Particle Zeta Potential Research Articles

Transferrin-Conjugated Nanostructured Lipid Carriers for Targeting Artemisone to Melanoma Cells.

We report a successful formulation of Artemisone (ATM) in transferrin (Tf)-conjugated nanostructured lipid carriers (NLCs), achieving nearly a five-times increase in cell toxicity. The escalating cost of new drug discoveries led to the repurposing of approved drugs for new indications. This study incorporated Artemisone, an antimalarial drug, into a nanostructured lipid carrier (NLC) and tested for possible anticancer effects. The aim was to develop NLCs, and transferrin-conjugated NLCs (NLC-Tf) encapsulating Artemisone to enhance its delivery and anticancer activity. NLC formulations were prepared using high-pressure homogenization followed by ultrasonication and were characterized by particle size, zeta potential, and PDI. The conjugation of (Tf) to (NLC) was confirmed using IR, and the anticancer activity was tested using MTS assay. All formulations were in the nanometer size range (140-167 nm) with different zeta potential values. IR spectroscopy confirmed the successful conjugation of transferrin to NLC. Upon testing the formulations on melanoma cell lines using MTS assay, there was a significant decrease in viability and an increase in the encapsulated ATM-Tf toxicity compared to positive control ATM. The NLCs presented a promising potential carrier for delivering ATM to melanoma cells, and further conjugation with Tf significantly improved the ATM cytotoxicity.

An in vitro study for reducing the cytotoxicity and dose dumping risk of remdesivir via entrapment in nanostructured lipid carriers

The aim of this study was to synthesize and evaluate nanostructured lipid carriers (NLCs) loaded with Remdesivir (RDV) to control its side effects in COVID-19 patients. Due to the low solubility and short half-life of RDV in the blood, an injectable formulation was prepared using sulphobutylether-beta-cyclodextrin. However, it can accumulate in the kidney and cause renal impairment. NLCs improve the parenteral delivery of hydrophobic drugs such as RDV by increasing drug solubility and bioavailability. For the synthesis of RDV-NLCs, the aqueous phase containing Tween 80 was injected into the lipid phase under rapid stirring and was sonicated. The experimental conditions were optimized using Box-Behnken design and Design Expert software. The optimum formulation contained a total lipid of 2.13%, a total surfactant of 1%, and a hot bath time of 71 min. The optimum formulation showed particle size, polydispersity index, zeta potential, and entrapment efficiency values of 151.0 ± 1.7 nm (from 149.1 to 152.1), 0.4 ± 0.1 (from 0.3 to 0.5), −43.8 ± 1.2 mV (from −42.4 to −44.7), and 81.34 ± 1.57% (from 79.52 to 82.33%), respectively. RDV-NLCs showed acceptable stability for 30 days at 25 ℃ and were compatible with commonly used intravenous infusion fluids for 48 h. FE-SEM images of RDV-NLC showed spherical particles with a mean diameter of 207 nm. The NLC-RDV formulation showed a sustained release of RDV with a low risk of dose-dumping, minimizing potential side effects. In addition, RDV in the form of RDV-NLC causes less cytotoxicity to healthy normal kidney cells, which is expected to reduce renal impairment in COVID-19 patients.

Optimizing Encapsulation of Active Compounds of Carrot By-Product in TPP-Chitosomes.

Liposomes coated with chitosan by ionic gelation with tripolyphosphate (TPP-chitosomes) are interesting particles for stabilizing active compounds. However, the encapsulation condition must be optimized. The aim of this study was to optimize the encapsulation of phenolics and carotenoids of carrot pomace in TPP-chitosomes by using a Central Composite Design 23 and response surface methodology. The independent variables were the phospholipid (0.8-4.2 mg/mL), chitosan (2.6-9.4 mg/mL), and carrot pomace (4-14 g/100 mL of ethanol) concentrations; the responses were the encapsulation efficiency in TPP-chitosomes (EE) of phenolics, a-carotene, and b-carotene and the particle size and zeta potential of the particles. The zeta potential ranged from +17 to +37 mV, indicating that the liposomes were coated with chitosan and that the particle sizes were in the nanometric to submicrometric scale. The optimized condition for encapsulating carotenoids was 2.5 mg/mL phospholipids, 6.0 mg/mL chitosan, and 12 g of carrot pomace/100 mL of ethanol. In this condition, the EE of phenolics and α- and β-carotene was 95%, 98%, and 99%, respectively. Therefore, TPP-chitosomes containing encapsulated phenolics and carotenoids, which can be obtained from agro-industrial by-products, have potential application as natural pigments in food or cosmetics. TPP-chitosomes can also be used to encapsulate other types of natural pigments.

