Eudragit S100 Entrapped Liposome for Curcumin Delivery: Anti-Oxidative Effect in Caco-2 Cells

Curcumin is a natural polyphenol with strong antioxidant activity. However, this molecule shows a very poor bioavailability, instability, and rapid metabolism in vivo. In this work curcumin was loaded in Eudragit-coated liposomes to create a gastroresistant carrier, able to protect its load from degradation and free it at the site of absorption in the colon region. Small unilamellar vesicles were prepared and coated with Eudragit by a pH-driven method. The physico-chemical properties of the prepared systems were assessed by light scattering, transmission electron microscopy, infrared spectroscopy, and differential scanning calorimetry. The uptake of vesicles by Caco-2 cells and the anti-oxidant activity in cells were evaluated. The produced vesicles showed dimensions of about forty nanometers that after covering with Eudragit resulted to have micrometric dimensions at acid pH. The experiments showed that at pH > 7.0 the polymeric coating dissolves, releasing the nanometric liposomes and allowing them to enter Caco-2 cells. Delivered curcumin loaded vesicles were then able to decrease significantly ROS levels as induced by H2O2 in Caco-2 cells. The proposed work showed the possibility of realizing effective gastroresistant curcumin liposome formulations for the delivery of antioxidant molecules to Caco-2 cells, potentially applicable to the treatment of pathological conditions related to intestinal oxidative stress.

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Optimization of Innovative Three-Dimensionally-Structured Hybrid Vesicles to Improve the Cutaneous Delivery of Clotrimazole for the Treatment of Topical Candidiasis

Pharmaceutics ◽

10.3390/pharmaceutics11060263 ◽

2019 ◽

Vol 11 (6) ◽

pp. 263 ◽

Cited By ~ 4

Author(s):

Maria Letizia Manca ◽

Iris Usach ◽

José Esteban Peris ◽

Antonella Ibba ◽

Germano Orrù ◽

...

Keyword(s):

Electron Microscopy ◽

Transmission Electron Microscopy ◽

Chemical Properties ◽

Chemical Characterization ◽

Yeast Cells ◽

Unilamellar Vesicles ◽

Transmission Electron ◽

Physico Chemical

New three-dimensionally-structured hybrid phospholipid vesicles, able to load clotrimazole in a high amount (10 mg/mL), were obtained for the first time in this work by significantly reducing the amount of water (≤10%), which was replaced with a mixture of glycerol and ethanol (≈90%). A pre-formulation study was carried out to evaluate the effect of both the composition of the hydrating medium and the concentration of the phospholipid on the physico-chemical properties of hybrid vesicles. Four different three-dimensionally-structured hybrid vesicles were selected as ideal systems for the topical application of clotrimazole. An extensive physico-chemical characterization performed using transmission electron microscopy (TEM), cryogenic transmission electron microscopy (cryo-TEM), 31P-NMR, and small-angle X-ray scattering (SAXS) displayed the formation of small, multi-, and unilamellar vesicles very close to each other, and was capable of forming a three-dimensional network, which stabilized the dispersion. Additionally, the dilution of the dispersion with water reduced the interactions between vesicles, leading to the formation of single unilamellar vesicles. The evaluation of the in vitro percutaneous delivery of clotrimazole showed an improved drug deposition in the skin strata provided by the three-dimensionally-structured vesicles with respect to the commercial cream (Canesten®) used as a reference. Hybrid vesicles were highly biocompatible and showed a significant antifungal activity in vitro, greater than the commercial cream Canesten®. The antimycotic efficacy of formulations was confirmed by the reduced proliferation of the yeast cells at the site of infection in vivo. In light of these results, clotrimazole-loaded, three-dimensionally-structured hybrid vesicles appear to be one of the most innovative and promising formulations for the treatment of candidiasis infections.

