Monodisperse Research Articles

Poly(lactic acid hydroxyacetic acid)-poly(ethylene glycol)-modified ginsenoside Rg3 nanomedicine enhances anti-tumor effect in hepatocellular carcinoma

Objective This research aims to improve the bioavailability and anti-hepatocellular carcinoma (HCC) efficacy of Ginsenoside Rg3 by modification with poly (lactic acid hydroxyacetic acid)-poly(ethylene glycol) (PLGA-PEG). Methods PLGA-PEG-Rg3 was obtained by emulsification and evaluated it physiochemical characterization by FTIR, SEM, laser particle-size analyzer and HPLC. The effect of the PLGA-PEG-Rg3 and Rg3 on HepG2 cells was compared in vitro studies, including cell proliferation, transwell and a series of apoptosis detection, and in-situ HCC model. Results The PLGA-PEG-Rg3 were 122 nm in size and 0.112 in polydispersity index with sustained release profile in vitro. Compared to Rg3, PLGA-PEG-Rg3 was more effective in suppressing HepG2 growth and inducing apoptosis by the mitochondrial apoptosis pathway in vitro. And PLGA-PEG modification enhanced the liver-targeting ability and drug circulation time of Rg3 in vivo, resulting in PLGA-PEG-Rg3 possessing superior performance in inhibiting tumor growth and prolonging the survival time of tumor-bearing mice than Rg3. Conclusions Overall, these results showed PLGA-PEG-Rg3 enhanced the anti-tumor effect of Rg3 in HCC.

Investigating the anticancer potential and apoptotic signaling of nanocapsule-loaded pyrogallol in ovarian cancer cells (A2780)

Nanoencapsulation technology enables the efficient delivery of natural bioactive compounds, enhancing stability and controlled release to improve bioavailability and therapeutic efficacy. Pyrogallol, a natural polyphenolic compound, has shown promising anticancer activities against various cancer cell lines. The purpose of this study was to synthesize and characterize nanocapsule-encapsulated pyrogallol (Na-Pyr) and investigate its anticancer potential, apoptotic signaling, and anti-metastatic properties. The process involved synthesizing the nanocapsules using the sol–gel method and evaluating their physical and chemical properties using various techniques. The MTT assay was used to test Na-Pyr’s cytotoxicity against various cancer cell lines, including ovarian cancer (A2780), human colorectal adenocarcinoma (HT-29), and pancreatic cancer (ASPC-1), with Huvec serving as the normal cell line. DAPI staining, real-time PCR, and flow cytometry were performed to examine apoptosis induction and cell cycle arrest. The results obtained from dynamic light scattering (DLS) manifested that Na-Pyr had a size of 176.4 ± 7.26 nm, an average zeta potential of about 42.1 ± 2.01 mV, and a polydispersity (PDI) index of 0.174 ± 0.02. Electron microscopy images exhibited a smooth surface and spherical shape, indicating material compatibility. Na-Pyr exhibited higher anticancer potential against ovarian cancer cells than HT-29 and ASPC-1 cancer cell lines with an IC50 value of 23.5 ± 0.95 μg/mL. Na-Pyr significantly modulates the Bax/Bcl2 ratio and activates the MMP9 pathway-mediated apoptosis. Flow cytometry analysis supported these findings, revealing increased percentages of necrotic, early apoptotic, and late apoptotic populations upon exposure to Na-Pyr. In conclusion, the study highlights the promising anticancer potential of Na-Pyr and its potential as an effective treatment strategy.

