scholarly journals Making Concentrated Pterostilbene Highly Bioavailable in Pressure Processed Phospholipid Nanoemulsion

Processes ◽  
2021 ◽  
Vol 9 (2) ◽  
pp. 294
Author(s):  
Fu-Min Sun ◽  
Yu-Jou Chou ◽  
Qingrong Huang ◽  
Jing-Yu Hu ◽  
Yuwen Ting
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Biological Activity ◽  
Light Scattering ◽  
Storage Stability ◽  
Aqueous Environment ◽  
High Pressure Homogenizer ◽  
Positive Effect ◽  
Monolayer Model

Pterostilbene, a dimethylether analog of resveratrol, has been found to have potent biological activity. However, the bioavailability of pterostilbene in the biological system is limited due to its poor solubility in an aqueous environment. A nanoemulsion system was designed for this purpose. Lecithin-based nanoemulsion was formed after 3 cycles through a high-pressure homogenizer at 500 psi. The rheological properties and particle size were measured using dynamic light scattering and a viscometer. The storage stabilities of the prepared formulation were determined based on its ability to maintain its particle size and loading concentration. According to the experimental results, the lecithin-based nanoemulsion system contained approximately 9.5% of pterostilbene. Over the 28-day stability test, the particle size, zeta potential, and encapsulation of pterostilbene in the nanoemulsion did not change significantly, indicating good storage stability. The positive effect of the prepared nanoemulsion system on bioavailability was studied and confirmed using in vitro lipolysis and a caco-2 monolayer model.

scholarly journals Double Optimization of Rivastigmine-Loaded Nanostructured Lipid Carriers (NLC) for Nose-to-Brain Delivery Using the Quality by Design (QbD) Approach: Formulation Variables and Instrumental Parameters

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 599 ◽  
Author(s):  
Sara Cunha ◽  
Cláudia Pina Costa ◽  
Joana A. Loureiro ◽  
Jorge Alves ◽  
Andreia F. Peixoto ◽  
...  
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Drug Release ◽  
Quality By Design ◽  
Nanostructured Lipid Carriers ◽  
Brain Delivery ◽  
High Pressure Homogenization ◽  
Ultrasound Technique ◽  
Formulation Variables

Rivastigmine is a drug commonly used in the management of Alzheimer’s disease that shows bioavailability problems. To overcome this, the use of nanosystems, such as nanostructured lipid carriers (NLC), administered through alternative routes seems promising. In this work, we performed a double optimization of a rivastigmine-loaded NLC formulation for direct drug delivery from the nose to the brain using the quality by design (QbD) approach, whereby the quality target product profile (QTPP) was the requisite for nose to brain delivery. The experiments started with the optimization of the formulation variables (or critical material attributes—CMAs) using a central composite design. The rivastigmine-loaded NLC formulations with the best critical quality attributes (CQAs) of particle size, polydispersity index (PDI), zeta potential (ZP), and encapsulation efficiency (EE) were selected for the second optimization, which was related to the production methods (ultrasound technique and high-pressure homogenization). The most suitable instrumental parameters for the production of NLC were analyzed through a Box–Behnken design, with the same CQAs being evaluated for the first optimization. For the second part of the optimization studies, were selected two rivastigmine-loaded NLC formulations: one produced by ultrasound technique and the other by the high-pressure homogenization (HPH) method. Afterwards, the pH and osmolarity of these formulations were adjusted to the physiological nasal mucosa values and in vitro drug release studies were performed. The results of the first part of the optimization showed that the most adequate ratios of lipids and surfactants were 7.49:1.94 and 4.5:0.5 (%, w/w), respectively. From the second part of the optimization, the results for the particle size, PDI, ZP, and EE of the rivastigmine-loaded NLC formulations produced by ultrasound technique and HPH method were, respectively, 114.0 ± 1.9 nm and 109.0 ± 0.9 nm; 0.221 ± 0.003 and 0.196 ± 0.007; −30.6 ± 0.3 mV and −30.5 ± 0.3 mV; 97.0 ± 0.5% and 97.2 ± 0.3%. Herein, the HPH was selected as the most suitable production method, although the ultrasound technique has also shown effectiveness. In addition, no significant changes in CQAs were observed after 90 days of storage of the formulations at different temperatures. In vitro studies showed that the release of rivastigmine followed a non-Fickian mechanism, with an initial fast drug release followed by a prolonged release over 48 h. This study has optimized a rivastigmine-loaded NLC formulation produced by the HPH method for nose-to-brain delivery of rivastigmine. The next step is for in vitro and in vivo experiments to demonstrate preclinical efficacy and safety. QbD was demonstrated to be a useful approach for the optimization of NLC formulations for which specific physicochemical requisites can be identified.

