Synthesized lemongrass oil‐chitosan nanoemulsion coating for enhanced post‐harvest preservation of bananas ( Musa AAA)

BackgroundPreparation of nanoformulations using natural products as bioactive substances is considered very promising for innovative larvicidal agents. On this context, oil in water nanoemulsions develop a main role, since they satisfactorily disperse poor-water soluble substances, such as herbal oils, in aqueous media. Pterodon emarginatus, popularly known as sucupira, has a promising bioactive oleoresin. However, to our knowledge, no previous studies were carried out to evaluate its potential against Culex quinquefasciatus, the main vector of the tropical neglected disease called lymphatic filariasis or elephantiasis. Thus, we aimed to investigate influence of different pairs of surfactants in nanoemulsion formation and investigate if a sucupira oleoresin-based nanoemulsion has promising larvicidal activity against this C. quinquefasciatus. We also evaluated morphological alteration, possible mechanism of insecticidal action and ecotoxicity of the nanoemulsion against a non-target organism.ResultsAmong the different pairs of surfactants that were tested, nanoemulsions obtained with polysorbate 80/sorbitan monooleate and polysorbate 80/sorbitan trioleate presented smallest mean droplet size just afterwards preparation, respectively 151.0 ± 2.252 and 160.7 ± 1.493 nm. They presented high negative zeta potential values, low polydispersity index (<0.300) and did not present great alteration in mean droplet size and polydispersity index after 1 day of preparation. Overall, nanoemulsion prepared with polysorbate 80/sorbitan monooleate was considered more stable and was chosen for biological assays. It presented low LC50 value against larvae (34.75; 7.31–51.86 mg/L) after 48 h of treatment and some morphological alteration was observed. The nanoemulsion did not inhibit acetylcholinesterase of C. quinquefasciatus larvae. It was not toxic to green algae Chlorella vulgaris at low concentration (25 mg/L).ConclusionsOur results suggest that optimal nanoemulsions may be prepared with different surfactants using a low cost and low energy simple method. Moreover, this prototype proved to be effective against C. quinquefasciatus, being considered an ecofriendly novel nanoproduct that can be useful in integrated control programs of vector control.

Background: Nyctanthes arbor-tristis (L.), generally known as Night Jasmine, is a medicinal plant renowned for its antimicrobial and antioxidant activities. Despite its traditional therapeutic use, there is limited scientific research on its detailed botanical characterization, phytochemical composition, and incorporation into advanced pharmaceutical formulations. This study aims to fill this gap by investigating the botanical and phytochemical profiles of N. arbor-tristis leaves and by developing optimized ethosomal gel formulations for enhanced topical drug delivery. Methodology: Comprehensive phytochemical screening revealed the existence of steroids, alkaloids, flavonoids, and tannins. Quality control parameters such as moisture content and ash values were evaluated. Ethosomal gels were prepared with phospholipids, cholesterol, and ethanol, and formulation optimization was performed using a Design of Experiments (DoE) approach. The developed formulations were systematically evaluated for particle size, polydispersity index, zeta potential, entrapment efficiency, and in vitro drug release profiles. Result and Discussion: Optimized formulations (EG-NAT-12 and EG-NAT-11) exhibited favorable nanoscale particle sizes (130.0 nm and 132.5 nm), low polydispersity indices (0.258 ± 0.027 and 0.274 ± 0.029), high negative zeta potentials (−23.5 mV to −24.0 mV), and high entrapment efficiencies (up to 89.8%). EG-NAT-12 demonstrated sustained drug release, with 84.0% released over 6 hrs. Stability testing confirmed the physical and chemical stability of the formulations over 45 days at both refrigerated and room temperatures. Conclusion: This study demonstrates the potential of Nyctanthes arbor-tristis ethosomal gels as effective topical drug delivery systems, integrating traditional herbal benefits with modern nanotechnology to enhance their efficacy.