Development of dual drug loaded-hydrogel scaffold combining microfluidics and coaxial 3D-printing for intravitreal implantation

Treating diabetic retinopathy (DR) effectively is challenging, aiming for high efficacy with minimal discomfort. While intravitreal injection is the current standard, it has several disadvantages. Implantable systems offer an alternative, less invasive, with long-lasting effects drug delivery system (DDS). The current study aims to develop a soft, minimally invasive, biodegradable, and bioadhesive material-based hydrogel scaffold to prevent common issues with implants. A grid-shaped scaffold was created using coaxial 3D printing (3DP) to extrude two bioinks in a single filament. The scaffold comprises an inner core of curcumin-loaded liposomes (CUR-LPs) that prepared by microfluidics (MFs) embedded in a hydrogel of hydroxyethyl cellulose (HEC), and an outer layer of hyaluronic acid-chitosan matrix with free resveratrol (RSV), delivering two Sirt1 agonists synergistically activating Sirt1 downregulated in DR. Optimized liposomes, prepared via MFs, exhibit suitable properties for retinal delivery in terms of size (<200 nm), polydispersity index (PDI) (<0.3), neutral zeta potential (ZP), encapsulation efficiency (∼97 %), and stability up to 4 weeks. Mechanical studies confirm scaffold elasticity for easy implantation. The release profiles show sustained release of both molecules, with different patterns related to different localization of the molecules. RSV released initially after 30 min with a total release more than 90 % at 336 h. CUR release starts after 24 h with only 4.78 % of CUR released before and gradually released thanks to its internal localization in the scaffold. Liposomes and hydrogels can generate dual drug-loaded 3D structures with sustained release. Microscopic analysis confirms optimal distribution of liposomes within the hydrogel scaffold. The latter resulted compatible in vitro with human retinal microvascular endothelial cells up to 72 h of exposition. The hydrogel scaffold, composed of hyaluronic acid and chitosan, shows promise for prolonged treatment and minimally invasive surgery.

Tityus stigmurus-Venom-Loaded Cross-Linked Chitosan Nanoparticles Improve Antimicrobial Activity.

The rapid resistance developed by pathogenic microorganisms against the current antimicrobial pool represents a serious global public health problem, leading to the search for new antibiotic agents. The scorpion Tityus stigmurus, an abundant species in Northeastern Brazil, presents a rich arsenal of bioactive molecules in its venom, with high potential for biotechnological applications. However, venom cytotoxicity constitutes a barrier to the therapeutic application of its different components. The objective of this study was to produce T. stigmurus-venom-loaded cross-linked chitosan nanoparticles (Tsv/CN) at concentrations of 0.5% and 1.0% to improve their biological antimicrobial activity. Polymeric nanoparticles were formed with a homogeneous particle size and spherical shape. Experimental formulation parameters were verified in relation to mean size (<180 nm), zeta potential, polydispersity index and encapsulation efficiency (>78%). Tsv/CN 1.0% demonstrated an ability to increase the antimicrobial venom effect against Staphylococcus aureus bacteria, exhibiting an MIC value of 44.6 μg/mL. It also inhibited different yeast species of the Candida genus, and Tsv/CN 0.5% and 1.0% led to a greater inhibitory effect of C. tropicalis and C. parapsilosis strains, presenting MIC values between 22.2 and 5.5 µg/mL, respectively. These data demonstrate the biotechnological potential of these nanosystems to obtain a new therapeutic agent with potential antimicrobial activity.

Improving Skin Cancer Treatment by Dual Drug Co-Encapsulation into Liposomal Systems-An Integrated Approach towards Anticancer Synergism and Targeted Delivery.

Skin cancer is a high-incidence complex disease, representing a significant challenge to public health, with conventional treatments often having limited efficacy and severe side effects. Nanocarrier-based systems provide a controlled, targeted, and efficacious methodology for the delivery of therapeutic molecules, leading to enhanced therapeutic efficacy, the protection of active molecules from degradation, and reduced adverse effects. These features are even more relevant in dual-loaded nanosystems, with the encapsulated drug molecules leading to synergistic antitumor effects. This review examines the potential of improving the treatment of skin cancer through dual-loaded liposomal systems. The performed analysis focused on the characterization of the developed liposomal formulations' particle size, polydispersity index, zeta potential, encapsulation efficiency, drug release, and in vitro and/or in vivo therapeutic efficacy and safety. The combination of therapeutic agents such as doxorubicin, 5-fluorouracil, paclitaxel, cetuximab, celecoxib, curcumin, resveratrol, quercetin, bufalin, hispolon, ceramide, DNA, STAT3 siRNA, Bcl-xl siRNA, Aurora-A inhibitor XY-4, 1-Methyl-tryptophan, and cytosine-phosphate-guanosine anionic peptide led to increased and targeted anticancer effects, having relevant complementary effects as well, including antioxidant, anti-inflammatory, and immunomodulatory activities, all relevant in skin cancer pathophysiology. The substantial potential of co-loaded liposomal systems as highly promising for advancing skin cancer treatment is demonstrated.

