Sesame Oil-Based Nanostructured Lipid Carriers of Nicergoline, Intranasal Delivery System for Brain Targeting of Synergistic Cerebrovascular Protection

Nicergoline (NIC) is a semisynthetic ergot alkaloid derivative applied for treatment of dementia and other cerebrovascular disorders. The efficacy of sesame oil to slow and reverse the symptoms of neurodegenerative cognitive disorders has been proven. This work aimed to formulate and optimize sesame oil-based NIC-nanostructured lipid carriers (NIC–NLCs) for intranasal (IN) delivery with expected synergistic and augmented neuroprotective properties. The NIC–NLC were prepared using sesame oil as a liquid lipid. A three-level, three-factor Box–Behnken design was applied to statistically optimize the effect of sesame oil (%) of the total lipid, surfactant concentration, and sonication time on particle size, zeta potential, and entrapment efficacy as responses. Solid-state characterization, release profile, and ex vivo nasal permeation in comparison to NIC solution (NIC–SOL) was studied. In vivo bioavailability from optimized NIC–NLC and NIC–SOL following IN and IV administration was evaluated and compared. The optimized NIC–NLC formula showed an average particle size of 111.18 nm, zeta potential of −15.4 mV, 95.11% entrapment efficacy (%), and 4.6% loading capacity. The NIC–NLC formula showed a biphasic, extended-release profile (72% after 48 h). Permeation of the NIC–NLC formula showed a 2.3 enhancement ratio. Bioavailability studies showed a 1.67 and 4.57 fold increase in plasma and brain following IN administration. The results also indicated efficient direct nose-to-brain targeting properties with the brain-targeting efficiency (BTE%) and direct transport percentage (DTP%) of 187.3% and 56.6%, respectively, after IN administration. Thus, sesame oil-based NIC–NLC can be considered as a promising IN delivery system for direct and efficient brain targeting with improved bioavailability and expected augmented neuroprotective action for the treatment of dementia.

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Preparation and characterization of natural quercetin-based Mongolia Medicine SenDeng-4 nanoemulsion (N-QUE-NE) and its antibacterial activity..

Current Drug Delivery ◽

10.2174/1567201818666201214143631 ◽

2020 ◽

Vol 18 ◽

Author(s):

Yanfang Zhang ◽

Rina Du ◽

Pengwei Zhao ◽

Sha Lu ◽

Rina Wu ◽

...

Keyword(s):

Particle Size ◽

Antibacterial Activity ◽

Zeta Potential ◽

High Speed ◽

Antibacterial Effect ◽

Average Particle Size ◽

Antagonistic Effect ◽

Dilution Method ◽

Average Particle

Background: Quercetin is the main active ingredient of Xanthoceras sorbifolia Bunge. Traditional compatibility theory of traditional Chinese medicine has typically reported a synergistic interaction among multiple components, while the synergistic effects of nanoemulsion have not been fully clarified. Objective: To study preparation and characterization of quercetin-based Mongolia Medicine Sendeng-4 nanoemulsion (NQUE-NE) and its antibacterial activity and mechanisms. Methods: The morphology of the nanoemulsion was observed by transmission electron microscopy (TEM), and the zeta potential, polydispersity index (PDI), and particle size distribution were determined by the nanometer particle size analyze. The stability of nanoemulsion was investigated by light test, high speed centrifugal test and storage experiment at different temperature. The combined bacteriostatic effect of N-QUE-NE was studied in vitro by double-dilution method and checkerboard dilution method. Results: The appearance of N-QUE-NE was pale yellow, clear and transparent. The nanoemulsion particles were spherical and uniformly distributed under TEM. The PDI was 0.052, the average particle size was 19.6nm, and the Zeta potential was -0.2mV. When quercetin nanoemulsion (QUE-NE) was used in combination with tannin nanoemulsion (TAN-NE) and toosendanin nanoemulsion (TOO-NE), it exhibited a synergistic antibacterial effect. However, the combination of QUE-NE and geniposide nanoemulsion (GEN-NE) exhibited an antagonistic effect. It was revealed that the antibacterial effect was in order of quercetin-tannin-toosendanin nanoemulsion (QUE-TAN-TOO-NE) ＞ quercetin-tannin nanoemulsion (QUE-TANNE) ＞ QUE-NE ＞ quercetin-tannin-toosendanin-geniposide nanoemulsion (QUE-TAN-TOO-GEN-NE). Conclusion: This study explored the preparation and efficacy of N-QUE-NE, and the results showed that quercetin, tannin and toosendanin had satisfactory synergistic antibacterial effects. The antagonistic effect of quercetin and geniposide in nanoemulsion indicated that it is not beneficial to the antibacterial effect of Sendeng-4, and further research needs to be conducted to clarify its antibacterial effect.

