Nanoprecipitation Technique Research Articles

Preparation and characterizations of chitosan–octanoate nanoparticles for efficient delivery of curcumin into prostate cancer cells

The goal of the research was to develop a hydrophobic octanoate salt of chitosan (CS–OA) and use the salt as a nanoparticle platform for the delivery of curcumin (CUR) into prostate cancer cells. The nanoprecipitation technique was used to prepare the nanoparticles, which were measured for particle size and encapsulation efficacy relative to CUR–CS nanoparticles. The cytotoxicity of CUR–OA–CS nanoparticles was evaluated in prostate cancerous cells (PC3 and DU145) in comparison with the corresponding blank nanoparticles and hydroalcoholic CUR solution. PXRD, SEM, and TEM were also used to examine the CUR–CS–OA nanoparticles. The average diameters of the CUR–CS–OA and CUR–CS nanoparticles were 268.90 ± 3.77 nm and 221.90 ± 2.79 nm, respectively, with encapsulation efficiencies of 61.37 ± 1.70% and 60.20 ± 3.17%. PXRD and SEM suggested CUR amorphization in the CS–OA nanoparticles. The void nanoparticles exhibited concentration-dependent antiproliferative action, which was attributed to the cellular uptake of CS. CUR loading into these nanoparticles increased their cytotoxicity even more. The potential of CS–OA nanoparticles as a special delivery system for additional cytotoxic drugs into different malignant cells can be further explored.

PH sensitive lipid polymeric hybrid nanoparticle (LPHNP) of paclitaxel and curcumin for targeted delivery in breast cancer

Objective The study aimed at designing a pH sensitive Lipid polymeric Hybrid nanoparticle (LPHNP) for targeted release of Paclitaxel (PTX) and Curcumin (CUR) in breast cancer. Significance Such systems shall result in controlled triggered release in acidic microenvironment of tumor cells with improved pharmacokinetic profile. Methods Chitosan-coated CUR and PTX coloaded pH-sensitive LPHNPs were synthesized employing nanoprecipitation technique. The synthesized NPs were characterized in terms of particle size, polydispersity index (PDI), zeta potential, and morphology. Results LPHNPs co-loaded with curcumin (CUR) and paclitaxel (PTX) were successfully formulated, achieving a size of 146 nm, a PDI of 0.18, and an entrapment efficiency exceeding 90%. In vitro release studies demonstrated controlled release of CUR and PTX under tumor pH conditions showing 1.6 fold and 1.7 fold higher release in ABS pH 5 in comparison to PBS 7.4 for PTX and CUR respectively. MTT-assay studies revealed enhanced cytotoxicity of CUR and PTX as LPHNPs showing IC50 value of free CUR & PTX 480.06 µg/mL decreasing to 282.97 µg/mL for CS-CUR-PTX-LPHNPs. In vivo pharmacokinetic evaluations in rats confirmed significantly improved bioavailability, with a 3.8-fold increase in AUC for CUR and a 6.6-fold increase for PTX. Additionally, the LPHNPs demonstrated controlled release and prolonged retention, evidenced by a 2.2-fold increase in the half-life (t1/2) of CUR and a 1.3-fold increase in the half-life of PTX. Conclusions: The results underscores potential of chitosan-coated LPHNP as a promising delivery platform, offering high drug loading, optimal size for cellular penetration, and prolonged blood circulation for cancer.

A macromolecule infliximab loaded reverse nanomicelles-based transdermal hydrogel: An innovative approach against rheumatoid arthritis

Infliximab (IFX) is used as a biotherapeutic agent for the treatment of rheumatoid arthritis (RA); however, its biological activity is lost orally because of variations in gastric pH and enzymatic degradation, and reduced bioavailability. The authors have tried to improve the efficacy of macromolecule delivery through transdermal route. Polycaprolactone-Polyethylene glycol-Polycaprolactone (PCL-PEG-PCL) triblock copolymer previously synthesized and was used as an efficient carrier for the preparation of IFX loaded reverse nanomicelles (IFX-RNMs). The RNMs were fabricated via nanoprecipitation technique, characterized and then were incorporated into a Carbopol-based hydrogel with eucalyptus oil (EO) as a penetration enhancer. The optimized RNMs had a particle size of 72.32 nm and an encapsulation efficiency of 83 %. In vitro release, exhibited a sustained pattern of IFX from the prepared carrier system, ex-vivo skin permeation and fluorescence microscopic studies revealed that IFX-RNMs loaded hydrogel with EO markedly improved permeation. An in vivo study was carried out on a CFA-induced RA mice model that revealed significant improvements in the results of behavioral parameters, biochemical assays, histopathological and radiological analysis. Overall, the results concluded that the IFX-RNMs loaded hydrogel can be used as a suitable approach for treating RA.