Interactions of human serum albumin with phosphate and Tris buffers: impact on paclitaxel binding and nanoparticles self-assembly

Aim To investigate the conformational changes in human serum albumin (HSA) caused by chemical (CD) and thermal denaturation (TD) at pH 7.4 and 9.9, crucial for designing controlled drug delivery systems with paclitaxel (PTX). Methods Experimental and computational methods, including differential scanning calorimetry (DSC), UV-Vis and intrinsic fluorescence spectroscopy, mean diameter, polydispersity index (PDI), ζ-potential, encapsulation efficiency (EE), in vitro release and protein docking studies were conducted to study the HSA denaturation and nanoparticles (NPs) preparation. Results TD at pH 7.4 produced smaller NPs (287.1 ± 12.9 nm) than CD at pH 7.4 with NPs (584.2 ± 47.7 nm). TD at pH 9.9 exhibited high EE (97.3 ± 0.2%w/w) with rapid PTX release (50% within 1h), whereas at pH 7.4 (96.4 ± 2.1%w/w), release only 40%. ζ-potentials were around −30 mV. Conclusion Buffer type and pH significantly influence NP properties. TD in PBS at pH 7.4, provided optimal conditions for a stable and efficient drug delivery system.

Study on Thermally Induced Lignin Aggregation Kinetics for the Preparation of Uniformly Sized Lignin Nanoparticles in Water.

Lignin nanoparticles (LNPs) present a potential avenue for the high-value utilization of lignin. However, the simple and ecofriendly method of thermally induced self-assembly for the preparation of LNPs has been overlooked due to a lack of sufficient understanding of the lignin aggregation mechanism. Therefore, this study focuses on the kinetics of thermally induced lignin aggregation. It was found that lignin aggregates formed at lower temperatures exhibit poor stability and are more prone to continuous growth through coalescence. This apparent contradiction with the conventional understanding of thermoresponsive polymers could be attributed to changes in the viscoelasticity of the lignin aggregates during phase separation. Based on this finding, we worked out strategies to optimize the preparation of LNPs in water through thermally induced self-assembly. Pure LNPs with well-defined interfaces and a minimum polydispersity index (PDI) of 0.12 were obtained by increasing the temperature to 125-150 °C. Furthermore, combined with noncovalent modification, LNPs with a PDI of 0.08 would even be formed at 80 °C. Notably, the resulting pure LNPs show potential for application in photonic crystal products that require excellent monodispersity. This study provides a new approach for the environmentally friendly preparation of LNPs with a controllable morphology.

Nanoencapsulation of quinoa oil enhanced the antioxidant potential and inhibited digestive enzymes

Quinoa oil is rich in unsaturated fatty acids and vitamin E, but its instability limits its application in food, pharmaceutical, and cosmetic products. Nanoencapsulation emerges as a promising strategy to promote water dispersibility, preserve and enhance functional properties, and increase the bioavailability of bioactive compounds. This study encapsulated quinoa oil through O/W emulsification, using porcine gelatin (OG) and isolated whey protein (OWG) as encapsulating agents. The particles were characterized by different physical and chemical methods and evaluated in vitro for cytotoxicity using Chinese hamster ovary (CHO) cells, human hepatocarcinoma cells (HepG2) and epithelial cells, and bioactive potential through the determination of Total Antioxidant Capacity (CAT) (acidic and neutral media) and iron chelation, and inhibition of digestive enzymes (α-amylase and amyloglucosidase). OG and OWG particles presented smooth surfaces, with an average size between 161 ± 7 and 264 ± 6 nm, with a polydispersity index of 0.11 ± 0.03 and 0.130 ± 0.04, encapsulation efficiency of 74 ± 1.47 % and 83 ± 2.92 %, and water dispersibility >70 %, respectively. Free and nanoencapsulated quinoa oil did not show cytotoxic effects (cell viability >70 %). Nanoencapsulation promoted the enhancement of the antioxidant activity of quinoa oil in the range of 50–63 % in a neutral medium and 96–153 % in an acidic medium than free oil (p < 0.05). OG and OWG also enhanced the inhibition of the enzymes α-amylase (by 5–7 %) and amyloglucosidase (6–9 times more) than free oil (p < 0.05). The results showed that nanoencapsulation increased the potential for quinoa oil application, enabling the development of innovative products.