scholarly journals CELASTROL NANOEMULGEL FORMULATION AND IN VITRO PENETRATION TEST

2020 ◽  
pp. 82-91
Author(s):  
NUR ALAM ABDULLAH ◽  
MAHDI JUFRI ◽  
ABDUL MUNIM ◽  
FADLINA CHANY SAPUTRI
Keyword(s):  
Particle Size ◽  
Ternary Phase ◽  
Ph Value ◽  
Ternary Phase Diagram ◽  
In Vitro Test ◽  
Inflammatory Drug ◽  
Anti Inflammatory ◽  
High Pressure Homogenizer ◽  
Skin Morphology

Objective: To obtain formulations of Celastrol (Cst) nanoemulgel via transdermal route. Celastrol is classified in BCS 4 class as an anti-inflammatory drug. These routes are considered to reduce the risk of Celastrol side effects and have the same characteristics as skin morphology. Methods: Celastrol nanoemulgel was prepared by a high-pressure homogenizer (HPH) technique. To find the optimum nanoemulsion area by using the Chemix 7.00 ternary phase program. Celastrol nanoemulgel was evaluated by measuring the particle size, PDI, morphology, zeta potential, stability tests and in vitro using Franz diffusion cell Results: Results showed the ideal formula based on the ternary phase diagram using chemix 7.00 is oil: smix: water (5:45:50), with particle size 89.9±5 nm, PDI 0.1, and zeta-21 mV. The morphological shape is quite spherical ≤ 100±5 nm. The pH value of this formula is 4.5, which compatible with the pH of the skin. The highest recovery rate of Celastrol and encapsulation efficiency (EE) were formulas 3 μg/ml and 5 μg/ml, with EE 91.70% and 94.54%, respectively. In vitro test results showed that the formula 3 μg/ml and 5 μg/ml give better penetration results than the formula 2.5 μg/ml. Thus, Celastrol nanoemulgel formula has good potential to be developed as a transdermal anti-inflammatory drug. Conclusion: Transdermal nanoemulgel containing Celastrol has been successfully developed with particle size ≤ 200±2 nm.

Fig. 31 Internals of colloid mill. (From Ref. 29.) colloid mills, typically equipped with rotor diameters of 10-30 cm, provide flow rates in the area of 4000-6000 L/hr, depending upon the viscosity. The key operating requirements of colloid mills are to feed the mill with a well-blended premix and to set the gap at the correct and reproducible setting. There is of-ten some difficulty with setting the gap at exactly the required distance, since the cali-bration of the gap can only be done at the manufacturer. This is less of a problem if the mill is well made and the product is not abrasive. If abrasive wear attacks the ro-tor or stator, the gap may become larger than the setting on the machine indicates. Colloid mills are generally used as "polishing" machines for emulsions or sus-pensions. That is, after the product has been totally and uniformly blended, the batch is passed through the colloid mill one or two times to further reduce the droplet or particle size. Whether or not multiple recycling passes are required depends on prod-uct requirements. Generally speaking, the colloid mill produces emulsions and suspen-sions with particle-size distributions smaller than the particle sizes obtainable using fixed gap rotor/stator mixers. They do represent an extra step in the process, and their use is suggested only when it is found that this added ability to disperse is necessary to produce a fine enough particle- or droplet-size product to enhance a product's stabil-ity. 3. Piston Homogenizers The most powerful device for producing emulsions and suspensions is the piston ho-mogenizer or high-pressure homogenizer. This device uses a high-power positive dis-placement piston-type pump to produce pressures of 3000-10,000 psig and then force

1998 ◽  
pp. 361-363
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Abrasive Wear ◽  
Droplet Size ◽  
High Power ◽  
Particle Size Distributions ◽  
Flow Rates ◽  
Extra Step ◽  
High Pressure Homogenizer ◽  
Multiple Recycling

scholarly journals Comparative Study on Curcumin Loaded in Golden Pompano (Trachinotus blochii) Head Phospholipid and Soybean Lecithin Liposomes: Preparation, Characteristics and Anti-Inflammatory Properties

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2328
Author(s):  
Xia Gao ◽  
Xiangzhou Yi ◽  
Zhongyuan Liu ◽  
Xiuping Dong ◽  
Guanghua Xia ◽  
...  
Keyword(s):  
Particle Size ◽  
Synergistic Effect ◽  
Storage Stability ◽  
Soybean Lecithin ◽  
Ζ Potential ◽  
Golden Pompano ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
And Storage