This study aimed to develop Imatinib Mesylate (IMT)-loaded Poly Lactic-co-Glycolic Acid (PLGA)-D-α-tocopheryl polyethylene glycol succinate (TPGS)- Polyethylene glycol (PEG) hybrid nanoparticles (CSLHNPs) with optimized physicochemical properties for targeted delivery to glioblastoma multiforme. Glioblastoma multiforme (GBM) is the most destructive type of brain tumor with several complications. Currently, most treatments for drug delivery for this disease face challenges due to the poor blood-brain barrier (BBB) and lack of site-specific delivery. Imatinib Mesylate (IMT) is one of the most effective drugs for GBM, but its primary issue is low bioavailability. Therefore, nanotechnology presents a promising solution for targeted IMT delivery to GBM. This article primarily explores the fabrication of IMT-loaded core-shell lipid-polymer hybrid nanoparticles (CSLHNPs) to achieve enhanced brain delivery with therapeutic efficacy. The primary objective of this study is to develop optimized, stable IMT-loaded hybrid nanoparticles with an encapsulated polymer matrix and to evaluate these nanoparticles using sophisticated instruments such as SEM and TEM to achieve smooth, spherical nanoparticles in a monodispersed phase. The enhanced stable formulation yielded a notable increase in entrapment efficiency, reaching 58.89 ± 0.5%. The physical stability analysis of nanoparticles was assessed over 30 days under conditions of 25 ± 2°C and 60 ± 5% relative humidity. Hemolytic assays affirmed the biocompatibility and safety profile of the nanoparticles. In vitro drug release kinetics revealed a sustained IMT release over 48 hours. The formulated CSLHNPs achieved a narrow size distribution with a mean vesicle diameter of 155.03 ± 2.41 nm and a low polydispersity index (PDI) of 0.23 ± 0.4, indicating monodispersity. A high negative zeta potential of -23.89 ± 3.47 mV ensured excellent colloidal stability in physiological conditions. XRD analysis confirmed the successful encapsulation of IMT within the nanoparticle matrix, with the drug transitioning to an amorphous state for enhanced dissolution. During cell-cell viability assays on LN229, glioblastoma cells were treated with IMT-loaded nanoparticles and showed a significantly enhanced inhibitory effect compared to free IMT. These hybrid nanoparticles demonstrated potential in reducing oxidative stress-induced cellular damage by mitigating reactive oxygen species (ROS). Thus, the prepared IMT hybrid nanoparticles showed higher cellular uptake and superior cytotoxicity compared to the plain drug. This study posits the IMT-PLGA-TPGS-DSPE PEG 2000-CSPLHNPs as a formidable and innovative drug delivery system for Glioblastoma Multiforme (GBM) treatment, warranting further exploration into their clinical application potential. Future work could involve conducting in vivo studies to evaluate the pharmacokinetics, biodistribution, and therapeutic efficacy of the IMT-PLGA-TPGS-DSPE PEG 2000-CSPLHNPs in animal models of Glioblastoma Multiforme (GBM). Additionally, further research may focus on optimizing the nanoparticle formulation for enhanced targeting capabilities, investigating long-term stability under varied storage conditions, exploring potential combination therapies to synergize with the nanoparticles, and assessing the scalability and manufacturability of the developed drug delivery system for potential clinical translation. Integration of advanced imaging techniques for real- time tracking and visualization of nanoparticle distribution within tumours could also be a promising direction for future investigations.

Introduction: Ethosomes are soft and flexible vesicles mainly composed of phospholipids, ethanol and water. The presence of a high amount of ethanol ensure deeper drug penetration; however, an optimal formulation is necessary. This study aims to develop and characterize Fluconazole loaded classical ethosomes using Box-Behken design, in order to achieve to an optimal formulation having a minimal vesicle size, low polydispersity index, high zeta potential and good entrapment efficiency (% EE). Methods: Fluconazole ethosomes were prepared using cold method and tested for vesicle size, polydispersity index, zeta potential and EE%. Box-Behken design was created using Design Expert® Software, where the impact of sonication time and amount of ethanol and soybean lecithin on resulting formulation were investigated. Results: It was determined that increasing the concentration of ethanol up to an optimized limit reduces vesicle size and improves % EE. It was also observed that soybean lecithin concentrations affected positively vesicle size but negatively % EE. Whereas sonication time had an inverse effect both on, vesicle size and EE%. All prepared formulations showed a low polydispersity index and a good zeta potential indicating homogeneity and high stability. Therefore, the optimal formulation had % EE of 80.05±0.306 % and vesicular size of 226.501±5.34 nm with polydispersity index of 0.487±0.0078. Conclusion: In summary, using Box-Behnken design can enhance the understanding of the correlations between the variables involved in ethosome formation and their effects on vesicle size, polydispersity index and % EE. The optimal formulation obtained can be incorporated into drug delivery systems to enhance skin permeation and antifungal activity.