A Novel Encapsulation Approach to Enhance the Delivery and Antitumor Activity of Docetaxel in Breast Cancer Therapy

Docetaxel (DTX) is one of the most potent anticancer drugs but its extensive side effects necessitate innovative formulations. In this study, we aimed to investigate the expression pattern of apoptotic proteins, cell cycle arrest, and apoptosis induction after treatment with encapsulated DTX in alginate-chitosan nanoparticles in both breast cancer cells (MCF-7) and peripheral blood mononuclear cells (PBMCs). The characterization of the nanoparticles revealed a spherical shape with a size <50 nm, a hydrodynamic diameter of 200 nm, a Polydispersity Index of 0.5, and an encapsulation efficiency of 98.75 %. The free drug was released completely within 11 h while encapsulated DTX was released only 34 % in 96 h. The encapsulated drug indicated higher cytotoxicity on MCF-7 cells and the half inhibitory concentration (IC50) value was 2 µg/ml after 72 h. Quantitative real-time PCR demonstrated a significant increase in cell death as the expression of apoptosis regulatory protein (Bcl-2) was downregulated with no impact on Bax in the MCF-7 cells. A notable decrease in the expression pattern of pro-inflammatory cytokine (IL-1β) in PBMCs indicated less inflammation induction. Flow cytometry analysis revealed that the newly formulated drug induced less opoptosis in PBMCs than the free DTX. Cell cycle arrest in the sub-G1 phase was observed for the free drug while the encapsulated drug exhibited no significant changes. Our results suggest the high toxicity of the formulated drug in contrast to the free DTX on the MCF-7 cell line, minimal blood cell side effects, and no inflammation positioning it as a promising alternative to free docetaxel.

Preparation of Aloysia citriodora (Lemon verbena) extract loaded lipid-nano capsules for topical antibacterial treatment

Nanocapsules have become a promising drug delivery approach for fighting bacterial infections. Extract from Aloysia citriodora (Lemon verbena), known for its biological activities and culinary applications, was investigated as a potential source for topical antibacterial treatment. The aim was to prepare and optimize lipid nanocapsules loaded with Aloysia citriodora extract, using both water and ethanol as solvents. The production, optimization, and characterization of these nanocapsules were conducted employing a Box-Behnken design to examine the impact of various factors on the polydispersity index, particle size, and entrapment efficiency. Assessments were made on solubility, stability, pH, and homogeneity, along with evaluations of in-vitro drug release, dermatokinetic properties, antioxidant activity, and antibacterial effects. The physical stability and quality of the nanocapsules were demonstrated with an average size of 104.6 nm and a polydispersity index (PDI) of 0.246. The encapsulation effectiveness was determined to be 87.08 %. In-vitro drug release studies revealed sustained release characteristics by the Korsmeyer Peppas model. Additionally, the formulation displayed significant antioxidant activity and promising antibacterial effects against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus. Stability tests over ninety days showed that the formulation maintained structural integrity, consistent pH values and drug content, and good spreadability. The nanoformulation combined the benefits of Aloysia citriodora extract with the advantages of nanocapsule technology, offering a novel approach to addressing various pharmaceutical and antimicrobial challenges.

Controlled Ring-Opening Polymerization of Methyl Glycolide with Bifunctional Organocatalyst.