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Pharmacokinetic Evaluation of 99mTc-radiolabeled Solid Lipid Nanoparticles and Chitosan Coated Solid Lipid Nanoparticles

Current Drug Metabolism ◽

10.2174/1389200220666191112145808 ◽

2020 ◽

Vol 20 (13) ◽

pp. 1044-1052

Author(s):

Nasrin Abbasi Gharibkandi ◽

Sajjad Molavipordanjani ◽

Jafar Akbari ◽

Seyed Jalal Hosseinimehr

Keyword(s):

Solid Lipid Nanoparticles ◽

Lipid Nanoparticles ◽

High Resistivity ◽

Scanning Calorimetry ◽

Liver Uptake ◽

Solid Lipid ◽

Transmission Electron ◽

Main Portion ◽

Pharmacokinetic Behavior

Background: Solid Lipid Nanoparticles (SLNs) possess unique in vivo features such as high resistivity, bioavailability, and habitation at the target site. Coating nanoparticles with polymers such as chitosan greatly affects their pharmacokinetic behavior, stability, tissue uptake, and controlled drug delivery. The aim of this study was to prepare and evaluate the biodistribution of 99mTc-labeled SLNs and chitosan modified SLNs in mice. Methods: 99mTc-oxine was prepared and utilized to radiolabel pre-papered SLNs or chitosan coated SLNs. After purification of radiolabeled SLNs (99mTc-SLNs) and radiolabeled chitosan-coated SLNs (99mTc-Chi-SLNs) using Amicon filter, they were injected into BALB/c mice to evaluate their biodistribution patterns. In addition, nanoparticles were characterized using Transmission Electron Microscopy (TEM), Fourier-transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Powder Diffraction (XRD) and Dynamic Light Scattering (DLS). Results: 99mTc-oxine with high radiochemical purity (RCP~100%) and stability (RCP > 97% at 24 h) was used to provide 99mTc-SLNs and 99mTc-Chi-SLNs with high initial RCP (100%). TEM image and DLS data suggest 99mTc- SLNs susceptibility to aggregation. To that end, the main portion of 99mTc-SLNs radioactivity accumulates in the liver and intestines, while 99mTc-Chi-SLNs sequesters in the liver, intestines and kidneys. The blood radioactivity of 99mTc-Chi-SLNs was higher than that of 99mTc-SLNs by 7.5, 3.17 and 3.5 folds at 1, 4 and 8 h post-injection. 99mTc- Chi-SLNs uptake in the kidneys in comparison with 99mTc-SLNs was higher by 37.48, 5.84 and 11 folds at 1, 4 and 8h. Conclusion: The chitosan layer on the surface of 99mTc-Chi-SLNs reduces lipophilicity in comparison with 99mTc- SLNs. Therefore, 99mTc-Chi-SLNs are less susceptible to aggregation, which leads to their lower liver uptake and higher kidney uptake and blood concentration.

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Radiation-induced Grafting of Styrene onto Polyethylene Films for Preparation of Cation Exchange Membranes: Effect of Crosslinking+

Journal of Applied Membrane Science & Technology ◽

10.11113/amst.v2i1.4 ◽

2017 ◽

Vol 2 (1) ◽

Author(s):

M. M. Nasef ◽

H. Saidi ◽

A. H. Yahaya

Keyword(s):

Cation Exchange ◽

Chemical Properties ◽

Exchange Capacity ◽

Gravimetric Analysis ◽

Scanning Calorimetry ◽

Swelling Properties ◽

Ion Exchange Capacity ◽

Physico Chemical ◽

Styrene Divinylbenzene ◽

Radiation Induced

Crosslinked cation exchange membranes bearing sulfonic acid groups (PE-g-PSSA/DVB) were prepared by radiationinduced grafting of styrene/divinylbenzene (DVB) mixtures onto low density polyethylene (PE) films followed by sulfonation reactions. The effect of addition of DVB (2 and 4%) on the grafting behavior and the physico-chemical properties of the membranes such as ion exchange capacity, swelling and ionic conductivity were evaluated incorrelation with grafting yield (Y%). The structural and thermal properties of the membranes were also studied using differential scanning calorimetry (DSC) and thermal gravimetric analysis (TGA), respectively. Crosslinking with DVB was found to considerably affect the properties of the membranes in a way that reduces the swelling properties and enhances the chemical stability. The ion conductivity of the crosslinked membranes recorded a level of 10–2 S/cm at sufficient grafting yield (28%) despite the reduction caused by the formation of crosslinking structure. The results of this work suggest that membranes prepared in this study are potential alternatives for various electrochemical applications.