In this study, we compared the characteristics and in vitro anti-inflammatory effects of two curcumin liposomes, prepared with golden pompano head phospholipids (GPL) and soybean lecithin (SPC). GPL liposomes (GPL-lipo) and SPC liposomes (SPC-lipo) loaded with curcumin (CUR) were prepared by thin film extrusion, and the differences in particle size, ζ-potential, morphology, and storage stability were investigated. The results show that GPL-lipo and SPC-lipo were monolayer liposomes with a relatively small particle size and excellent encapsulation rates. However, GPL-lipo displayed a larger negative ζ-potential and better storage stability compared to SPC-lipo. Subsequently, the effects of phospholipids in regulating the inflammatory response of macrophages were evaluated in vitro, based on the synergistic effect with CUR. The results showed that both GPL and SPC exerted excellent synergistic effect with CUR in inhibiting the lipopolysaccharide (LPS)-induced secretion of nitric oxide (NO), reactive oxygen species (ROS), and pro-inflammatory genes (tumor necrosis factor (TNF)-α, interleukin 1β (IL-β), and interleukin 6 (IL-6)) in RAW264.7 cells. Interestingly, GPL-lipo displayed superior inhibitory effects, compared to SPC-lipo. The findings provide a new innovative bioactive carrier for development of stable CUR liposomes with good functional properties.

scholarly journals SYNTHESIS, SPECTRAL CHARACTERIZATION AND ANTIFUNGAL STUDIES ON LANTHANUM (III) AND PRASEODYMIUM (III) COMPLEXES WITH N2O2DIAZADIOXAMACROCYCLES

2020 ◽  
Vol 8 (11) ◽  
pp. 01-10
Author(s):  
Priti Tripathi ◽  
◽  
Akhilesh Kumar Srivastava ◽  
Om Prakash Pandey ◽  
Soumitra Kumar Sengupta ◽  
...  
Keyword(s):  
Particle Size ◽  
Biological Activity ◽  
Antifungal Activity ◽  
Schiff Bases ◽  
Lanthanide Complexes ◽  
Scherrer Formula ◽  
In Vitro Antifungal Activity ◽  
Nm Range

A novel series of N2O2diazadioxamacrocyclic complexes of type [Ln(mac)Cl3] has been synthesized via the condensation reactions of a 3-(phenyl/substituted phenyl)-4-amino-5-hydrazino-1,2,4-triazoles with salicylaldehyde and 1,4-dibromobutane in the presence of lanthanum(III) chloride and praseodymium(III) chloride in ethanol. All the newly synthesized compounds were characterized by elemental analysis, electronic absorption, IR, 1HNMR. The particle size of the complexes have been calculated from XRD spectral using Debye-Scherrer formula and these are found to be in 29-31 nm range. In order to evaluate the biological activity of Schiff bases and to assess the role of Ln(III) and Pr(III) metal on biological activity, the hydrazine triazole Schiff bases and their lanthanide complexes have been studies for in vitro antifungal activity against Fusariumoxysporum, CurvularialunataandColletotrichumfalcatum.

scholarly journals The study of biological activity nanomaterial in cultivation conditions pigs sperm and oocytes in vitro

1970 ◽  
pp. 256-260 ◽  
Author(s):  
O. V. Shcherbak ◽  
A. B. Ziuziun ◽  
O. S. Osypchuk ◽  
S. I. Kovtun ◽  
N. P. Halahan ◽  
...  
Keyword(s):  
Cell Culture ◽  
Biological Activity ◽  
Culture Medium ◽  
Culture Conditions ◽  
Cell Culture Medium ◽  
Animal Genetic Resources ◽  
Cultivation In Vitro ◽  
Breeding And Genetics ◽  
Positive Effect

Aim. To assess the biological activity of nanomaterial UFS/BSA/NANA of culture conditions with different concentrations of spermatozoa and the oocyte-cumulus complexes of pigs in vitro. Methods. For study biological activity in experiments used ejaculate cryopreserved sperms of three boars (Bank Animal Genetic Resources Institute of Animal Breeding and Genetics nd. a. M.V. Zubets of National Academy of Agrarian Science of Ukraine) and freshly prepared oocytes pigs. Results. In study effect of different concentrations NM (UFS/BSA/NANA) on viability gametes boar. The most active sperms when we add UFS/BSA/NANA in concentration 0.001 %. Adding UFS/BSA/NANA 0.1 % concentration in the cell culture medium has provided formation mature pigs oocytes for significantly higher level, which was 20.2 % more compared to the control and 18.7 % higher, when we add UFS/BSA/NANA in concentration 0.001 %. Conclusions. It is demonstrated the positive effect on defrosted boars sperms with adding UFS/BSA/NANA in concentration 0.001 %, their biological activity increased by 13.3 % compared with control. It is demonstration that add UFS/BSA/NANA in concentration 0.1 % in cell culture medium with pig’s oocytes, level of maturation increased by 20.2 %.Keywords: oocytes, sperms, pigs, cultivation in vitro, ultra-fine silica (UFS).