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Formulation and Evaluation of Polymeric Nanoparticles of an Antiviral Drug for Gastroretention

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2011.4.4.6 ◽

2012 ◽

Vol 4 (4) ◽

pp. 1557-1562 ◽

Cited By ~ 1

Author(s):

Ankit Anand Kharia ◽

A K Singhai ◽

R Verma

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Average Particle Size ◽

Chlorinated Solvents ◽

Entrapment Efficiency ◽

The Body ◽

Hydrophilic Polymers ◽

Polydispersity Index ◽

Average Particle ◽

Loading Efficiency

The aim of present study was to formulate and evaluate nanoparticles of acyclovir by using different hydrophilic polymers. Acyclovir was selected as a suitable drug for gastro-retentive nanoparticles due to its short half life, low bioavailability, high frequency of administration, and narrow absorption window in stomach and upper part of GIT. The nano-precipitation method was used to prepare nanoparticles so as to avoid both chlorinated solvents and surfactants to prevent their toxic effect on the body. Nanoparticles of acyclovir were prepared by using hydrophilic polymers such as bovine serum albumin, chitosan, and gelatin. The prepared formulations were then characterized for particle size, polydispersity index, zeta potential, loading efficiency, encapsulation efficiency and drug-excipient compatibility. The prepared nanoparticulate formulations of acyclovir with different polymers in 1:1 ratio have shown particle size in the range of 250.12-743.07 nm, polydispersity index (PDI) in the range of 0.681-1.0, zeta potential in the range of -14.2 to +33.2 mV, loading efficiency in the range of 8.74-17.54%, and entrapment efficiency in the range of 55.7%-74.2%. Nanoparticulate formulation prepared with chitosan in 1:1 ratio showed satisfactory results i.e. average particle size 312.04 nm, polydispersity index 0.681, zeta potential 33.2 mV, loading efficiency 17.54%, and entrapment efficiency 73.4%. FTIR study concluded that no major interaction occurred between the drug and polymers used in the present study.

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Effect of Poly(Vinyl Pyrrolidone) on Dispersing Carbon Black Particles

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.796.432 ◽

2013 ◽

Vol 796 ◽

pp. 432-436

Author(s):