Synergistic Effect of Surface Hydrophobicity and <i>In-Vitro</i> Antimicrobial Activity of Polymeric Nano-Formulation in Textile Finishing

Fouling and damage of variety of surfaces including textile material is a global challenge. As textile wears next to the skin and health issues are more significant. Thus in an effort to address the issues related to textile surfaces damage, antimicrobial polymeric textile finishing was developed to impart antimicrobial functionalities to the textile fabric. The nanoprecipitation technique was done to synthesize antimicrobial polymeric nanoparticles and applied on to the cotton textile fabric via layer-by-layer self-assembled multilayers dip coating technique. The particle size and zeta potential of the nanoparticles was evaluated form dynamic light scattering analysis (DLS) as 216 nm and-11.2 mV. The antimicrobial polymeric finishing of cotton textile was done by alternate dip coating in polyelectrolytes and nanoformulation. The structural morphology and roughness of the resultant textile was studied by SEM and optical profilometery. While the surface hydrophobicity was found to increase with the number of bilayers coating of hydrophobic polymeric formulation as measured in term of contact angle θ. In-vitro antimicrobial activity was studied against gram negative E. coli and gram positive S. aureus with significant zone of inhibition against both strains. Thus surface hydrophobicity and antimicrobial activity of the textile fabric was synergistically achieved and have potential for biomedical and industrial application.

Unveiling the synergistic effect of octenyl succinic anhydride and pulsed electric field on starch nanoparticles

In this study, guinea starch nanoparticles (GSNP) were prepared by nanoprecipitation technique and modified with octenyl succinic anhydride (3 %) and pulsed electric field (1.5, 3.0, and 4.5 kV/cm). The effect of dual modification on the physicochemical, structural, morphological, thermo-pasting, and rheological properties of GSNP was investigated. The dual modification successfully incorporated octenyl groups into GSNP, as confirmed by 1H nuclear magnetic resonance spectroscopy and Fourier transform infrared spectroscopy. The degree of substitution increased from 0.0254 to 0.0347, with particle size ranging from 241.30 to 292.50 nm and zeta potential of −23.11 to −29.98 mV. TEM micrographs revealed that all SNP samples had self-aggregated granules with a mean size below 120 nm, and XRD confirmed a V-type crystalline structure. The amylose content and water absorption capacity decreased from 34.02 % to 24.63 % and from 2.45 to 1.91 g/g, respectively, while the oil absorption capacity and relative crystallinity increased from 3.42 to 4.01 g/g and from 17.82 % to 34.76 %, with modification. The gelatinization and degradation temperature of modified samples were higher while pasting properties exhibited variation with modification. The rheological properties of modified SNP samples exhibited more pronounced shear thinning, attributed to their weaker gel structure and fluid-like gel network. Overall, results suggested that modified GSNPs have potential for stabilizing Pickering emulsion and delivery of carrier materials for active functional substances.

Formulation Design and Characterization of Nilotinib Polymeric Nanoparticles by Nanoprecipitation Technique for the Improved Drug Solubility and Dissolution Rate

Introduction: Nilotinib is a BCS class-IV poorly water-soluble kinase inhibitor drug, that was used for this study to prepare the polymeric nanoparticles by nanoprecipitation technique using Eudragit RL-100 and RS-100 as polymers, Killophore P-188 as a surfactant, and PEG 400 used as a non-volatile, and nontoxic solvent for the improvement of the drug solubility and dissolution rate. Method: The initial process and formulation variables are screened out based on the selected critical quality attributes such as drug release (%), particle size (nm), zeta potential (mV), and polydispersity index. The FT-IR and DSC studies reveal that the drug has no compatibility between the selected drug and the polymers and does not show any additional drug peaks after physical mixing and formulations. The prepared nanoparticles were further characterized to evaluate the particle size (nm), polydispersity index (PDI), zeta potential (mV), entrapment efficiency (%), and in-vitro drug release (%). From the in vitro drug release study, Eudragit RL-100 and Killophore P-188-based formulations showed optimum drug entrapment efficiency with improved drug solubility and dissolution rate in PEG 400 compared to Eudragit RS-100-based formulations. The accelerated stability data for the optimized formulation batch (F6) before and after storage conditions at 40±2 0C and 75±5% RH indicates that the optimized formulation (F6) is more stable for up to 6 months without changes in drug entrapment efficiency and in vitro dissolution rate. Dissolution kinetic data and diffusion exponent values suggested that optimized formulation followed the Higuchi model with a non-Fickian transport mechanism. Result: According to the results, the preparation method proposed in this study is the most suitable for generating polymeric nanoparticles of nilotinib for improved drug solubility and dissolution rate. Conclusion: The nilotinib-based polymeric nano-formulation proved a potential alternative for better drug release with an enhanced solubility rate.