Quality by design approach of apocynin loaded clove oil based nanostructured lipid carrier as a prophylactic regimen in hemorrhagic cystitis in vitro and in vivo comprehensive study

Apocynin (APO) is a naturally occurring acetophenone with eminent anti-inflammatory and anti-oxidant peculiarities. It suffers from poor bioavailability due to low aqueous solubility. Herein, APO was loaded in a Clove oil (CO) based Nanostructured lipid carrier (NSLC) system using a simple method (ultrasonic emulsification) guided by a quality-by-design approach (23 full factorial design) to optimize the formulated NSLCs. The prepared NSLCs were evaluated regarding particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (EE%). The optimal formula (F2) was extensively investigated through transmission electron microscope (TEM), Fourier transform infrared (FT-IR) spectroscopy, Differential scanning calorimetry (DSC), X-ray diffractometry (XRD), in vitro release, and stability studies. Cytotoxicity against human urinary bladder carcinoma (T24) cell line and in vivo activity studies in rats with induced cystitis were also assessed. The results disclosed that the optimal formula (F2) had PS of 214.8 ± 5.8 nm with EE% of 79.3 ± 0.9%. F2 also exhibited a strong cytotoxic effect toward the T24 cancer cells expressed by IC50 value of 5.8 ± 1.3 µg/mL. Pretreatment with the optimal formula (orally) hinted uroprotective effect against cyclophosphamide (CP)-induced hemorrhagic cystitis (HC) in rat models, emphasized by histopathological, immunohistochemical, and biochemical investigations. In consideration of the simple fabrication process, APO-loaded CO-based NSLCs can hold prospective potential in the prophylaxis of oncologic and urologic diseases.

Synthesis and characterization of selenium nanoparticles stabilized by Grifola frondosa polysaccharides and gallic acid conjugates

Selenium nanoparticles (SeNPs) are of interest for their versatility and low toxicity, but bare SeNPs are unstable and tend to aggregate and precipitate as black elemental Se, which limits the application of SeNPs. This study evaluated the physicochemical properties, physical stability, antioxidant activities and cytotoxicity of SeNPs stabilized by Grifola frondosa polysaccharides (GFPs) and GFPs-gallic acid conjugates (GFPs-GA). The results showed that the particle size (PZ), polymer index (PDI) and zeta potential (ZP) of the GFPs-SeNPs and GFPs-GA-SeNPs were 58.72 ± 0.53 nm, 0.11, −8.36 ± 0.21 mV and 61.80 ± 0.16 nm, 0.12, −9.37 ± 0.13 mV, respectively. Besides, the GFPs-SeNPs and GFPs-GA-SeNPs remained stable when stored at 4 °C for 70 days in darkness. SeNPs stabilized with GFPs have improved the antioxidant activity and selective toxicity to tumour cells. Interestingly, SeNPs stabilized with GFPs-GA further enhanced these biological activities. This work provided a simple and effective method to construct well-dispersed SeNPs in aqueous systems, demonstrating the important roles of GFPs and GFPs-GA in the size control, dispersion and stabilization of SeNPs. The prepared GFPs-SeNPs and GFPs-GA-SeNPs can serve as good selenium supplements and have potential prospects for antioxidant activity and tumour inhibition.

Innovative Formulation and Evaluation of Phytosomal Nanoparticles from Ixora Coccinea Linn and its Pharmacological Screening