A bifunctional thiourea-amine-based organocatalyst (Takemoto's catalyst), employing a metal-free approach, is presented for the regioselective ring-opening polymerization (ROP) of optically active (D and L) methyl glycolide (MG). In this study, a chiral version of Takemoto's catalyst efficiently promotes the ROP of MG at room temperature, yielding poly(lactic-co-glycolic acids) (PLGAs) with predicted molecular weights and narrow polydispersity indices (PDI≤1.2). These PLGAs exhibit highly alternating structures without transesterification, as confirmed by 1H NMR, SEC, and MALDI-TOF analyses. Additionally, various macromolecular architectures, including linear and star-shaped PLGAs, were successfully synthesized using corresponding multi-functional alcohol initiators while maintaining the same alternating structures and regioselectivity with PLGA obtained from benzyl alcohol as initiator. Computational studies were conducted to elucidate the mechanism of alternating PLGA formation, revealing two key transition states (TSs): TS-1, which implicates the nucleophilic attack of the hydroxyl group of the initiator or propagating chain on the carbonyl carbon of MG, and TS-2, which involves the subsequent ring-opening of the cyclic ester. The results indicate that ring-opening occurs at both the glycolyl and lactyl sites, with a preference for the glycolyl site, as supported by experimental results. The resulting atactic PLGAs are amorphous, rendering them suitable for drug delivery applications.

Curcumin-cyclodextrin inclusion complexes embedded in intrinsically active nano-assemblies: Preparation, characterization, antibacterial and antibiofilm activity against ESKAPE pathogens

Curcumin loaded β-CD inclusion complexes (CCDs) embedded in intrinsically active rhamnosomes (CCDRs) were developed as alternative antimicrobials at the nano-scale to control ESKAPE (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter spp.) pathogens. The physicochemical analysis of CCDRs demonstrated that the addition of glycolipids (rhamnolipids) during the development of liposomes (phospholipids based) provided stability while the average size (158±5 nm) and polydispersity index (PDI) values of 0.2 demonstrated homogenous population of rhamnosomes. The incorporation of rhamnolipids with phospholipids increased the zeta potential to -45±1 mV with 76±1 % encapsulation efficiency for curcumin with enhanced photochemical and storage stability. In vitro, release studies demonstrated sustained release of curcumin due to its incorporation in β-CD molecular buckets, which were loaded in the aqueous liposomal core. These CCDRs with intrinsic antibacterial and antibiofilm potential enhanced the antimicrobial spectrum against ESKAPE pathogens demonstrating synergism between curcumin and rhamnolipids, by targeting multiple sites of bacterial cells and biofilms as compared to conventional antibiotics. Our study outlines that rhamnolipids and curcumin loaded inclusion complexes together offer an exciting potential for functionalized liposomal delivery systems that would be promising for the development of effective alternative therapeutics against ESKAPE pathogens.

Multi-functional RAFT reagent to prepare fluorescent hyper-branched macromolecular probes for the detection of Fe3+ ions

Reversible addition-fragmentation chain transfer (RAFT) polymerization has the advantages of precise control, high yield, and narrow molecular weight distribution. These merits make it an ideal method for the preparation of hyper-branched fluorescent polymers (FL-HBPs). In this work, a multi-functional RAFT reagent (AVCT-NLP) was prepared for the synthesis of monodisperse FL-HBPs. Firstly, dithionate compound (CN1) containing a CC double bond was synthesized by the reaction of 4-nitrophenol with 1-(bromomethyl)-4-vinylbenzene. Subsequently, the NO2 group on CN1 was reduced to NH2, and the −Br on the 4-bromo-1,8-naphthalic anhydride was substituted to emit fluorescence. Finally, the fluorophore was introduced by the reaction of NH2 with the anhydride on the naphthalene ring to obtain AVCT-NLP which contains fluorophore, dithionate, and CC double bond in one molecule. AVCT-NLP was then used to synthesize the homopolymer (PAVCT-NLP) as both monomer and RAFT reagent. Moreover, PAVCT-NLP served as a macromolecular RAFT reagent, and hydrophilic monomer methacrylic acid (MAA) or 3-butene-1,2-diol were polymerized to obtain amphiphilic hyper-branched polymers (FL-AHBP-1, FL-AHBP-2). All the as-prepared macromolecules (PAVCT-NLP, FL-AHBP-1, and FL-AHBP-2) exhibited specific recognition and high sensitivity for Fe3+. The fluorescence quenching reached up to 74.4 %, with the limit of detection (LOD) as low as 1.82 nM. Additionally, the probe demonstrated pH stability and environmental adaptability. Due to the multi-functional structures of AVCT-NLP, it could be subjected to RAFT polymerization to obtain a monodisperse hyper-branched polymer. All polymers have a high fluorophore density and the polydispersity index (PDI) of the polymer is close to 1.00. This paper provided an effective approach for synthesizing polymer fluorescent probes with versatile structure and fluorescence properties in future applications.