Arg-Specific serine Protease-Targeted edoxaban tosylate monohydrate-Poly (lactic-co-glycolic acid) Nanoparticles: Investigating Stuart-Prower factor targeting and intestinal distribution through Ex-Vivo fluorescent visualization

The goal of the current study was to formulate and examine the potential of poly (lactic-co-glycolic acid) (PLGA) as carriers to facilitate the targeted administration of edoxaban tosylate monohydrate (ETM). ETM-PLGA-NPs were effectively formulated using the nanoprecipitation technique. Particle size, drug entrapment percentage, zeta potential, assessment of intestinal absorption, FT-IR, SEM, drug dissolution behavior, and histopathology investigations were used to describe ETM-PLGA-NPs. The produced NPs had a roughly spherical shape with a particle size of 99.85 d.nm, a PDI of 0.478, and a zeta potential of 38.5 mV with a maximum drug entrapment of 82.1 %. FTIR measurements showed that the drug’s chemical stability remained intact after preapred into nanoparticles. In vitro drug release behavior followed the Higuchi model and revealed an early burst release of 30 % and persistent drug release of 78 % from optimized NPs for up to 120 hrs. According to in vitro data, a 1:10 ratio of ETM to PLGA provided longer-lasting ETM release and improved encapsulation efficiency. Images captured with an inverted fluorescent microscope exhibited that NPs may both greatly increase the amount of ETM accumulated in the intestinal tract and make it easier for ETM to enter the membrane beneath the cells of the intestines. The study found that using PLGA nanoparticles to encapsulate the ETM resulted in longer circulation duration (aPTT, PT, TT). In vivo investigations found that nanoparticles encapsulated had no negative impact on hematological parameters, lung, liver, or kidney tissues. All things considered, the NPs are a potential delivery method to increase the oral absorption and antithrombotic activity of ETM.

Production and characterisation of antioxidant and antibacterial polymeric nanoparticles loaded with Oenocarpus bataua phenolic extract

SummaryOne recent trend in the food industry is using natural antioxidants and antimicrobials as additives for developing multi‐functional packaging. In this study, phenolic compounds from patawa (PEP), a neglected Amazon palm tree, were extracted and encapsulated in nanoparticles based on acetylated cashew gum polysaccharide (acCGP) and chitosan (CS) using a nanoprecipitation technique. The primary objective was to evaluate the antioxidant activity and antibacterial properties of PEP and acCGP/CS@PEP. Results from HPLC‐MS showed that PEP is mainly composed of epicatechin, naringenin and rutin. acCGP/CS@PEP nanoparticles showed a spheric and smooth microstructure, observed with 40.1% PEP encapsulation into the nanoparticles. The main encapsulated phenolics were luteolin, quercetin and epicatechin. Also, FTIR spectroscopy, X‐ray diffraction and differential scanning calorimetry analyses evidenced the success of PEP encapsulation. Results from antioxidant activity evidenced that acCGP/CS@PEP has a DPPH scavenging activity 45‐fold higher than the unencapsulated PEP, a 5‐fold higher ferric reducing power and 20‐fold higher antioxidant potential against ABTS. Similarly, acCGP/CS@PEP had higher antibacterial activity against Escherichia coli (MIC = 2.24 mg mL−1), Salmonella enteritis (MIC = 4.48 mg mL−1) and Staphylococcus aureus (MIC = 4.48 mg mL−1). Analysis by SEM evidenced that acCGP/CS@PEP had a potent destructive effect with disruption of the bacterial cell membrane and liberation of cytoplasmic content. These findings demonstrated that PEP could be efficiently encapsulated in acCGP/CS nanoparticles, and this strategy could improve the efficiency of PEP as a bioactive compound for developing active packaging.