ABSTRACTThe aim of this study was to produce and characterize micro‐ and nanoparticulate lipid carriers for pomegranate seed oil (PSO) to preserve its functional properties. The results of the dynamic light scattering (DLS) technique revealed that formulation proportions minimally affected particle size, with lipid nanoparticles (LNs) ranging from 308 to 325 nm, and LN4:1 being the most monodisperse formulation. Lipid microparticles (LMs) ranged from 1251 to 4364 nm, demonstrating the efficiency of hot homogenization with rotor–stator for micrometer‐sized particles. SEM analysis further confirmed the morphology, showing well‐defined spherical shapes and the presence of particle clusters, likely due to the lyophilization process and the lipid nature of the carriers. All formulations exhibited stable dispersion (high negative zeta potential). Formulations with greater color difference (ΔE*) and a lower polydispersity index (PDI), such as LN4:1, indicate more effective oil homogenization and enhanced protection of the oil and its bioactive components. Compatibility and preservation of PSO characteristics were confirmed by XRD and FTIR. Encapsulation efficiency values for the formulations ranged from 40.0% to 66.1%, indicating satisfactory oil encapsulation. Furthermore, the encapsulation process effectively protected the antioxidant activity of PSO, with a decrease in the DPPH scavenging percentage from 55.4% (free PSO) to values ranging from 41.4% to 51.3% (lipid carriers). Overall, this study demonstrates the feasibility of producing PSO micro‐ and nanoparticles with the methods employed, suggesting applications in sustainable packaging.Practical Applications: The development of lipid micro and nanoparticles for the encapsulation of pomegranate seed oil (PSO) offers significant potential in the food industry, particularly for creating biodegradable active packaging. Encapsulation enhances the stability of bioactive compounds, including punicic acid, tocopherols, and polyphenols, protecting them from oxidative degradation. This preservation improves the shelf life and functional properties of food products. Additionally, the controlled release mechanism of these lipid carriers can enhance the bioavailability of PSO's antioxidants, contributing to improved nutritional value and health benefits. These findings suggest potential applications in the formulation of functional foods, nutraceuticals, and packaging solutions that maintain the quality and safety of food products over time.

The effect of ethanol or acetone, as oil phase solvents, upon the form of paeonol-loaded poly(butyl-2-cyanoacrylate) encapsulated nanocapsules (Pae@PNCs) by interfacial spontaneously polymerization were investigated. Pae@PNCs characterizations including morphology, radius distribution, polydispersity index (PDI), particle size, zeta potential, entrapment efficiency (EE%), drug loading (DL%) and in vitro paeonol release kinetics were evaluated. Results show that 100% acetone have a significant effect on forming nanocapsules, which showed the smaller size (168.3 ± 6.76 nm) under scanning electron microscopy (SEM) and one radius distribution by the particle size analyser. The data showed that using 100% acetone to prepare Pae@PNCs was leading to smaller particle size and lower polydispersity index (PDI), higher zeta potential, better EE (%) and perfect DL (%), which is linear decrease in radius (r2 = 0.939) and PDI (r2 = 0.974) and linear increase EE% (r2 = 0.9879) and DL% (r2 = 0.9892) with the acetone concentration (range 10–100% v/v). Paeonol encapsulated into and adhered on PNCs were confirmed by UV–Visible spectra (UV–Vis), Fourier transform infrared spectroscopy (FTIR) and Differential scanning calorimetry (DSC). Drug release behavior in vitro showed that 100% acetone as solvents on developing Pae@PNCs have greater advantages in controlling and prolonging paeonol release. Results demonstrated that solvents have a significant influence on forming Pae@PNCs.

Although caffeine was suggested as one of the pharmacological agents for the cellulite treatment, its skin permeation restricted. The present work was aimed at formulating caffeine loaded nanostructured lipid carriers (CAF-NLCs) containing coconut oil as a topical delivery system. CAF-NLCs were prepared by the ultrasonic emulsification method, using coconut oil as a liquid lipid. The proper selection of solid lipid and surfactants for these formulations were investigated. Subsequently, physicochemical properties, entrapment efficacy, stability, and in vitro drug release were evaluated. The CAF-NLCs containing coconut oil was successfully prepared using glyceryl behenate as a solid lipid and showed an interesting entrapment efficiency (62-99%). The obtained CAF-NLCs presented the nanosized range (≈ 60-390 nm), with a low polydispersity index and high negative zeta potential values (over ‐30 mV). However, the type and concentration of surfactant also affected these properties. These results suggested that CAF-NLCs containing coconut oil are the promising carrier for delivery of caffeine following topical application.