Xia Yuan

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Carbon Black ◽

Ultrasonic Method ◽

Aqueous Media ◽

Average Particle Size ◽

Sodium Dodecyl ◽

Vinyl Pyrrolidone ◽

Average Particle ◽

Poly Vinyl Pyrrolidone

The effects of poly (vinyl pyrrolidone)(PVP) on dispersing carbon black (CB) particles were investigated by measuring Z-average particle size, Zeta potential and centrifugal stability of CB dispersions. Addition of PVP in a dispersing medium significantly reduces the size of suspended CB particles, especially in water. The dispersing efficiency of PVP was found to have been enhanced by adding an anionic surfactant, sodium methylenedinaphthalene disulphonate (NNO) in the aqueous media. The particle size of CB dispersed with PVP and NNO was 175.7 nm, significantly smaller than that dispersed with PVP and sodium dodecyl sulfate (SDS). The performance of PVP-encapsulated CB particles and that of PVP-adsorbed CB particles were also compared. The particle size and Zeta potential of PVP-encapsulated CB particles were similar to those of PVP-adsorbed CB particles using ultrasonic method, but the centrifugal stability of PVP-encapsulated CB dispersions was significantly improved. The relative absorbency of PVP/CB dispersions was increased from 42.0% to 63.7%. However, the PVP-encapsulated layer can be destroyed by prolonged ultrasonic treatment because the ultrasound over a long period of time can not only break up the flocculation bridge in the crosslinking matrix of PVP, but also flake off the PVP shells on the surface of CB particles.

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Effect of the Dispersion State in Y5O4F7 Suspension on YOF Coating Deposited by Suspension Plasma Spray

Coatings ◽

10.3390/coatings11070831 ◽

2021 ◽

Vol 11 (7) ◽

pp. 831

Author(s):

Seungjun Lee ◽

Jaehoo Lee ◽

Nongmoon Hwang

Keyword(s):

Particle Size ◽

Light Scattering ◽

Dynamic Light Scattering ◽

Zeta Potential ◽

Average Particle Size ◽

Average Particle ◽

Electrophoretic Light Scattering ◽

Electrosteric Stabilization ◽

Dispersion State ◽

Yttrium Oxyfluoride

The stable Y5O4F7 suspension for dense yttrium oxyfluoride (YOF) coating by suspension plasma spraying (SPS) was developed. Electrostatically and electrosterically stabilized aqueous Y5O4F7 suspensions were prepared and compared with a commercially available Y5O4F7 suspension without dispersant. The wettability and dispersibility of the Y5O4F7 suspensions were evaluated in terms of the zeta potential, average particle size, and size distribution with electrophoretic light scattering (ELS) and dynamic light scattering (DLS). The viscosity was measured and the sedimentation was tested to examine the fluidity and stability of the Y5O4F7 suspensions. When electrostatic (BYK-154) and electrosteric (BYK-199) dispersants were added to the Y5O4F7 suspension, the isoelectric point (IEP) of Y5O4F7 particles in the suspension shifted to lower pH. The zeta potential of both of electrostatically and electrosterically stabilized Y5O4F7 suspensions were higher than ±40 mV at pH of 8.6, respectively, which were much higher than of the Y5O4F7 suspension without dispersant. Meanwhile, the average particle size of the electrosterically stabilized Y5O4F7 suspension was much smaller than that of the electrostatically stabilized one. The electrosteric stabilization had a great effect on improving the wettability and dispersibility of the Y5O4F7 suspension. The coating rate of the electrosterically stabilized Y5O4F7 suspension was the highest among the three tested suspensions. In addition, the YOF coating deposited with the electrosterically stabilized Y5O4F7 suspension had the highest hardness and the lowest porosity.

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BIO-NANOPARTICLES: GREEN SYNTHESIS OF GOLD NANOPARTICLES AND ASSESSMENT OF BIOLOGICAL EVALUATION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i6.34826 ◽

2019 ◽

pp. 133-138

Author(s):

RATIH DYAH PERTIWI ◽

SUWALDI ◽

ERNA PRAWITA SETYOWATI ◽

RONNY MARTIEN

Keyword(s):