Starch nanoparticle preparation by the nanoprecipitation technique: Effects of formulation parameters

This study investigates how key formulation parameters influence the formation of starch nanoparticles using the nanoprecipitation technique. When loaded with different compounds, starch nanoparticles present a promising option for controlled drug delivery in food, biomedical, and pharmaceutical applications. The work thoroughly examines factors such as polymer concentration, NaOH concentration, solvent ratios, stirring speed, injection flow, and properties of the non-solvent phase. Characterization is conducted using dynamic light scattering, laser Doppler electrophoresis, and scanning electron microscopy, followed by statistical analysis. Increasing the stirring speed notably decreases nanoparticle size, yielding dimensions of 161.5±2.1 nm, 157.6±2.5 nm, and 136.0±0.8 nm at 500, 700, and 900 rpm, respectively. Higher starch concentrations slightly increase the zeta potential of starch nanoparticles to values of −1.97±0.4 mV, −3.1±0.7 mV, and −3.9±1.5 mV for concentrations of 0.5 %, 1 %, and 2 %, respectively. This charge can be attributed to the hydroxyl functional groups in starch monomers. The study also assesses the stability of starch nanoparticles at different pH levels (4, 7.4, and 9) and explores the use of cryoprotectants during freeze-drying. Remarkably, nanoparticles show enhanced stability at pH 7.4, maintaining their initial sizes over six weeks. Cryoprotectants, even in small amounts, effectively preserve nanoparticle size post-freeze-drying. By adjusting formulation parameters, researchers can tailor the physicochemical characteristics of nanoparticles to achieve specific sizes and ensure stability.

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.

Therapeutic effect of F127-folate@PLGA/CHL/IR780 nanoparticles on folate receptor-expressing cancer cells.

Theragnostic platforms, which integrate therapeutic and diagnostic capabilities, have gained significant interest in drug research because of to their potential advantages. This study reports the development of a novel multifunctional nanoparticle carrier system based on poly(ᴅ,ʟ-lactic-co-glycolic acid) (PLGA) for the targeted delivery of the chemotherapeutic agent chlorambucil (CHL) and the imaging agent IR780. The approach in this study incorporates Pluronic F127-folate onto the PLGA nanoparticles, which enables targeted delivery to folate receptor-expressing cancer cells. The F127-folate@PLGA/CHL/IR780 nanoparticles were formulated using a nanoprecipitation technique, resulting in small size, high homogeneity, and negative surface charge. Importantly, the folate-targeted nanoparticles demonstrated enhanced uptake and cytotoxicity in folate receptor-positive cancer cell lines (MCF-7 and HepG-2) compared to folate receptor-negative cells (HEK 293). Additionally, the F127-folate@PLGA/CHL/IR780 nanoparticles exhibited a lower IC50 value against cancer cells than non-targeted F127@PLGA/CHL/IR780 nanoparticles. These findings suggest that the developed F127-folate@PLGA/CHL/IR780 nanoparticles hold promise as a theragnostic system for targeted cancer therapy and diagnosis, leveraging the advantages of PLGA, folate targeting, and the integration of therapeutic and imaging agents.

Polymeric pH-Responsive Metal-Supramolecular Nanoparticles for Synergistic Chemo-Photothermal Therapy.

Stimuli-responsive drug delivery carriers, particularly those exhibiting pH sensitivity, have attracted significant scholarly interest due to their promising potential in anticancer therapeutic applications. This phenomenon can primarily be ascribed to the inherently acidic nature of tumor microenvironments. However, pH-responsive carriers frequently require the incorporation of functional groups or materials sensitive to pH changes. Given the pH-sensitive characteristics of metal coordination with natural small-molecule drugs, organometallic supramolecules present a facile and effective strategy for integrating pH-responsive behavior into these systems. Meanwhile, utilizing the natural compound luteolin in conjunction with iron ions (Fe3+) through the advanced engineering technique of flash nanoprecipitation (FNP) results in the synthesis of stable, highly loaded nanoparticles (NPs) exhibiting a supramolecular photothermal effect. Our experimental findings substantiate that the photothermal effect persists over time, even after the pH-responsive release phase has ended. Consequently, these polymeric pH-responsive metallic supramolecular nanoparticles integrate chemotherapy and photothermal therapy, creating a synergistic approach to cancer treatment. This bifunctional platform, which exhibits both pH-responsive and photothermal properties, presents a highly promising avenue for biomedical applications, particularly in the area of tumor therapies. Its dual function offers a potentially efficacious approach to tumor treatment.