Development of chitosan nanoparticle loaded with Tricholoma fracticum extract and evaluation of in vitro antioxidant activity

SummaryThe objective of this study was to develop Tricholoma fracticum extract‐loaded chitosan nanoparticles (TFNPs) by ionic gelation method and to evaluate their in vitro antioxidant activity. Phenolic and flavonoid contents in the T. fracticum extract were measured spectrophotometrically and chromatographically. Characterisation of NPs was evaluated by field emission scanning electron microscopy (FE‐SEM), transmission electron microscopy (TEM), ZETA analysis, Fourier‐transform infrared spectroscopy (FT‐IR), UV–visible spectroscopy (UV–Vis) and thermogravimetric analysis (TGA). In vitro antioxidant capacity was determined using 2,2‐diphenyl‐1‐picrylhydrazyl (DPPH) and 2,2′‐azino‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid) (ABTS) assays. The phenolic and flavonoid contents in the T. fracticum extract were measured as 7.1 ± 0.3 mg Gallic Acid Equivalent/g extract and 5.5 ± 0.6 mg Quercetin Equivalent/g extract, respectively. The particle size, polydispersity index (PDI) and zeta potential of Blank NP1 and TFNP were 265.5 ± 15.8 nm, 0.4, 38.7 ± 4.0 mV and 333.2 ± 16.3 nm, 0.4, 37.0 ± 4.1 mV, respectively. The highest antioxidant activity was observed in TFNP, followed by T. fracticum extract, chitosan and blank NP, respectively. The preserved or enhanced antioxidant activity observed in the encapsulated T. fracticum extract indicates the potential for loading similar mushroom extracts onto chitosan and thus preserving their bioactive properties.

Ethanolic Cashew Leaf Extract Encapsulated in Tripolyphosphate–Chitosan Complexes: Characterization, Antimicrobial, and Antioxidant Activities

Ethanolic cashew leaf extract (ECL-E) is rich in phenolic compounds and shows remarkable antioxidative and antimicrobial activities. Encapsulation could stabilize ECL-E as the core. Tripolyphosphate (TPP)–chitosan (CS) nanoparticles were used to load ECL-E, and the resulting nanoparticles were characterized. The nanoparticles loaded with ECL-E at different levels showed differences in encapsulation efficiency (47.62–89.47%), mean particle diameters (47.30–314.60 nm), positive zeta potentials (40.37–44.24 mV), and polydispersity index values (0.20–0.56). According to scanning electron micrographs, the nanoparticles had a spherical or ellipsoidal shape, and a slight agglomeration was observed. The appropriate ratio of CS/ECL-E was 1:3, in which an EE of 89.47%, a particle size of 256.05 ± 7.70 nm, a zeta potential of 40.37 ± 0.66 mV, and a PDI of 0.22 ± 0.05 were obtained. The nanoparticles also exhibited high antioxidant activities, as assayed by DPPH and ABTS radical scavenging activities, ferric reducing ability power (FRAP), and oxygen radical absorbance capacity (ORAC). Low minimum inhibitory concentration and minimum bactericidal concentration were observed against Pseudomonas aeruginosa (9.38, 75.00 mg/mL) and Shewanella putrefaciens (4.69, 75.00 mg/mL). In addition, ECL-E loaded in nanoparticles could maintain its bioactivities under various light intensities (1000–4000 Lux) for 48 h. Some interactions among TPP, CS, and ECL-E took place, as confirmed by FTIR analysis. These nanoparticles had the increased storage stability and could be used for inactivating spoilage bacteria and retarding lipid oxidation in foods.