The use of herbal extracts in pharmaceutical formulations has gained significant attention due to their therapeutic potential and minimum side effects and shows pharmacological profiles as anti-inflammatory, anticancer, and antimicrobial. Thus, the intent of the current study was to develop a potential drug carrier system phytosomal nanoparticle using an extract of the plant “Ixora coccinea”. The extract of Ixora coccinea was prepared by using the maceration method and it is incorporated into Phytosome nanoparticles by using the solvent evaporation method. The impact of various process parameters and material attributes on the average particle size and drug entrapment efficacy. Extract loaded Phytosomal nanoparticles were characterized by particle size determination, Zeta potential, FTIR, and UV spectroscopy. The pharmacological screening consolidated antimicrobial activity was carried out by the well diffusion method, wherein it was performed against Gram Positive (B. Cerus, NCIM-2703) and Gram Negative (E. coli, NCIM 2832) bacteria strains. Which resulted in showing phytosomal nanoparticles show good activity than the extract. The anti-inflammatory activity was carried out by the protein denaturation method, which concluded that Ixora Coccinea phytosomal nanoparticles show better activity. Therefore, it results in moderate anti-inflammatory activity as compared to standard Diclofenac sodium. Keywords: Phytosome nanoparticles, Solvent evaporation method, Invitro anti-inflammatory activity.

Preparation and evaluation of liposomal gel containing Neolamarckia cadamba leaves extract for anti-inflammatory activity

The objective of present research work is to develop liposomes as a carrier system for methanolic extract, its incorporation in to gel formulations and to characterize the prepared and develop liposomal gel formulation. Formulation was carried out by thin film technique. Scanning electron micrograph of the prepared nanosponges at 50.00 kx magnification showed that the liposome was porous with a smooth surface morphology and spherical shape. The porous nature of liposome was clearly observed in the SEM images. Particle size and zeta potential was determined by Malvern Zeta sizer. The particle size analysis confirmed that the prepared sample were in the nanometer range. Average particle size obtained for the formulations F1 to F5 were 162.7 nm to 195.6 nm. Zeta potential values of liposome indicated that the formulated liposomes are stable. The amount of drug being entrapped in liposome was calculated and all the prepared liposome was found to possess very high entrapment efficiency. The viscosity of liposome loaded gel is found to 6842±0.32cps. The pH of liposome loaded gel is 6.3 and spreadability is 12.11, indicating that liposome loaded gel has high release and permeability. The in vitro anti-inflammatory effect of Neolamarckia cadamba extract was evaluated against denaturation of egg albumin. The present findings exhibited a concentration dependent inhibition of protein (albumin) denaturation by Neolamarckia cadamba throughout the concentration range of 20-100μg/ml. Diclofenac sodium (at the concentration range of 20-100 μg/ml) was used as reference drug which also exhibited concentration dependent inhibition of protein denaturation; however, the effect of diclofenac sodium was found to be less active when compared with extract name. Moreover, the results demonstrated that the liposome-based drug delivery approach could be a valuable tool to improve the therapeutic efficacy of phytochemicals by improving their absorption, and bioavailability via altering their physicochemical and release properties. Keywords: Liposomes, Neolamarckia cadamba, Qualitative phytochemical screening, Thin film technique, In vitro anti-inflammatory activity.

Designing of nematode egg parasitic fungus, Purpureocillium lilacinum, nanoemulsion for management of Meloidogyne incognita infection in tomato

Summary Purpureocillium lilacinum is a potent biocontrol agent against Meloidogyne spp. and various other plant-parasitic nematodes in crops. However, existing commercial formulations of P. lilacinum suffer from drawbacks like short shelf life and inconsistent performance in different environmental conditions. To address these issues, a new nano-formulation of P. lilacinum was developed and tested against Meloidogyne incognita infecting tomatoes. Initially, edible oil-based emulsions were prepared using probe ultrasonication, with 40 formulations screened and 14 selected for further testing. Seven of these emulsions remained stable at room temperature (28 ± 4°C) for 8 weeks, with stability assessed based on particle size, zeta potential, and particle shape using particle size analysis and transmission electron microscopy (TEM). Among these, NE 8 (comprising 10 ml of 1% carboxyl methyl cellulose (CMC), 1.25 ml of Tween 80 and 5 ml of sunflower oil) exhibited superior characteristics, with an average particle size of 226.6 nm, a zeta potential of −54.80 mV, and a spherical morphology under TEM examination. The P. lilacinum nanoemulsion formulation was produced by homogenising NE 8 emulsion and spores at a 1:1 ratio, ensuring efficient spore dispersion and encapsulation without loss of viability. In vitro tests demonstrated 100% immobility of M. incognita second-stage juveniles (J2) and 100% parasitism of eggs at a concentration of 5.0 ml l−1. Under glasshouse conditions, soil drenching with the nano-formulation at concentrations ranging from 0.5 to 5.0 ml l−1 resulted in enhanced tomato growth and significant suppression of M. incognita populations in soil and roots, with increased egg mass parasitism. Bio-safety tests confirmed that P. lilacinum nano-formulation at concentrations of 0.25 ml l−1 and 5.0 ml l−1 had no harmful effects on the earthworm Eudrilus eugeniae.