Hyaluronic Acid-Based Nanoparticles Loaded with Rutin as Vasculo-Protective Tools against Anthracycline-Induced Endothelial Damages.

Anthracycline-based therapies exert endothelial damages through peroxidation and the production of proinflammatory cytokines, resulting in a high risk of cardiovascular complications in cancer patients. Hyaluronic acid-based hybrid nanoparticles (LicpHA) are effective pharmacological tools that can target endothelial cells and deliver drugs or nutraceuticals. This study aimed to prepared and characterized a novel LicpHA loaded with Rutin (LicpHA Rutin), a flavonoid with high antioxidant and anti-inflammatory properties, to protect endothelial cells against epirubicin-mediated endothelial damages. LicpHA Rutin was prepared using phosphatidylcholine, cholesterol, poloxamers, and hyaluronic acid by a modified nanoprecipitation technique. The chemical-physical characterization of the nanoparticles was carried out (size, zeta potential, morphology, stability, thermal analysis, and encapsulation efficiency). Cytotoxicity studies were performed in human endothelial cells exposed to epirubicin alone or in combination with Free-Rutin or LicpHA Rutin. Anti-inflammatory studies were performed through the intracellular quantification of NLRP-3, MyD-88, IL-1β, IL-6, IL17-α, TNF-α, IL-10, and IL-4 using selective ELISA methods. Morphological studies via TEM and image analysis highlighted a heterogeneous population of LicpHA particles with non-spherical shapes (circularity equal to 0.78 ± 0.14), and the particle size was slightly affected by Rutin entrapment (the mean diameter varied from 179 ± 4 nm to 209 ± 4 nm). Thermal analysis and zeta potential analyses confirmed the influence of Rutin on the chemical-physical properties of LicpHA Rutin, mainly indicated by the decrease in the surface negative charge (from -35 ± 1 mV to -30 ± 0.5 mV). Cellular studies demonstrated that LicpHA Rutin significantly reduced cell death and inflammation when compared to epirubicin alone. The levels of intracellular NLRP3, Myd-88, and proinflammatory cytokines were significantly lower in epirubicin + LicpHA Rutin-exposed cells when compared to epirubicin groups (p < 0.001). Hyaluronic acid-based nanoparticles loaded with Rutin exerts significant vasculo-protective properties during exposure to anthracyclines. The overall picture of this study pushes towards preclinical and clinical studies in models of anthracycline-induced vascular damages.

Formulation and Evaluation of Quercetin Loaded Sago Starch Nanoparticles

Aim: Formulation and evaluation of the QLSS nanoparticles as a drug delivery system. Background: Poor drug solubility and permeability, particularly in BCS Class IV drugs, hamper their pharmacokinetics and targeted action. This study aims to address this by utilizing starch nanoparticles as a novel carrier for enhanced delivery and improved bioavailability. Objective: Formulation of the QLSS nanoparticles and their % drug entrapment, drug loading, average particle size, surface morphological examination, in-vitro drug release study, and cytotoxicity activity using an MTT assay against the A549 cancer cell line. Method: QLSS nanoparticles were prepared by the nanoprecipitation technique with some modifications, &amp;assessment, including surface morphological analysis, drug loading, drug entrapment percentage, average particle size, in-vitro drug release study, and cytotoxicity activity. result: The average particle size and surface morphology of prepared optimized QLSS nanoparticles (QLSS 3) were found to be approximately 43.24–113.51 nm and spherical in shape with a 292.1nm of Z-average size. The percentage yield was found to be 80% of QLSS-3. The percentages of drug encapsulation efficiency and loading capacity were found to be 68% and 42.5%, respectively. The drug in-vitro release outcomes were found to be 96.12±1.8% within 12 hours. 10µg/ml of QLSS 3 inhibited 66.31% of A549 cancer cells. Result: The average particle size and surface morphology of prepared optimized QLSS nanoparticles (QLSS 3) were found to be approximately 43.24-113.51 nm and spherical in shape with a 292.1nm Z-average size. The percentage yield was found to be 80 ± 2.0% of QLSS-3. Loading capacity and the percentages of drug encapsulation efficiency were found to be 42.5 ± 1.2% and 68 ± 2.2%, respectively. The results of the in-vitro drug's release were found to be 96.12 ± 1.8% within 12 hours. 10μg/ml of QLSS 3 inhibited 66.31 ± 1.4% of A549 cancer cells. Conclusion: In this research study, sago starch was used for the first time as a drug carrier for quercetin. The results of the studies confirmed the improvement in pharmacokinetic parameters of the BCS-IV class drug.