Particle Size ◽

Gold Nanoparticles ◽

Zeta Potential ◽

Absorption Spectra ◽

Biological Activities ◽

Average Particle Size ◽

Antioxidant Properties ◽

Biological Evaluation ◽

Nano Particles ◽

Average Particle

Objective: The design like bio-nano particles are beneficial over chemical and physical composition due to the eco-friendly and lower-cost synthesis of nanoparticles. The current study was purposed for the biosynthesis of gold nanoparticles (GNPs) and their antioxidant evaluation. Methods: Aqua extract of Muntingia calabura, Linn was applied for the synthesis of GNPs and confirmed by UV visible and ATR-Fourier Transform Infra-Red (ATR-FTIR) spectroscopy. Transmission Electron Microscope and Particle Size Analyser were used for the shape zeta potential and determination of size. Antioxidant activity was examined by DPPH (1,1 diphenyl-2-picryl-hydrazyl) radical scavenging method. Results: The result showed that UV–vis absorption spectra of H Au Cl4 at 290 nm while absorption spectra of biosynthesis gold nanoparticles at 540 nm. The forming of nanoparticles were spherical, having an average particle size of 88 nm, and the result of zeta potential was 9.5 mV. Analysis of ATR-FTIR revealed the possible involvement of phytochemical constituents in gold nanoparticles of aqua extract. Green synthesized nanoparticles showed enhanced antioxidant properties. Conclusion: Green synthesized GNPs showed enhanced biological activities. Present results also support the benefit of using the biosynthesis method for the production of gold nanoparticles that have the potential of antioxidant and biology activities.

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Improving the Intercellular Uptake and Osteogenic Potency of Calcium Phosphate via Nanocomplexation with the RALA Peptide

Nanomaterials ◽

10.3390/nano10122442 ◽

2020 ◽

Vol 10 (12) ◽

pp. 2442

Author(s):

Michelle O’Doherty ◽

Eoghan J. Mulholland ◽

Philip Chambers ◽

Sreekanth Pentlavalli ◽

Monika Ziminska ◽

...

Keyword(s):

Particle Size ◽

Calcium Phosphate ◽

Zeta Potential ◽

Average Particle Size ◽

Average Particle ◽

Type I ◽

Amphipathic Peptide ◽

Matrix Deposition ◽

Post Transfection ◽

Osteogenic Response

Calcium phosphate-base materials (e.g., alpha tri-calcium phosphate (α–TCP)) have been shown to promote osteogenic differentiation of stem/progenitor cells, enhance osteoblast osteogenic activity and mediate in vivo bone tissue formation. However, variable particle size and hydrophilicity of the calcium phosphate result in an extremely low bioavailability. Therefore, an effective delivery system is required that can encapsulate the calcium phosphate, improve cellular entry and, consequently, elicit a potent osteogenic response in osteoblasts. In this study, collagenous matrix deposition and extracellular matrix mineralization of osteoblast lineage cells were assessed to investigate osteogenesis following intracellular delivery of α-TCP nanoparticles. The nanoparticles were formed via condensation with a novel, cationic 30 mer amphipathic peptide (RALA). Nanoparticles prepared at a mass ratio of 5:1 demonstrated an average particle size of 43 nm with a zeta potential of +26 mV. The average particle size and zeta potential remained stable for up to 28 days at room temperature and across a range of temperatures (4–37 °C). Cell viability decreased 24 h post-transfection following RALA/α-TCP nanoparticle treatment; however, recovery ensued by Day 7. Immunocytochemistry staining for Type I collagen up to Day 21 post-transfection with RALA/α-TCP nanoparticles (NPs) in MG-63 cells exhibited a significant enhancement in collagen expression and deposition compared to an untreated control. Furthermore, in porcine mesenchymal stem cells (pMSCs), there was enhanced mineralization compared to α–TCP alone. Taken together these data demonstrate that internalization of RALA/α-TCP NPs elicits a potent osteogenic response in both MG-63 and pMSCs.

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Third-Generation Cephalosporin-Loaded Chitosan Used to Limit Microorganisms Resistance

Materials ◽

10.3390/ma13214792 ◽

2020 ◽

Vol 13 (21) ◽

pp. 4792

Author(s):

Letiția Doina Duceac ◽

Gabriela Calin ◽

Lucian Eva ◽

Constantin Marcu ◽

Elena Roxana Bogdan Goroftei ◽

...