Niosome preparation of atorvastatin drug with green preparation approach for in-vitro study of transdermal absorption with lavender essential oil

Introduction: Studies have pointef to anti-inflammatory properties of atorvastatin. In this research, noisome nanoparticles have been used to increase skin penetration and drug retention. Method: Atorvastatin niosomes were prepared using the sonication method. The effect of cholesterol: surfactant mixture ratio was investigated on physicochemical properties of nanoparticles. Studies have been performed on the morphological features, and characterization of nanoparticles. The toxicity of optimal formulation was investigated on a normal human fibroblast cell line. Different percentages of lavender essential oil were added to the optimal formulation gel, and skin drug delivery studies were performed. Results: The optimal formulation had the optimum particle size, PDI, zeta potential, and EE%, which leads to higher stability and dissolution of atorvastatin in the body. Morphological studies conducted on properties of nanoparticles illustrated a spherical shape and no interference with other formulation components. No cytotoxicity was detected for improved formulation of nanoparticles, including atorvastatin. In-vitro skin permeation results indicated that gel containing 0.5% lavender essential oil atorvastatin noisome (Atrosome) could enhance the dermal delivery of atorvastatin where a higher concentration of atorvastatin can be detected in skin layers. Conclusion: As evidenced by the results of this study, preparing nanoparticles from atorvastatin and adding essential oil to the final formulation exerts a positive effect on local drug delivery. Moreover, drug delivery with nanocarriers significantly increased the percentage of drug retention in the target site.

Myristic Acid Solid Lipid Nanoparticles Enhance the Oral Bioavailability and Therapeutic Efficacy of Rifaximin against MRSA Pneumonia.

Methicillin-resistant Staphylococcus aureus (MRSA) pneumonia is one of the leading causes of death and an immense financial burden on healthcare systems. Rifaximin (RFX) has good antibacterial activity against MRSA, but its clinical application is limited due to its poor oral absorption. Solid lipid nanoparticles have good biocompatibility, high drug loading, sustained release performance, and the inertia of lipids in gastric acid, which facilitates oral drug delivery. In order to improve the oral bioavailability of rifaximin and expand the clinical application of RFX for MRSA pneumonia, this study developed RFX-loaded myristic acid solid lipid nanoparticles (RFX-SLNs). This study first prepared RFX-SLNs through hot melt emulsification and ultrasonic methods and selected the optimal formula of RFX-SLNs through single-factor screening. Afterward, the particle size, zeta potential, and polydispersity index (PDI) of the RFX-SLNs were measured, the morphology of RFX-SLNs was observed by transmission electron microscopy, and the encapsulation efficiency (EE) and drug loading capacity (LC) of RFX-SLNs were detected by high-performance liquid chromatography. Then, the sustained release ability and oral bioavailability of RFX-SLNs were studied through in vitro release and pharmacokinetics. Finally, the therapeutic effect of RFX-SLNs on MRSA pneumonia infection was studied by using a mouse MRSA pneumonia infection model. The optimal formulation of RFX-SLNs was 1% RFX with water (3% PVA) and oil (myristic acid) ratio of 1:19. RFX-SLNs were spherical in shape with a smooth surface and uniform size. The EE and LC of three different batches of RFX-SLNs were 89.35±2.47%, 90.45±3.69%, 88.72±1.18%, and 9.50 ± 0.01%, 10.09±0.01%, and 9.68±0.00%, respectively. In vitro release and pharmacokinetic studies showed that the myristic acid solid lipid nanoparticles showed excellent sustained release as expected and increased the oral bioavailability of RFX by 2.18 times. This indicates that RFX-SLNs can be used for the oral treatment of bacterial infections. Compared to RFX, RFX-SLNs showed good therapeutic effects in a mouse MRSA pneumonia infection model. This study indicates that the myristic acid solid lipid nanoparticles might be an effective way to enhance the oral absorption and therapy effects of RFX and other insoluble drugs. This not only opens up avenues for the clinical application of RFX but also provides a way for the development of new dosage forms of water-soluble drugs and the expansion of their clinical application scope.