A promising nystatin nanocapsular hydrogel as an antifungal polymeric carrier for the treatment of topical candidiasis

The escalating crisis of antimicrobial resistance (AMR) poses a severe threat to global health, demanding innovative strategies to rejuvenate conventional antibiotics against multidrug-resistant (MDR) pathogens like Salmonella typhimurium. This study presents an integrated experimental and computational investigation into an oleic acid-based nano-emulsion designed to restore amoxicillin's potency. The amoxicillin-loaded nano-emulsion, prepared via spontaneous emulsification and ultrasonication, yielded stable, semi-spherical nanoparticles with a mean hydrodynamic diameter of 199.6 nm, a low polydispersity index (0.331), and a high negative zeta potential of −46.3 mV, ensuring excellent colloidal stability. In vitro antimicrobial testing against MDR S. Typhimurium revealed a profound 2.3-fold enhancement in antibacterial activity; the nano-formulation produced an inhibition zone 133% larger (35.0 ± 2.1 mm) than free amoxicillin (15.0 ± 1.8 mm). To elucidate the molecular underpinnings, molecular docking and 100 ns molecular dynamics simulations confirmed the stable, high-affinity binding of amoxicillin within the catalytic cleft of its target enzyme, Penicillin-Binding Protein 3 (PBP3a). The interaction, with a strong binding affinity of −9.4 kcal mol−1, was energetically driven by dominant van der Waals (−27.1 kcal mol−1) and electrostatic (−80.6 kcal mol−1) forces, yielding a total binding free energy of −32.0 ± 8.0 kcal mol−1via MM-PBSA analysis. Crucially, in silico ADMET predictions forecast a paradigm shift in pharmacokinetics, projecting a 132 000-fold increase in intestinal absorption and a 95-fold reduction in hepatotoxicity risk. These integrated findings provide a robust, mechanistically detailed rationale for using oleic acid nano-emulsions as a powerful delivery platform to overcome bacterial resistance.

The present study aimed to develop diclofenac sodium nanoemulgel for managing pain and inflammation using the low-energy emulsification technique. Nanoemulsion of diclofenac was formulated using clove oil with adequate amount of surfactants and cosurfactants, and it was converted to hydrogel form using Carbopol 980 as the gelling agent. The droplet size of the oil globules in the nanoemulsion was found to be 64.07 ± 2.65 nm with a low polydispersity index (0.238 ± 0.02) along with high negative zeta potential (−39.06 mV). The developed nanoemulgel exhibited non-Newtonian and pseudoplastic behavior. Thein vitrorelease profile of the developed nanoemulgel was higher as compared to marketed and conventional gel. The carrageenan-induced paw edema test was performed in rats to evaluate the anti-inflammatory activity of developed nanoemulgel. The developed nanoemulgel showed significantly higher (p&lt;0.01) effect in reducing pain and inflammation symptoms as compared to marketed as well as conventional gel of diclofenac. The overall findings of the study suggest that the developed nanoemulgel formulation of diclofenac can be used as a potential approach for the management of pain and inflammation.

Tilmicosin (TMS) is widely used to treat bacterial infections in veterinary medicine, but the clinical effect is limited by its poor solubility, bitterness, gastric instability, and intestinal efflux transport. Nanostructured lipid carriers (NLCs) are nowadays considered to be a promising vector of therapeutic drugs for oral administration. In this study, an orthogonal experimental design was applied for optimizing TMS-loaded NLCs (TMS-NLCs). The ratios of emulsifier to mixed lipids, stearic acid to oleic acid, drugs to mixed lipids, and cold water to hot emulsion were selected as the independent variables, while the hydrodynamic diameter (HD), drug loading (DL), and entrapment efficiency (EE) were the chosen responses. The optimized TMS-NLCs had a small HD, high DL, and EE of 276.85 ± 2.62 nm, 9.14 ± 0.04%, and 92.92 ± 0.42%, respectively. In addition, a low polydispersity index (0.231 ± 0.001) and high negative zeta potential (−31.10 ± 0.00 mV) indicated the excellent stability, which was further demonstrated by uniformly dispersed spherical nanoparticles under transmission electron microscopy. TMS-NLCs exhibited a slow and sustained release behavior in both simulated gastric juice and intestinal fluid. Furthermore, MDCK-chAbcg2/Abcb1 cell monolayers were successfully established to evaluate their absorption efficiency and potential mechanism. The results of biodirectional transport showed that TMS-NLCs could enhance the cellular uptake and inhibit the efflux function of drug transporters against TMS in MDCK-chAbcg2/Abcb1 cells. Moreover, the data revealed that TMS-NLCs could enter the cells mainly via the caveolae/lipid raft-mediated endocytosis and partially via macropinocytosis. Furthermore, TMS-NLCs showed the same antibacterial activity as free TMS. Taken together, the optimized NLCs were the promising oral delivery carrier for overcoming oral administration obstacle of TMS.