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Mining a Nanoparticle Dataset, Compiled Within the MODENA-COST Action

Research Anthology on Synthesis, Characterization, and Applications of Nanomaterials ◽

10.4018/978-1-7998-8591-7.ch071 ◽

2021 ◽

pp. 1706-1724

Author(s):

Sabine Van Miert ◽

Jan Creylman ◽

Geert R. Verheyen

Keyword(s):

Chemical Properties ◽

In Vitro Testing ◽

Cost Action ◽

Robust Model ◽

Physico Chemical ◽

Classification And Regression ◽

Toxic Potential ◽

Sheer Number

Engineered nanomaterials (ENM) have new or enhanced physico-chemical properties compared to their micron-sized counterparts, but may also have an increased toxic potential. Animal and in vitro testing are typically employed to investigate the toxic effects of (nano)materials. The sheer number of ENMs and their physico-chemical parameters make it impossible to only use in vivo and in vitro testing, and modelling technologies are also deployed to find relationships between ENM parameters and toxicity. A heterogenous dataset containing information on 192 nanoparticle endpoints was compiled within the MODENA COST-Action consortium. Here, the available data was mined to identify relationships between nanoparticle properties and cell-death as measured with four cytotoxicity assays. ANOVA, collinearity analyses and classification and regression trees gave indications on potential relations between the NP-properties and toxicity, but could not deliver a robust model. More information and datapoints are necessary to build well-validated models.

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In Vitro Physico-Chemical Characterization and Standardized In Vivo Evaluation of Biocompatibility of a New Synthetic Membrane for Guided Bone Regeneration

Materials ◽

10.3390/ma12071186 ◽

2019 ◽

Vol 12 (7) ◽

pp. 1186

Author(s):

Lívia da Costa Pereira ◽

Carlos Fernando de Almeida Barros Mourão ◽

Adriana Terezinha Neves Novellino Alves ◽

Rodrigo Figueiredo de Brito Resende ◽

Marcelo José Pinheiro Guedes de Uzeda ◽

...

Keyword(s):

Bone Regeneration ◽

Chemical Properties ◽

Chemical Characterization ◽

Guided Bone Regeneration ◽

Tissue Reaction ◽

In Vivo Evaluation ◽

Physico Chemical ◽

Tissue Reactions

This study’s aim was to evaluate the biocompatibility and bioabsorption of a new membrane for guided bone regeneration (polylactic-co-glycolic acid associated with hydroxyapatite and β-tricalcium phosphate) with three thicknesses (200, 500, and 700 µm) implanted in mice subcutaneously. Scanning electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy, and the quantification of carbon, hydrogen and nitrogen were used to characterize the physico-chemical properties. One hundred Balb-C mice were divided into 5 experimental groups: Group 1—Sham (without implantation); Group 2—200 μm; Group 3—500 μm; Group 4—700 μm; and Group 5—Pratix®. Each group was subdivided into four experimental periods (7, 30, 60 and 90 days). Samples were collected and processed for histological and histomorphometrical evaluation. The membranes showed no moderate or severe tissue reactions during the experimental periods studied. The 500-μm membrane showed no tissue reaction during any experimental period. The 200-μm membrane began to exhibit fragmentation after 30 days, while the 500-μm and 700-µm membranes began fragmentation at 90 days. All membranes studied were biocompatible and the 500 µm membrane showed the best results for absorption and tissue reaction, indicating its potential for clinical guided bone regeneration.

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Synthesis and Cytotoxicity Studies of Wood-Based Cationic Cellulose Nanocrystals as Potential Immunomodulators

Nanomaterials ◽

10.3390/nano10081603 ◽

2020 ◽

Vol 10 (8) ◽

pp. 1603

Author(s):

Yusha Imtiaz ◽

Beza Tuga ◽

Christopher W. Smith ◽

Alexander Rabideau ◽

Long Nguyen ◽

...