CRUDE INULIN DERIVED FROM DAHLIA TUBER AS NANOMATERIAL AND ITS CHARACTERIZATION

Objective: Dahlia tuber (Dahlia sp.) is one of the inulin sources that could be planted in Indonesia. Inulin is fructan-based polysaccharide. Therefore, the research aimed to investigate inulin from the extract of dahlia tuber as a drug excipient, especially for nanoparticles based on inulin-cysteamine thiomer. Methods: Crude inulin was isolated from dahlia tuber using ethanol for maceration. The resulting inulin was characterized using FT-IR and oxidized using sodium periodate (NaIO4) to increase solubility. Afterward, the oxidized crude inulin was further modified by conjugation with cysteamine to produce a cationic thiomer using reductive amination. The thiomer was evaluated regarding the number of thiol groups and solubility. The nanoparticles were prepared using ionic gelation methods. The resulting nanoparticles were evaluated for particle size and zeta potential. Results: Inulin can be isolated from dahlia tuber with its content of 18.60±4.45% and carbohydrate of 61.75±0.75%. Crude inulin can be conjugated with cysteamine to generate a cationic thiomer using NaCNBH3 as a reductant, which can increase its solubility with free thiol group content of 415.21±40.39 µmol/g. Nanoparticles were generated from crude inulin-cysteamine thiomer with sodium tripolyphosphate (NaTTP), leading to a particle size of 180 nm and zeta potential of-10.8 mV. Conclusion: As a potential nanoparticulate drug delivery system, a cationic thiomer could be synthesized from inulin derived from dahlia tuber grown in Indonesia.

DUMB CANE (DIEFFENBACHIA SEGUINE (JACQ.) SCHOTT) EXTRACT NANOEMULSION: PREPARATION, CHARACTERIZATION AND ITS ACTIVITY AS AN INFLAMMATION-INDUCING AGENT IN RATS

Objective: This study aimed to characterize Dumb cane extract nanoemulsion for injection preparation and test its activity as an inflammation-inducing agent in rat intraplantar with IL-6 and TNF-alpha parameters in blood serum as well as the swelling response in paw. Methods: Nanoemulsion was made from an emulsion base of olive oil, coconut oil, tween 80 propylene glycol, and water for injection, as well as varying concentrations of Dumb cane extract (1%, 2%, and 4%) using vortex mixing and sonication methods. The characterization included particle size, zeta potential, and polydispersity index using the Zetasizer tool. Induction was carried out intraplantar in male rats. The parameters observed were the volume of swelling in paw and IL-6 and TNF-alpha in blood serum. Results: Dumb cane extract nanoemulsion concentrations of 1%, 2%, and 4% have particle size characteristics in the range of 20.3±0.17–30.1±0.68 nm, and zeta potential -31.4±1.59–33.1±1.33 mV. Dumb cane nanoemulsion can induce intraplantar inflammation with high IL-6 and TNF-alpha levels, significantly different from normal controls. Volume swelling occurred 4 h after intraplantar induction at a nanoemulsion concentration of 4%. Conclusion: Dumb cane extract nanoemulsion can be an alternative agent for inducing intraplantar inflammation in rat models.

Enhancement of the anticancer potential and biosafety of BSA-modified, bacterial membrane-coated curcumin nanoparticles

Bacteria and bacterial components have been widely used as bionanocarriers to deliver drugs to treat tumors. In this study, we isolated bacterial outer membrane vesicles (OMVs) with good stability and high yield for macrophage polarization and cell recruitment. Using ultrasound baths, these bacterial OMVs were combined with curcumin nanoparticles (OMV CUR NPs), following which these nanoparticles were modified with bovine serum albumin (BSA) to achieve high biosafety and tumor-targeting effects. The particle size, PDI, and zeta potential of the BSA-OMV CUR NPs were 157.9 nm, 0.233, and −15.1 mV, respectively. The BSA-OMV CUR NPs exhibited high storage stability, low cytotoxicity, sustained release, enhanced cellular uptake of CUR, induction of tumor cell apoptosis, and inhibition of tumor cell proliferation and migration. By determining the survival rate, body length, heart rate, head size, eye size, and pericardium size of the zebrafish, we found that the BSA-OMV CUR NPs were safe for application in vivo. Moreover, an increase in antiproliferation, antiangiogenic and antimetastatic effects of BSA-OMV CUR NPs was demonstrated in wild-type and transgenic tumor-transplanted zebrafish embryos.