From process effluents to intestinal health promotion: Developing biopolymer-whey liposomes loaded with gingerol to heal intestinal wounds and neutralize oxidative stress

Comparative pharmacodynamic study delineating the efficacy of amantadine loaded nano-emulsified organogel via intranasal versus transdermal route in rotenone-induced Parkinson's disease rat model

The aim of this research work was to develop a topical gel formulation containing nanoparticle to diabetic foot ulcer (DFU). In this respect, the nanoparticle formulations were prepared by using spontaneous emulsification technique. The linezolid (LZD) loaded nanoparticle formulation exhibited an low average particle size (PS) of 195.27±5.42 nm, low polydispersity index (PI) of 0.214±0.019, a high zeta potential (ZP) of 20.57±0.35 and high drug entrapment efficiency (EE) of 99.746±0.021%. In order to enhance topical residence time, the LZD-loaded nanoparticles were dispersed in a gel formulation using Methocel TM K4M (HPMC) and Carbopol® 974 P NF. The formulated gels demonstrated favorable characteristics, including an appropriate pH value, suitable mechanical performance, and desirable viscosity and spreadability for topical administration. All formulations displayed pseudoplastic flow and exhibited typical gel-type mechanical spectra at the specified frequency value. Moreover, the developed formulation achieved sustained drug release as intended for these systems. During the ex vivo drug diffusion studies, 0.007±0.004% of LZD was found in receptor phase, and this was an indicator of local effect. The optimum formulation was stable for 6 months. The initial findings suggest that the formulated topical gel containing LZD-loaded nanoparticles holds promise as an effective drug delivery system for DFU management. However, further comprehensive investigations are required to substantiate this hypothesis.

Objective: This project will construct a Cyclodextrin-Based Nanosponge (CDNS) gel and test its topical skin application to improve Posaconazole's (PO) therapeutic impact, distribution, and preservation. Methods: Using convection heating, Cyclodextrin (CDs) (β-CD, 2-HP-β-CD, and SBE-β-CD) were employed to crosslink diphenylcarbonate Nanosponge (NS). Make Posaconazole-Loaded Nanosponges (PONS) by freeze-drying. Box–Behnken Experimental Design (BBD) was used to formulate Carbopol 974 (1–3%, w/w), Propylene glycol (5–10%), and ethanol (10–20%, w/w). The relationship between procedural parameters and quality factors was examined using statistical screening. Analysis of Variance (ANOVA) was used for pilot studies. Key techniques affect contour, Response Surface Methodology (RSM), and perturbation graph quality measures. Results: The average particle size of plain NS was 120–220 nm, while PO loaded ones were 48–51 nm with low Polydispersity Index (PDI). High Zeta Potential (ZP) suggests stable, low-agglomeration chemicals. The formulation demonstrated strong encapsulation efficiency (85.78±4.13%) with a viscosity range of 3476.34±213.12 to 3538.28±164.24 and showed 14% degradation over three months. All test formulations exhibited significantly higher PO skin penetration 12 h post-application (range: 41.64±1.72 μg/cm² to 54.12±1.89 μg/cm²) compared to the control group (5.68±0.23 μg/cm²). In vitro release tests indicated NS complexes released medicines faster than pure medications. PONS3, PONS7, and PONS12 with controlled release were chosen for topical hydrogel research due to their effective PO release regulation. NS resisted photodegradation and chemical degradation of PO for 6 mo. Model carbopol gel with NS compositions tested skin permeability, antifungal efficacy, and stability. PONS steadily permeated rat skin for 12 h. Conclusion: The slow drug release, greater skin penetration, and superior storage stability of the gel formulation based on CDNS of PO imply that it has great potential as a topical delivery system.