Keyword(s):

Particle Size ◽

Antibiotic Resistance ◽

Zeta Potential ◽

Average Particle Size ◽

Chitosan Nanoparticles ◽

World Health ◽

Multi Drug Resistance ◽

Prolonged Release ◽

Average Particle ◽

Gravimetric Analysis

From their discovery, antibiotics have significantly improved clinical treatments of infections, thus leading to diminishing morbidity and mortality in critical care patients, as well as surgical, transplant and other types of medical procedures. In contemporary medicine, a significant debate regarding the development of multi-drug resistance involves all types of pathogens, especially in acute care hospitals due to suboptimal or inappropriate therapy. The possibility of nanotechnology using nanoparticles as matrices to encapsulate a lot of active molecules should increase drug efficacy, limit adverse effects and be an alternative helping to combat antibiotic resistance. The major aim of this study was to obtain and to analyze physico-chemical features of chitosan used as a drug-delivery system in order to stop the antibiotic resistance of different pathogens. It is well known that World Health Organization stated that multidrug resistance is one of the most important health threats worldwide. In last few years, nano-medicine emerged as an improved therapy to combat antibiotic-resistant infections agents. This work relies on enhancement of the antimicrobial efficiency of ceftriaxone against gram(+) and gram(−) bacteria by antibiotic encapsulation into chitosan nanoparticles. Physicochemical features of ceftriaxone-loaded polymer nanoparticles were investigated by particle size distribution and zeta potential, Fourier-transform infrared spectroscopy (FTIR), Thermal Gravimetric Analysis (TG/TGA), Scanning Electron Microscopy (SEM) characteristics techniques. The obtained results revealed an average particle size of 250 nm and a zeta potential value of 38.5 mV. The release profile indicates an incipient drug deliverance of almost 15%, after 2 h of approximately 83%, followed by a slowed drug release up to 24 h. Characteristics peaks of chitosan were confirmed by FTIR spectra indicating a similar structure in the case of ceftriaxone-loaded chitosan nanoparticles. A good encapsulation of the antibiotic into chitosan nanoparticles was also provided by thermo-gravimetric analysis. Morphological characteristics shown by SEM micrographs exhibit spherical nanoparticles of 30–250 nm in size with agglomerated architectures. Chitosan, a natural polymer which is used to load different drugs, provides sustained and prolonged release of antibiotics at a specific target by possessing antimicrobial activity against gram(+) and gram(−) bacteria. In this research, ceftriaxone-loaded chitosan nanoparticles were investigated as a carrier in antibiotic delivery.

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Adsorption of Hazardous Heavy Metals Using Reactive Inorganic Agents in Synthetic Wastewater

Materials Science Forum ◽

10.4028/www.scientific.net/msf.658.5 ◽

2010 ◽

Vol 658 ◽

pp. 5-8

Author(s):

Jong Oh Kim ◽

Jin Woo Lee

Keyword(s):

Heavy Metals ◽

Particle Size ◽

Zeta Potential ◽

Adsorption Capacity ◽

Average Particle Size ◽

Synthetic Wastewater ◽

Average Particle ◽

Xrf Analysis ◽

Reactive Agents ◽

Main Components

This study focused on the adsorption characteristics of hazardous heavy metals using reactive inorganic agents in synthetic wastewater. Basic properties of five reactive agents were analyzed by zeta potential, particle size, XRF and SEM. Zeta potential of five adsorbents was 45, 7, 14, -2 and 45 mV, respectively. Average particle size was in the range of 1.4 to 9㎛. By XRF analysis, main components were Na, Al, Si, S and Fe in reactive agents and no great differences in Mg, K, Ca and Ti components. As, Zn, Ni, Cu, Cr, Cd and Pb were used as target heavy metals. Adsorption capacity of Pb and Cu was in the order: TN 315Ny-T3>TN820L>TN315NY.