Impact of ultrasound process on cassava starch nanoparticles and Pickering emulsions stability

Using green techniques to convert native starches into nanoparticles is an interesting approach to producing stabilizers for Pickering emulsions, aiming at highly stable emulsions in clean label products. Nanoprecipitation was used to prepare the Pickering starch nanoparticles, while ultrasound technique has been used to modulate the size of these nanoparticles at the same time as the emulsion was developed. Thus, the main objective of this study was to evaluate the stabilizing effect of cassava starch nanoparticles (SNP) produced by the nanoprecipitation technique combined with ultrasound treatment carried out in the presence of water and oil (more hydrophobic physicochemical environment), different from previous studies that carry out the mechanical treatment only in the presence of water. The results showed that the increased ultrasound energy input could reduce particle size (117.58 to 55.75 nm) and polydispersity (0.958 to 0.547) in aqueous dispersions. Subsequently, Pickering emulsions stabilized by SNPs showed that increasing emulsification (ultrasonication) time led to smaller droplet sizes and monomodal size distribution. Despite flocculation, long-term ultrasonication (6 and 9 min) caused little variation in the droplet size after 7 days of storage. The cavitation effects favored the interaction between oil droplets through weak attraction forces and particle sharing, favoring the Pickering stabilization against droplet coalescence. Our results show the potential to use only physical modifications to obtain nanoparticles that can produce coalescence-stable emulsions that are environmentally friendly.

Development and evaluation of dexamethasone-loaded bioadhesive polymeric nanocapsules for mitigating cardiac and gastric adverse effects of free dexamethasone

PurposeDespite having a wide range of therapeutic advantages, dexamethasone (DEXM)-free formulations have some negative side effects that manifest over time. Polymeric nanocapsules (PNCs) exhibit a core-shell structure that can encapsulate and control the release of drug products. Accordingly, the present study aimed to develop a new nanoparticulate system, PNCs, as drug nanocarriers of DEXM and to exemplify the difference in safety profile regarding the gastropathic and cardiopathic effects of DEXM PNCs versus free DEXM.MethodsDexamethasone-loaded alginate nanocapsules were prepared using the nanoprecipitation technique and evaluated for different parameters. In-vivo assessment of the safety profile of the DEXMs (free and PNCs) necessitated three animal groups: vehicle, free DEXM, and DEXM PNCs groups. Treatments with DEXM were administered intraperitoneally, once daily, for 7 days. Stomach and heart samples were investigated for tissue damage. Tissue insults were assessed via macroscopic, biochemical, histopathological, and immunohistochemical analyses.ResultsThe selected PNCs exhibited a small particle size of 287 ± 7.5 nm, a zeta-potential of -21.06 ± 0.23 mV, an encapsulation efficiency of 91.53 ± 0.5%, and a prolonged release profile for up to 48 h as compared with a free drug. Gastric damage indicators showed more serious mucosal damage with free DEXM, hemorrhagic ulcers, and enhanced oxidative stress than the DEXM PNCs. Biomarkers of cardiac damage were significantly elevated with free DEXM and significantly lower in the DEXM PNCs group.ConclusionDexamethasone was successfully encapsulated into polymeric nanocapsules of sodium alginate coating polymer. The developed alginate nanocapsules exhibited desirable parameters and a superior anticipated side effect profile regarding gastric and cardiac damage.

Preparation of Tofacitinib-Loaded Poly(lactic-co-glycolic acid) Sustained Release Nanoparticles by High-Gravity Nanoprecipitation Technique and Its Performance in Rheumatoid Arthritis

Preparation of Tofacitinib-Loaded Poly(lactic-<i>co</i>-glycolic acid) Sustained Release Nanoparticles by High-Gravity Nanoprecipitation Technique and Its Performance in Rheumatoid Arthritis

Hemocompatible and biocompatible hybrid nanocarriers for enhanced oral bioavailability of paclitaxel: in vivo evaluation