Artificial chemotaxis under electrodiffusiophoresis

HypothesisThrough a large parameter space, electric fields can tune colloidal interactions and forces leading to diverse static and dynamical structures. So far, however, field-driven interactions have been limited to dipole-dipole and hydrodynamic contributions. Nonetheless, in this work, we propose that under the right conditions, electric fields can also induce interactions based on local chemical fields and diffusiophoretic flows. ExperimentsHerein, we present a strategy to generate and measure 3D chemical gradients under electric fields. In this approach, faradaic reactions at electrodes induce global pH gradients that drive long-range transport through electrodiffusiophoresis. Simultaneously, the electric field induces local pH gradients by driving the particle's double layer far from equilibrium. FindingsAs a result, while global pH gradients lead to 2D focusing away from electrodes, local pH gradients induce aggregation in the third dimension. Evidence points to a mechanism of interaction based on diffusiophoresis. Interparticle interactions display a strong dependence on surface chemistry, zeta potential and diameter of particles. Furthermore, pH gradients can be readily tuned by adjusting the voltage and frequency of the electric field. For large Péclet numbers, we observed a collective chemotactic-like collapse of particles. Remarkably, such collapse occurs without reactions at a particle's surface. By mixing particles with different sizes, we also demonstrate, through experiments and Brownian dynamics simulations, the emergence of non-reciprocal interactions, where small particles are more drawn towards large ones.

Physicochemical characteristics of highly concentrated suspensions with some types of Ukrainian coal

ABSTRACT The investigation results of granulometric composition, zeta potential, sedimentation stability, and viscosity of some water-coal suspensions made of Ukrainian coal from the “Stepova” mine, Lviv-Volyn region, are reported. The most effective granulometric composition of the water-coal suspension consisting of the rough and fine fractions is found from the analysis of the abovementioned physicochemical characteristics of the suspensions. Based on the complex investigation of the zeta potential of the dispersed phase particles, viscosity, and sedimentation stability of the suspensions, it was established that the best technological effectiveness can be expected for the suspensions containing 60% of the rough fraction (sized between 100 and 250 µm) and fine particles sized between 20 and 40 µm. In such systems, the particles form a quasi-stable structure, where the lower-charged small particles are located in the interparticle space between the highly charged bigger particles. All particles bear the same charge, increasing the system’s sedimentation stability and avoiding decomposition for at least 5 days. This time seems reasonable for the preparation, storage, and pumping of the suspensions while their viscosity and stability meet the relevant technological requirements.

Fabrication, characterization, and dihydromyricetin-loaded bioavailability of Pickering emulsions stabilized by Ampelopsis grossedentata polysaccharide -fish collagen peptide composite nanoparticles

A novel strategy was devised to synthesize robust nanocarriers by conjugating fish collagen peptides (FCP) with Ampelopsis grossedentata polysaccharide (AGP), culminating in the creation of FCP-AGP nanoparticles (FCAGPs) for advanced drug delivery systems. The innovative approach entailed the systematic investigation of particle size, zeta potential, and surface hydrophobicity alterations in FCAGPs upon varying AGP concentrations. The optimized FCAGP-4 nanoparticles, boasting a precisely engineered AGP content of 2.0 % (w/v) and an average particle diameter finely tuned to 353.2 ± 10.5 nm, demonstrated outstanding characteristics in dispersibility, stability, and emulsifying capacity. Furthermore, the water contact angle of FCAGP nanoparticles notably increased from 46.3 ± 2.8° to 70.2 ± 5.6°, indicating enhanced surface hydrophobicity. The mechanism by which FCAGP nanoparticles were attached to the surface of oil droplets to stabilize the emulsions was elucidated by confocal laser scanning microscopy (CLSM) and scanning electron microscopy (SEM). Significantly, a modified sample pretreatment technique was employed to demonstrate clearly the emulsion phase interface on the SEM.Innovative FCAGP-stabilized Pickering emulsions achieved 65.39 % in DMY bioavailability, facilitating its slow-release and enhanced bioaccessibility during in vitro digestion. Pickering emulsions loaded DMY demonstrated improved stability and sustained release under simulated digestive conditions, bolstering its therapeutic efficacy. Our findings solidify the theoretical basis for green synthesis of propeptide-polysaccharide nanoparticles and introduce a novel strategy for targeted propeptide Pickering emulsions in drug delivery, highlighting the transformative potential of FCAGP nanoparticles in enhancing lipophilic drug bioavailability and pharmacological impact.