scholarly journals FORMULATION AND EVALUATION OF POLYMERIC NANOSUSPENSION OF NARINGENIN

2017 ◽  
Vol 9 (6) ◽  
pp. 60 ◽  
Author(s):  
R. Sumathi ◽  
S. Tamizharasi ◽  
T. Sivakumar
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Dissolution Rate ◽  
Oral Bioavailability ◽  
Safety Evaluation ◽  
Drug Formulation ◽  
High Pressure Homogenization ◽  
Erythrocyte Hemolysis ◽  
Poorly Soluble

Objective: The objective of this study was to formulate and evaluate the poorly soluble drug, naringenin (NAR) into nanosuspension to increase the solubility and enhance the dissolution rate and then improve its bioavailability.Methods: Nanosuspenion of naringenin (NARNS) was prepared using high-pressure homogenization method using Soya lecithin, Polaxamer-407, Polaxamer-188, Hydroxypropyl methyl cellulose (HPMC) and Tween-80. Ten formulations were prepared to show the effect of stabilizer and its ratio. D-α-Tocopheryl polyethene glycol succinate 1000 (TPGS) was added as a co-stabilizer. All these formulations were evaluated for their particle size, PDI, zeta potential, FT-IR study, drug content, saturation solubility studies, entrapment efficiency, in vitro permeability and in vitro drug release. The formulation was further evaluated for scanning electron microscope (SEM), differential scanning calorimetry (DSC) and Powder X-ray diffraction (P-XRD) and hemocompatibility assessment.Results: All the prepared formulations were in the nano size. The optimum concentration of the stabilizer was in the formulation was found 1:1.5:1 (drug: stabilizer: co-stabilizer ratio). Dramatic effect of the particle size reduction was found by the addition of the co-stabilizer (TPGS) in formulation N2 that has P. S 80.52±0.13 nm. The solubility and dissolution of NAR in the form of NARNS were significantly higher than those of pure NAR. SEM report shows that naringenin nanosuspension revealed a smooth texture. P-XRD crystallography diffraction and DSC studies indicated that the crystalline state of NAR was converted into amorphous nature. The safety evaluation showed that NARNS provided a lower rate of erythrocyte hemolysis. Conclusion: In this study, (NARNS) was successfully carried out by high-pressure homogenization technique and characterized. The physio-chemical characterization shown that crystalline naringenin was converted to a polymorphic form (DSC and P-XRD Study) which evidenced by enhanced dissolution rate in comparisons of the formulation with (NAR) pure drug. The NARNS has shown 7.5±0.4 fold increased relative bioavailability when compared to the NAR. The increased drug dissolution rate may have a significant impact in absorption which in turn the improved oral bioavailability of naringenin. Thus, this delivery system may prefer to improve the dissolution of poorly soluble drugs like NAR and thus enhanced oral bioavailability. The safety evaluation showed that nanoformulation (NF2) shows a lower rate of erythrocyte hemolysis. These findings suggest that the selected formulation may represent a promising new drug formulation for intravenous administration in the treatment of certain cancers.

scholarly journals Physical characteristics of nanoemulsion from chitosan/nutmeg seed oil and evaluation of its coating against microbial growth on strawberry

Food Research ◽  
2019 ◽  
pp. 821-827 ◽  
Author(s):  
R. Horison ◽  
F.O. Sulaiman ◽  
D. Alfredo ◽  
A.A. Wardana
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Microbial Growth ◽  
Seed Oil ◽  
Physical Characteristics ◽  
Particle Size Analyzer ◽  
High Pressure Homogenizer

The objectives of this research were to characterize nanoemulsion from chitosan/nutmeg seed oil and to evaluate its coating on fresh strawberry which stored at 10oC for 5 days. The ultraturrax and high-pressure homogenizer were used to prepare 1.34±0.25 - 5.79±1.61 nm of nanoemulsion size which confirmed by particle size analyzer. The morphology observed by SEM that exhibited the oil globules were covered by chitosan. They were aggregated and rough droplets. Interactions among the materials were observed using FTIR which led to the presence of a new peak at 1736 cm-1 . The coated strawberry by high-pressure homogenizer-emulsion showed the best result suppressing microbial (2.41±0.01) and mould-yeast (2.78±0.10) growth at the end of storage compared to control which were 3.37±0.02 and 3.69±0.14 for microbial and mould-yeast count respectively.