Oral administration of BCS class IV anticancer agents has always remained challenging and frequently results in poor oral bioavailability. The goal of the current study was to develop hybrid nanoparticles (HNPs) employing cholesterol and poloxamer-407 to boost paclitaxel's (PTX) oral bioavailability. A series of HNPs with different cholesterol and poloxamer-407 ratios were developed utilizing a single-step nanoprecipitation technique. The PTX loaded HNPs were characterized systematically via particle size, zeta potential, polydispersity index, surface morphology, in vitro drug release, FTIR, DSC, XRD, acute oral toxicity analysis, hemolysis evaluation, accelerated stability studies, and in vivo pharmacokinetic analysis. The HNPs were found within the range of 106.6±55.60 – 244.5±88.24 nm diameter with the polydispersity index ranging from 0.20±0.03 – 0.51±0.11. SEM confirmed circular, nonporous, and smooth surfaces of HNPs. PTX loaded HNPs exhibited controlled release profile. The compatibility between the components of formulation, thermal stability, and amorphous nature of HNPs were confirmed by FTIR, DSC, and XRD, respectively. Acute oral toxicity analysis revealed that developed system have no deleterious effects on the animals' cellular structures. HNPs demonstrated notable cytotoxic effects and were hemocompatible at relatively higher concentrations. In vivo pharmacokinetic profile (AUC0-∞, AUMC0-∞, t1/2, and MRT0-∞) of the PTX loaded HNPs was improved as compared to pure PTX. It is concluded from our findings that the developed HNPs are hemocompatible, biocompatible and have significantly enhanced the oral bioavailability of PTX.

Formulation and Characterization of Nanoparticle-Protein Sirtuin 1 (NPS1) by Nanoprecipitation Technique

Atherosclerosis is a cardiovascular disease caused by endothelial dysfunction. This situation will trigger the bone marrow to immediately replace it with new endothelial progenitor cells (EPC) cells. However, some studies suggest that EPC can experience premature senescence. Sirtuin-1 (SIRT1) is a cellular post-translational protein that has the task of repairing dysfunctional EPC cells. Studies have tried to develop SIRT1 activation, but currently, there are no studies that have attempted to increase SIRT1 levels in cells. Nanoparticles (NPS) are one of the methods in nanomedicine, which has the advantage of being a drug carrier. So, further research is needed on adding exogenous SIRT1 levels, NPS, which can improve the quality of EPC cells and prevent premature senescence. This study aims to report the formulation and characterization stages of nanoparticles carrying SIRT1 (NPS1) with different solvents, such as ethanol and aquadest. The method used in this formulation uses nanoprecipitation. The characterization of nanoparticles at this stage included organoleptic tests, pH tests, and quantifying using Nanodrops in determining the presence of adsorbed proteins. The pH and organoleptic test showed that the NPS1 formulation was acidic (K1 = 5.412 ± 0.73; K2 = 3.624 ± 0.45; F1 = 5.418 ± 0.55; F2 = 4.182 ± 0.07), yellow in color, and had a characteristic odor. Thus, the formulation and characteristics of NPS1 can be used as a method in drug development for anti-senescence therapy in EPC cells in further research, both in vitro, in vivo, and evaluation of preparations that are still very possible to be developed.

Preparation of starch/PVA nanoparticles and evaluation of their ability to stabilize Pickering emulsions

Biodegradable and biocompatible polymer-based nanoparticles (NPs) hold great promise for various industries. We report the first development of composite NPs consisting of starch (St) and polyvinyl alcohol (PVA) using the nanoprecipitation technique with ethanol as an antisolvent. We varied the St:PVA ratios in the precursor solutions to evaluate their impact on the structure and properties of the composite NPs. The ratios used were 4:1, 1:1, and 1:4. Characterization by X-ray diffraction, differential scanning calorimetry, and thermogravimetric analysis revealed distinct XRD and TGA patterns for the composite St/PVANPs compared to their corresponding physical blends. This indicated the presence of mixed St/PVA crystallites within their structures. Additionally, the crystallinity of St/PVANPs increased with rising St content. Dynamic light scattering and scanning electron microscopy showed that nanoparticle sizes increased with higher PVA proportions. The St/PVANPs showed superior performance as stabilizers in Pickering emulsions, forming denser continuous networks in the gel-like structure of the emulsions. Additionally, increasing the PVA content in the composition of St/PVANPs strengthened the structure of Pickering emulsions. The emulsion stabilized by St20/PVA80NPs showed exceptional stability for one month. These findings highlight the potential of St/PVANPs as innovative materials for various applications, including emulsion stabilization.