Formulation and characterization of nanoemulsion biopesticide from Balanite aegyptiaca seed kernel extract

Consumers’ growing awareness and desire for food free of pesticide residues led to the incubation of this research work. The study aimed at developing a nanoemulsion formulation of Balanite aegyptiaca seed kernel extract for use as a biopesticide. A preliminary study was carried out on the solubility and miscibility of surfactant, carrier, and deionized water utilizing the low-energy spontaneous emulsification method. Information from the study was then used to plot a ternary phase diagram (TPD) showing both the isotropic zone and the anisotropic zones, from which a point with a surfactant, oil, and water ratio (20:20:60) was selected from the isotropic zone for the formulation. The developed nanoemulsion was tested for stability and thermostability, and both results revealed the system was stable. Similarly, the physiochemical properties of the developed nanoemulsion system were characterized, and the results showed that the system revealed the following properties: mean particle size of 173.2±21.6, polydispersity index (PDI) of 0.403±0.038, surface tension of 32.53±0.71, viscosity of 37.33±0.67 mPas, and a pH of 4.92±0.02. The formulation appears homogeneous, clear, and transparent, which further indicates it’s a nanoemulsion formulation. Therefore, the nanoemulsion formulation of B. aegyptiaca seed kernel can serve as a safe and environmentally friendly substitute for synthetic pesticides in the management of plant diseases.

Development and Investigation of a Nanoemulgel Formulated from Tunisian Opuntia ficus-indica L. Seed Oil for Enhanced Wound Healing Activity.

The aim of this study is to develop a nanoemulgel encapsulating a Tunisian Prickly Pear (Opuntia ficus-indica L.) seed oil (PPSO) to assess, for the first time, the in vivo efficacy of this nanoformulation on wound healing. Phytocompounds of this oil have been reported in the literature as having powerful pharmacological activities. However, it remains poorly exploited due to low bioavailability. A nanoemulsion (NE) was designed by determining the required hydrophilic-lipophilic balance (HLB) and subsequently characterized. The mean droplet size was measured at 56.46 ± 1.12 nm, with a polydispersity index (PDI) of 0.23 ± 0.01 using dynamic light scattering. The zeta potential was -31.4 ± 1.4 mV, and the morphology was confirmed and assessed using transmission electron microscopy (TEM). These characteristics align with the typical properties of nanoemulsions. The gelification process resulted in the formation of a nanoemulgel from the optimum nanoemulsion. The high wound healing efficiency of the nanoemulgel was confirmed compared to that of a medicinally marketed cream. The outcomes of this research contribute valuable insights, for the first time, into the potential therapeutic applications of PPSO and its innovative pharmaceutical formulation for wound healing.

Timescale dependent homogeneous assembly of lipid-polymer hybrid nanoparticles in laminar mixing for enhanced lung cancer treatment

The homogeneity of core–shell structure lipid-polymer hybrid nanoparticles (HNPs) is crucial for efficient intracellular cargo delivery. While microfluidic techniques have been recognized for their capabilities in precisely controlling the size and drug encapsulation efficiency, there is little research exploring the impact of mass transfer behavior within microchannels on the homogeneous assembly process of HNPs. Here, we manipulated the laminar flow state within TrM device to achieve controlled assembly of HNPs and explored a timescale dependent assembly technique to ensure the homogeneity of folate modified HNPs (FHNPs). Our founding indicate that this method enabled the control over the growth kinetics of PLGA cores within a timescale (τgrow) of 1–15 ms. The homogeneous ligand assembly on the surface of FHNPs can only be achieved when τgrow exceeds the timescale of functional lipid coating (τcoating). Compared to conventional bulk mixing methods, this strategy significantly reduces the risk of heterogeneous assembly in FHNPs fabrication and ensures consistent reproducibility across batches. The homogeneous FHNPs (HFHNPs) fabricated through this method exhibit precise control over particle size (ranging from 75 nm to 150 nm), low polydispersity index, and consistent core–shell structure. Furthermore, this strategy enhances the density of available folate ligands on the surface of FHNPs. In subsequent in vitro and in vivo anti-tumor assays, the icariside Ⅱ (IS) loaded HFHNPs (IS@HFHNPs) exhibited enhanced cellular uptake and tumor accumulation behavior. the timescale dependent homogeneous assembly method for HNPs developed in this research presents a promising avenue for maintaining quality in the synthesis of self-assembly composite nanomecidine.