Optimization of Lipid-Based Nanoparticles Formulation Loaded with Biological Product Using A Novel Design Vortex Tube Reactor via Flow Chemistry.

Lipid-based nanoparticles (LNPs) is increasingly recognized for their potential in drug delivery, offering protection to hydrophobic drugs from degradation. Industrial synthesis of LNPs, exemplified by Pfizer-BioNTech and Moderna mRNA vaccines, utilizes flow chemistry or microfluidics, showcasing its scalability. This study explores the utilization of a novel design reactor, the vortex tube reactor, within flow chemistry for LNPs synthesis, aiming to optimize its conditions and compare them with batch synthesis. LNPs were synthesized using the vortex tube reactor, incorporating bovine serum albumin (BSA) as a model drug in the aqueous phase, alongside 1.2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and cholesterol in the organic phase. Design of experiments (DoE), specifically Box-Behnken design, was employed to optimize parameters, including X1: the flow rate ratio (10-100 mL/min), X2: the aqueous-to-organic volumetric ratio (1:1-10:1), and X3: the number of reactor units (1-5 units). Responses evaluated encompassed physical properties and productivity. Optimized conditions were determined by minimizing particle size (Y1), polydispersity index (Y2), and zeta potential (Y3), while maximizing entrapment efficiency (Y4), drug loading (Y5), and productivity (Y5). Results indicated that optimal conditions were achieved at X1 of 100 mL/min, X2 of 5.278, and X3 of 1 unit. LNPs synthesized under these conditions exhibited favorable physical properties and productivity, with uniformity maintained across batches. The vortex tube reactor demonstrated superiority over batch synthesis, yielding smaller particles (166.23 ± 0.98 nm), more uniform nanoparticles (PDI 0.17 ± 0.01), and higher entrapment (67.75 ± 1.55%) and loading capacities (36.39 ± 0.83%), indicative of enhanced productivity (313.4 ± 12.88 mg/min). This study elucidates the potential of flow chemistry, particularly utilizing the vortex tube reactor, for large-scale LNPs formulation, offering insights into parameter relationships and advancing nanoparticle synthesis for drug delivery applications.

Recombinant human epidermal growth factor-loaded liposomes and transferosomes for dermal delivery: Development, characterization, and cytotoxicity evaluation.

Recombinant human epidermal growth factor (rhEGF) is widely utilized as an antiaging compound in wound-healing therapies and cosmetic purposes. However, topical administration of rhEGF has limited treatment outcomes because of its poor percutaneous penetration and rapid proteinase degradation. To overcome these obstacles, this study aims to develop and characterize rhEGF-containing conventional liposomes (rhEGF-CLs) and transferosomes (rhEGF-TFs) as efficient dermal carriers. Physicochemical characterization such as particle size, zeta potential (ZP), morphology, encapsulation efficiency (EE%), and release properties of nanocarriers as well as in vitro cytotoxicity in human dermal fibroblast (HDF) and human embryonic kidney (HEK293) cell lines were investigated. rhEGF-TFs at the rhEGF concentration ranging from 0.05 to 1.0 μg/mL were chosen as the optimum formulation due to the desired release profile, acceptable EE%, optimal cell proliferation, and minimal cytotoxicity compared to the control and free rhEGF. However, higher concentrations caused a decrease in cell viability. The ratio 20:80 of Tween 80 to lipid was optimal for rhEGF-TFs-2, which had an average diameter of 233.23 ± 2.64 nm, polydispersity index of 0.33 ± 0.05, ZP of -15.46 ± 0.29 mV, and EE% of 60.50 ± 1.91. The formulations remained stable at 5°C for at least 1 month. TEM and SEM microscopy revealed that rhEGF-TFs-2 had a regular shape and unilamellar structure. In vitro drug release studies confirmed the superiority of rhEGF-TFs-2 in terms of optimal cumulative release of rhEGF approximately 82% within 24 h. Franz diffusion cell study showed higher rhEGF-TFs-2 skin permeation compared to free rhEGF solution. Taken together, we concluded that rhEGF-TFs can be used as a promising formulation for wound healing and skin regeneration products.