Keyword(s):

Cellulose Nanocrystals ◽

Chemical Properties ◽

Neutral Red ◽

Cationic Polymers ◽

Experimental Conditions ◽

Physiological Processes ◽

Transmission Electron ◽

Physico Chemical ◽

Cytotoxicity Studies ◽

Low Cytotoxicity

Polysaccharides have been shown to have immunomodulatory properties. Modulation of the immune system plays a crucial role in physiological processes as well as in the treatment and/or prevention of autoimmune and infectious diseases. Cellulose nanocrystals (CNCs) are derived from cellulose, the most abundant polysaccharide on the earth. CNCs are an emerging class of crystalline nanomaterials with exceptional physico-chemical properties for high-end applications and commercialization prospects. The aim of this study was to design, synthesize, and evaluate the cytotoxicity of a series of biocompatible, wood-based, cationic CNCs as potential immunomodulators. The anionic CNCs were rendered cationic by grafting with cationic polymers having pendant +NMe3 and +NH3 moieties. The success of the synthesis of the cationic CNCs was evidenced by Fourier transform infrared spectroscopy, dynamic light scattering, zeta potential, and elemental analysis. No modification in the nanocrystals rod-like shape was observed in transmission electron microscopy and atomic force microscopy analyses. Cytotoxicity studies using three different cell-based assays (MTT, Neutral Red, and LIVE/DEAD®) and three relevant mouse and human immune cells indicated very low cytotoxicity of the cationic CNCs in all tested experimental conditions. Overall, our results showed that cationic CNCs are suitable to be further investigated as immunomodulators and potential vaccine nanoadjuvants.

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Potential Applications of Biphosphonates in Dental Surgical Implants

International Journal of Immunopathology and Pharmacology ◽

10.1177/039463200702000304 ◽

2007 ◽

Vol 20 (3) ◽

pp. 455-465 ◽

Cited By ~ 6

Author(s):

D. Berardi ◽

T. Carlesi ◽

F. Rossi ◽

M. Calderini ◽

R. Volpi ◽

...

Keyword(s):

Alveolar Bone ◽

Chemical Properties ◽

Osteonecrosis Of The Jaw ◽

In Vivo Experiments ◽

Surgical Implants ◽

Physico Chemical ◽

Potential Applications ◽

Collateral Effect

Biphosphonates are largely used for their unquestionable properties of inhibiting bone resorption by osteoclast in the treatment of various osteometabolic illnesses such as osteoporosis, multiple myeloma, tumors which metastasize to the bone and malignant hypercalcemia. In this literature review the physico-chemical properties, biologic activities and the mechanisms of action of biphosphonates are described. The use of these drugs is discussed, analyzing the quantity of results which have emerged through in vitro and in vivo experiments on animal models. In this study the efficiency of these drugs is demonstrated in contrasting the osteolitic processes of the alveolar bone, in promoting the neoformation and in bettering the quality of bone implants. However, it is important to draw attention to a worrying correlation which has emerged during the last 3–4 years, between osteonecrosis of the jaw (ONJ) and the systemic administration of aminobiphosphonates. This collateral effect did not emerge following the use of non-aminobiphosphonates. The aim of this revie w is to identify the guidelines for the use of biphosphonates in oral implant surgery.

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Characterization of Spent Catalysts during Hydrodemetallization of Atmosphere Residue

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.236-238.538 ◽

2011 ◽

Vol 236-238 ◽

pp. 538-542

Author(s):

Yong Jun Liu

Keyword(s):

Chemical Properties ◽

Analytical Techniques ◽

Resonance Spectroscopy ◽

Gravimetric Analysis ◽

X Ray Diffraction ◽

Transmission Electron ◽

Physico Chemical ◽

Spent Catalysts ◽

C Nmr

The deactivation behavior of industrial hydrodemetallization catalysts was investigated in the presented work. The main objective of the study is to contribute to a better understanding of the nature of the coke and metal deposition on the used catalysts by applying chemical analysis and various advanced analytical techniques, such as X-ray diffraction analysis (XRD), thermal gravimetric analysis (TGA), transmission electron microscopy (TEM), and solid-state carbon-13 nuclear magnetic resonance spectroscopy (13C NMR). The results are discussed scientifically based on the physico–chemical properties of origin and used catalysts.