Formulation, characterization, and stability of morin hydrate-loaded nanoemulsion

Morin hydrate (MH) is a bioflavonoid belonging to flavonol class. Despite its pharmacological activities, MH has inherent low aqueous solubility and chemical instability hindering biological applications of this flavonol. In this regard, this study aimed to develop and characterize nanoemulsion containing MH. Nanoemulsion formulations were prepared using phase inversion temperature method and characterized by size, polydispersity index (PdI), physical stability, AFM analysis, incorporation efficiency (IE), and in vitro release. Following the formulation design, F10 formulation was chosen to incorporate MH. Nanoemulsion containing MH (MH-NE) showed droplet size in nanometric scale (< 100 nm) with homogeneous size distribution (PdI < 0.1). In addition, good physical stability of MH-NE was demonstrated using analytical photocentrifugation method where the light transmission profiles did not change throughout the emulsions. According to AFM analysis, oil droplets were mostly spherical or semi-spherical having sizes uniformly distributed. The IE of MH into nanoemulsion was approximately 100%, and in vitro release profile of this flavonol from formulation was gradual throughout the experiment. Therefore, using a reproducible method of low energy emulsification we developed a stable colloidal dispersion of nanoemulsion containing MH.

Optimization and evaluation of a chitosan-coated PLGA nanocarrier for mucosal delivery of Porphyromonas gingivalis antigens

Recent advances in understanding Alzheimer's disease (AD) suggest the possibility of an infectious etiology, with Porphyromonas gingivalis emerging as a prime suspect in contributing to AD. P. gingivalis may invade systemic circulation via weakened oral/intestinal barriers and then cross the blood-brain barrier (BBB), reaching the brain and precipitating AD pathology. Based on the proposed links between P. gingivalis and AD, a prospective approach is the development of an oral nanovaccine containing P. gingivalis antigens for mucosal delivery. Targeting the gut-associated lymphoid tissue (GALT), the nanovaccine may elicit both mucosal and systemic immunity, thereby hampering P. gingivalis ability to breach the oral/intestinal barriers and the BBB, respectively.The present study describes the optimization, characterization, and in vitro evaluation of a candidate chitosan-coated poly(lactic-co-glycolic acid) (PLGA-CS) nanovaccine containing a P. gingivalis antigen extract. The nanocarrier was prepared using the double emulsion solvent evaporation method and optimized for selected experimental factors, e.g. PLGA amount, surfactant concentration, w1/o phase ratio, applying a d-optimal statistical design to target the desired physicochemical criteria for its intended application. After nanocarrier optimization, the nanovaccine was characterized in terms of particle size, polydispersity index (PdI), ζ-potential, encapsulation efficiency (EE), drug loading (DL), morphology, and in vitro release profile, as well as for mucoadhesivity, stability under simulated gastrointestinal conditions, antigen integrity, in vitro cytotoxicity and uptake using THP-1 macrophages.The candidate PLGA-CS nanovaccine demonstrated appropriate physicochemical, mucoadhesive, and antigen release properties for oral delivery, along with acceptable levels of EE (55.3 ± 3.5 %) and DL (1.84 ± 0.12 %). The integrity of the encapsulated antigens remained uncompromised throughout NPs production and simulated gastrointestinal exposure, as confirmed by SDS-PAGE and Western blotting analyses. Furthermore, the nanovaccine showed effective in vitro uptake, while exhibiting low cytotoxicity. Taken together, these findings underscore the potential of PLGA-CS NPs as carriers for adequate antigen mucosal delivery, paving the way for further investigations into their applicability as vaccine candidates against P. gingivalis.