cultures provide a more physiologically relevant platform for drug testing, highlighting the importance of understanding cell–extracellular matrix interactions in cancer research.
Cisplatin is known to induce oxidative stress and accumulation of reactive oxygen species (ROS), which are the primary causes of its undesirable side effects. Lipids are a major target of ROS undergoing oxidation upon interaction. Lipid peroxidation products are unstable and degrade into reactive compounds that can damage various biomolecules. Induction of oxidative stress and ROS formation is considered another mechanism of action of cisplatin. This article aims to investigate the effect of cisplatin on lipid peroxidation and the activity of the antioxidant enzyme catalase in whole blood and plasma.