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Solidification of Nanostructured Lipid Carriers Loaded Testosterone Undecanoate: In Vivo and In Vitro Study

Drug Research ◽

10.1055/a-0573-9132 ◽

2018 ◽

Vol 68 (08) ◽

pp. 457-464

Author(s):

Yabing Hua ◽

Wanqing Li ◽

Zhou Cheng ◽

Ziming Zhao ◽

Xiaoxing Yin ◽

...

Keyword(s):

In Vitro Study ◽

Cell Permeability ◽

Vacuum System ◽

Protective Agent ◽

Scanning Calorimetry ◽

Testosterone Undecanoate ◽

Transmission Electron ◽

Dissolution In Vitro

To enhance the bioavailability of testosterone undecanoate (TU) and overcome the current problem of soft capsules (Andriol Testocaps®), Nano-structured lipid carriers (NLC) for TU was developed. First, suspension of TU-loaded NLC (TU-NLC) was prepared by high pressure homogenization; then adsorbent or a protective agent β-cyclodextrin was used to solidify the suspension through a vacuum system; finally, the solid powder of TU-loaded NLC (solid TU-NLC) was filled into hard capsules. The characteristics of solid TU-NLC, were investigated in vitro and vivo. The particle size of TU-NLC was about 273.3 nm, the potential was 0.156±0.04. Transmission electron microscope (TEM) revealed that the NLC was spherical and uniform. Differential scanning calorimetry (DSC) suggested the drug had been encapsulated into NLC lipid matrix. The drug release proved that solid TU-NLC showed a higher dissolution in vitro. The CaCO-2 cell permeability showed that solid TU-NLC could enhance trans-membrane absorption of the TU. Moreover, the AUC of solid TU-NLC formulations (4304±550.50 μg/L*min) was higher than commercial product Andriol Testocaps® (3075±372.50 μg/L*min). In conclusion, solid TU-NLC could enhance the rate of dissolution, and had a relatively higher bioavailability than Andriol Testocaps® in vivo Graphical Abstract.

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Evaluation of the Physico-Chemical Properties of Liposomes Assembled from Bioconjugates of Anisic Acid with Phosphatidylcholine

International Journal of Molecular Sciences ◽

10.3390/ijms222313146 ◽

2021 ◽

Vol 22 (23) ◽

pp. 13146

Author(s):

Hanna Pruchnik ◽

Anna Gliszczyńska ◽

Aleksandra Włoch

Keyword(s):

Phase Transition ◽

Lipid Bilayer ◽

Chemical Properties ◽

Main Phase ◽

Cancer Therapies ◽

Dependent Manner ◽

Scanning Calorimetry ◽

Physico Chemical ◽

Anisic Acid ◽

The Impact

The aim of this work was the evaluation of the physico-chemical properties of a new type of liposomes that are composed of DPPC and bioconjugates of anisic acid with phosphatidylcholine. In particular, the impact of modified anisic acid phospholipids on the thermotropic parameters of liposomes was determined, which is crucial for using them as potential carriers of active substances in cancer therapies. Their properties were determined using three biophysical methods, namely differential scanning calorimetry (DSC), steady-state fluorimetry and attenuated total reflectance Fourier transform infrared spectroscopy (ATR-FTIR). Moreover, temperature studies of liposomes composed of DPPC and bioconjugates of anisic acid with phosphatidylcholine provided information about the phase transition, fluidity regarding chain order, hydration and dynamics. The DSC results show that the main phase transition peak for conjugates of anisic acid with phosphatidylcholine molecules was broadened and shifted to a lower temperature in a concentration- and structure-dependent manner. The ATR-FTIR results and the results of measurements conducted using fluorescent probes located at different regions in the lipid bilayer are in line with DSC. The results show that the new bioconjugates with phosphatidylcholine have a significant impact on the physico-chemical properties of a membrane and cause a decrease in the temperature of the main phase transition. The consequence of this is greater fluidity of the lipid bilayer.

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