Design, Synthesis and Evaluation of a Novel Teoptinib Derivative as an Effective Anti-hepatocellular Carcinoma Agent.

Hepatocellular Carcinoma (HCC) is a type of liver cancer known for its poor prognosis and high mortality. Teoptinib is a highly selective MET inhibitor that has been used in the treatment of liver cancer. Although good progress has been made in clinical treatment, further improvement is still needed. In this study, a series of novel Teoptinib derivatives were synthesized and evaluated as anti-cancer agents for the treatment of liver cancer, and an oral nanodrug delivery system was also explored. A series of novel Teoptinib derivatives were synthesized, and an oral nanodrug delivery system was also explored. HPLC, high-resolution mass spectrometer and NMR were used to determine the structure and molecular formula of the synthesized compounds. Zeta potential assay was used to access the particle size distribution and zeta potential of the nanoparticles. MTT assay, cell colony formation assay, cell apoptosis inhibition assay, cell scratch assay, and the MHCC-97H xenograft model of nude mice assay were used to evaluate the in vitro and in vivo anti-tumor activity of the synthesized compounds. Compound (R)-10 showed the best antitumor activity with 0.010 μM of the IC50 value against MHCC-97H, a human liver cancer cell line with high c-Met expression. The MHCC-97H xenograft model of nude mice assay showed that nano-prodrug of compound (R)-10 exhibited good in vivo activity with 87.67% of the TGI at the dosage of 8 mg/kg. We designed and synthesized a series of c-Met inhibitors containing different side chains and chiral centers as anti-liver cancer agents. Among them, compound (R)-10 shows a promising effect as a lead molecule for further study in the treatment of liver cancer. The successful incorporation of (R)-10 into a novel oral nanodrug delivery system highlights the importance of effective drug delivery systems for enhanced therapeutic efficacy.

Exploration of Nanomedicine-Based Dry Powder Inhalation Formulation Co-Loaded with Erlotinib and Curcumin for Treatment of Non-Small Cell Lung Cancer

Erlotinib is used as first-line chemotherapy for the treatment of non-small cell lung cancer (NSCLC), which accounts for approximately 85% of lung cancers. Curcumin has potential antitumor effects in different types of cancer including NSCLS with additional chemopreventive and radioprotective effects. The aim of the study was to develop erlotinib and curcumin co-loaded dry powder inhalation (EC-DPI) formulation using nanoprecipitation technique with a goal of achieving a stronger cytotoxic effect against A549 cancer cells. The optimized DPI formulation resulted in suitable particle size (313.28 ± 26.19 nm), polydispersity index (0.156 ± 0.016) and zeta potential (29.4 ± 1.22 mV). Carr’s index (6.62 ± 1.43) and Hausner ratio (1.058 ± 0.03) demonstrated excellent flowability of the powder. The fine particle fraction (64.7 ± 7.8%) and mass median aerodynamic diameter (2.98 ± 0.04 [Formula: see text]m) of the optimized formulation revealed good aerosol performance and its suitability for direct delivery to the lungs. In-vitro cytotoxic potential of EC-DPI was determined against A549 cancer cells and compared with curcumin-loaded DPI formulation (C-DPI) and erlotinib-loaded DPI formulation (E-DPI). The IC[Formula: see text] values for E-DPI and C-DPI were found to be 36.6 ± 2.4 [Formula: see text]M and 24.4 ± 2.7 [Formula: see text]M, respectively. The IC[Formula: see text] value for EC-DPI was 20.5 ± 2.1 [Formula: see text]M confirming the synergistic effect of both drugs against A549 cancer cells. The internalization of the drug inside A549 cells was detected by a cellular uptake study. The EC-DPI demonstrated the highest cellular uptake (0.07 ± 0.006 ng/[Formula: see text]g) followed by the formulation containing curcumin (0.05 ± 0.003 ng/[Formula: see text]g) and erlotinib (0.03 ± 0.004 ng/[Formula: see text]g) alone at the end of 6 h. Hence, the developed DPI formulation can be considered as a potential therapeutic approach for the direct delivery of erlotinib and curcumin to treat NSCLC.