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Preparation and Characterization of Chitosan Coated PLGA Nanoparticles of Resveratrol: Improved Stability, Antioxidant and Apoptotic Activities in H1299 Lung Cancer Cells

Coatings ◽

10.3390/coatings10050439 ◽

2020 ◽

Vol 10 (5) ◽

pp. 439 ◽

Cited By ~ 3

Author(s):

Hibah M. Aldawsari ◽

Nabil A. Alhakamy ◽

Rayees Padder ◽

Mohammad Husain ◽

Shadab Md

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Average Particle Size ◽

Spherical Shape ◽

Entrapment Efficiency ◽

Aqueous Solubility ◽

Plga Nanoparticles ◽

Steady Increase ◽

Average Particle

Resveratrol (RES) is a polyphenolic compound which has shown beneficial pharmacological effects such as anti-inflammatory, antioxidant, and anti-cancer effects. However, poor aqueous solubility, bioavailability, and low stability are the major limitations to the clinical application of RES. Therefore, in the present study, chitosan (CS) coated PLGA nanoparticles of RES (CS-RES-PLGA NPs) was developed, characterized and its anticancer activity was evaluated in the H1299 lung carcinoma cell line. The effects of the increase in CS coating and cryoprotectant concentration on particle size, polydispersity index (PDI) and zeta potential (ZP) were determined. The particle size, PDI, ZP and entrapment efficiency of the optimized CS-RES-PLGA NPs were found to be 341.56 ± 7.90 nm, 0.117 ± 0.01, 26.88 ± 2.69 mV and 75.13% ± 1.02% respectively. The average particle size and ZP showed a steady increase with an increase in CS concentration. The increase in positive zeta potential is evident for higher CS concentrations. The effect of trehalose as cryoprotectant on average particle size was decreased significantly (p < 0.05) when it was increased from 1%−5% w/v. TEM and SEM showed uniform particle distribution with a smooth surface and spherical shape. The CS coating provides modulation of in vitro drug release and showed a sustained release pattern. The stability of RES loaded PLGA NPs was improved by CS coating. CS-coated NPs showed greater cytotoxicity and apoptotic activities compared to free RES. The CS coated NPs had a higher antioxidant effect than the free RES. Therefore, CS coated PLGA NPs could be a potential nanocarrier of RES to improve drug solubility, entrapment, sustain release, stability and therapeutic application.

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Nanoformulation Development to Improve the Biopharmaceutical Properties of Fisetin Using Design of Experiment Approach

Molecules ◽

10.3390/molecules26103031 ◽

2021 ◽

Vol 26 (10) ◽

pp. 3031

Author(s):

Wan-Yi Liu ◽

Chia-Chen Lin ◽

Yun-Shan Hsieh ◽

Yu-Tse Wu

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Oral Delivery ◽

Encapsulation Efficiency ◽

Average Particle Size ◽

Amorphous State ◽

Polydispersity Index ◽

Morphological Observation ◽

Average Particle ◽

Biopharmaceutical Properties

This study aimed to design an effective nanoparticle-based carrier for the oral delivery of fisetin (FST) with improved biopharmaceutical properties. FST-loaded nanoparticles were prepared with polyvinyl alcohol (PVA) and poly(lactic-co-glycolic acid) (PLGA) by the interfacial deposition method. A central composite design of two independent variables, the concentration of PVA and the amount of PLGA, was applied for the optimization of the preparative parameter. The responses, including average particle size, polydispersity index, encapsulation efficiency, and zeta potential, were assessed. The optimized formulation possessed a mean particle size of 187.9 nm, the polydispersity index of 0.121, encapsulation efficiency of 79.3%, and zeta potential of −29.2 mV. The morphological observation demonstrated a globular shape for particles. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that the encapsulated FST was presented as the amorphous state. The dissolution test indicated a 3.06-fold increase for the accumulating concentrations, and the everted gut sac test showed a 4.9-fold gain for permeability at the duodenum region. In conclusion, the optimized FST-loaded nanoparticle formulation in this work can be developed as an efficient oral delivery system of FST to improve its biopharmaceutic properties.

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