scholarly journals Lavandula angustifolia PROPAGATED IN IN VITRO CULTURES ON MEDIA CONTAINING AgNPs AND AuNPs – AN ALTERNATIVE TO SYNTHETIC PRESERVATIVES IN COSMETICS

2020 ◽  
Vol 357 (56) ◽  
pp. 5-18
Author(s):  
Paula JADCZAK ◽  
◽  
Danuta KULPA ◽  
Keyword(s):  
Particle Size ◽  
Culture Medium ◽  
Culture Media ◽  
Particle Diameter ◽  
Plant Tissues ◽  
Lavandula Angustifolia ◽  
Dehydroacetic Acid ◽  
Cosmetic Emulsions ◽  
Positive Effect

We determined the preservation properties of Lavandula angustifolia propagated on media with gold or silver nanoparticles with a particle size of 13 and 30 nm. Cosmetic emulsions prepared by using lavender tissue that was propagated on media containing AuNPs and AgNPs showed increased preservative capacities when compared with the control ones. In the case of control cosmetic emulsions, which had no added plant tissues or dehydroacetic acid and benzoic acid (DHA BA), bacterial and fungal colonies appeared after the second week of the experiment. The addition of lavender tissue propagated on media without AuNPs or AgNPs protected the tasted samples from microbial contamination; in this case, bacterial contamination was detected after 4 weeks and fungal contamination after 6 weeks. The addition of lavender tissue propagated on medium containing AgNPs with a particle size of 13 nm at a concentration of 1 mg · dm−3 prolonged the time of detection of bacteria colonies to 8 weeks (0.9) and this result was close and comparable to the effect of DHA BA. Higher concentrations of AgNPs in the culture medium, as well as a larger particle diameter (30 nm), resulted in the decreased preservative capacity of plant tissues. The presence of AuNPs in the culture media showed a positive effect on the antimicrobial activity of lavender; however, to a lesser degree than in the case of AgNPs. Disintegrated fragments of lavender tissue propagated on media containing 1 mg ∙ dm−3 AgNPs with particle size of 13 nm can be used to preserve short shelf life cosmetic emulsions.

Preparation of Platelet Membrane Microparticles with High Pressure Homogenization Method.

Blood ◽  
2007 ◽  
Vol 110 (11) ◽  
pp. 4022-4022
Author(s):  
Cui-ping Li ◽  
Jian OuYang ◽  
Cheng-yin Huang ◽  
Guang-yao Shi ◽  
Xiao-ping Pei
Keyword(s):  
High Pressure ◽  
Homogenization Method ◽  
Platelet Membrane ◽  
Preparation Technique ◽  
Mean Diameter ◽  
Repeated Freezing ◽  
Viral Contaminants ◽  
High Pressure Homogenizer ◽  
Membrane Microparticles

Abstract Objective To investigate the preparation technique of infusible platelet membrane microparticles (IPMs), and evaluate hemostatic function and effect of IPMs on pathological thrombogenicity after transfused into model of rabbit thrombocytopenia. Methods Whole bloods collected in the street were used to prepare platelet concentrates(PCs),white cells were removed by white cell filter, and red cells by centrifugation at 1000rpm in for 10min. After that, platelets were washed twice with 0.9% NaCl solution by repeated resuspension and centrifugation, and adjusted concentration to 2×109/ml with 0.9% NaCl. The washed platelets were disrupted by repeated freezing (at −80°) and thawing (at 25°) three times, and were heated at 60° for twenty hours to inactivate any viral contaminants. Finally, the heat 2 treated platelets were crushed by high pressure homogenizer to form IPMs. In this study, particle analyser was applied to mean diameter and the particle size distribution of IPMs, APCT to test the procoagulation activity of IPMs in vitro. Hemostatic function and effect of IPMs onpathological thrombogenicity were observed after IPMs were transfused into thrombocytopenia rabbitmodels. Results mean diameter of IPMs was from 200 to 300 nm. The procoagulation activity of 50Lg/ml of IPMs was equal to 250×109/L of fresh platelets. Rabbit ear bleeding time and APCT significantly shortened from two hours to twelve hours after transfusion of 2mg IPMs per Kg into thrombocytopenia rabbit models, but other indexes such as PT, APTT, Fg, and TT changed less. Conclusions IPMs possess good hemostatic function and less effect on pathological thrombogenicity. It is a kind of promising biologic hemostatic reagent.

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