scholarly journals Cellular dosimetry of [177Lu]Lu-DOTA-[Tyr3]octreotate radionuclide therapy: the impact of modeling assumptions on the correlation with in vitro cytotoxicity

2020 ◽  
Vol 7 (1) ◽  
Author(s):  
Giulia Tamborino ◽  
Marijke De Saint-Hubert ◽  
Lara Struelens ◽  
Dayana C. Seoane ◽  
Eline A. M. Ruigrok ◽  
...  
Keyword(s):  
Radionuclide Therapy ◽  
In Vitro Cytotoxicity ◽  
Cellular Dosimetry ◽  
The Impact

scholarly journals Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

2018 ◽  
Vol 21 (1s) ◽  
pp. 225s-241s ◽  
Author(s):  
Jaber Emami ◽  
Hessam Yousefian ◽  
Hojjat Sadeghi
Keyword(s):  
Cancer Cell Line ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
In Vitro Cytotoxicity ◽  
Release Time ◽  
Nanostructured Lipid Carrier ◽  
Brain Delivery ◽  
Solvent Evaporation Method ◽  
The Impact

In the present study, a transferrin-conjugated nanostructured lipid carrier (TF-NLCs) for brain delivery of artemisinin (ART) was developed. ART-loaded NLCs (ART-NLCs) were prepared using solvent evaporation method and the impact of various formulation or process variables on the responses were assessed using a Taguchi design. Optimized ART-NLC was then coupled with transferrin as targeting ligand and its in vitro cytotoxicity was investigated against U-87MG brain cancer cell line. As a result, the following values are suggested by the software to prepare the optimized formulation: 20 mg Compritol®, 0.25% Tween 80, 5 mg oleic acid, 2.5 mL dichloromethane and 4 min sonication. Mean particle size (PS), zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), mean release time (MRT) of adopted formulation were confirmed to be 145 ± 12.5 nm, 24.3 ± 1.5 mV, 0.513 ± 0.021, 82.3 ± 7.3 % and 24.0 ± 1.1 h, respectively. Following conjugation of optimized ART-NLCs with TF, PS and MRT were increased, while ZP, and EE were decreased significantly. TF-ART-NLCs showed higher cytotoxic activity compared to non-targeted NLCs and free drug. These results indicated that the TF-ART-NLCs could potentially be exploited as a delivery system for anticancer and antimalarial drug ART in brain tumors and malaria.

scholarly journals Physicochemical Investigations of Chitosan-Based Hydrogels Containing Aloe Vera Designed for Biomedical Use

Materials ◽  
2020 ◽  
Vol 13 (14) ◽  
pp. 3073 ◽  
Author(s):  
Anna Drabczyk ◽  
Sonia Kudłacik-Kramarczyk ◽  
Magdalena Głąb ◽  
Magdalena Kędzierska ◽  
Anna Jaromin ◽  
...  
Keyword(s):  
Chemical Structure ◽  
Aloe Vera ◽  
Lower Surface ◽  
Strength Properties ◽  
In Vitro Cytotoxicity ◽  
Force Microscopy ◽  
Atomic Force ◽  
Murine Fibroblasts ◽  
The Impact

In this work, synthesis and investigations on chitosan-based hydrogels modified with Aloe vera juice are presented. These materials were synthesized by UV radiation. Investigations involved analysis of chemical structure by FTIR spectroscopy, sorption properties in physiological liquids, strength properties by texture analyzer, surface topography by Atomic Force Microscopy (AFM technique), and in vitro cytotoxicity by MTT test using L929 murine fibroblasts. Particular attention was focused both on determining the impact of the amount and the molecular weight of the crosslinker used for the synthesis as well as on the introduced additive on the properties of hydrogels. It was proven that modified hydrogels exhibited higher swelling ability. Introduced additive affected the tensile strength of hydrogels—modified materials showed 23% higher elongation. The greater amount of the crosslinker used in the synthesis, the more compact the structure, leading to the lower elasticity and lower sorption of hydrogels was reported. Above 95%, murine fibroblasts remained viable after 24 h incubation with hydrogels. It indicates that tested materials did not exhibit cytotoxicity toward these lines. Additionally, materials with Aloe vera juice were characterized by lower surface roughness. Conducted investigations allowed us to state that such modified hydrogels may be considered as useful for biomedical purposes.

scholarly journals Evaluation of the Antimicrobial Efficacy of N-Acetyl-L-Cysteine, Rhamnolipids, and Usnic Acid—Novel Approaches to Fight Food-Borne Pathogens

2021 ◽  
Vol 22 (21) ◽  
pp. 11307
Author(s):  
Ondrej Chlumsky ◽  
Heidi J. Smith ◽  
Albert E. Parker ◽  
Kristen Brileya ◽  
James N. Wilking ◽  
...  
Keyword(s):  
Bacterial Growth ◽  
Biofilm Formation ◽  
Usnic Acid ◽  
Food Contamination ◽  
In Vitro Cytotoxicity ◽  
Confocal Scanning Laser Microscopy ◽  
Food Borne Pathogens ◽  
Food Borne ◽  
The Impact

In the food industry, the increasing antimicrobial resistance of food-borne pathogens to conventional sanitizers poses the risk of food contamination and a decrease in product quality and safety. Therefore, we explored alternative antimicrobials N-acetyl-L-cysteine (NAC), rhamnolipids (RLs), and usnic acid (UA) as a novel approach to prevent biofilm formation and reduce existing biofilms formed by important food-borne pathogens (three strains of Salmonella enterica and two strains of Escherichia coli, Listeria monocytogenes, Staphylococcus aureus). Their effectiveness was evaluated by determining minimum inhibitory concentrations needed for inhibition of bacterial growth, biofilm formation, metabolic activity, and biofilm reduction. Transmission electron microscopy and confocal scanning laser microscopy followed by image analysis were used to visualize and quantify the impact of tested substances on both planktonic and biofilm-associated cells. The in vitro cytotoxicity of the substances was determined as a half-maximal inhibitory concentration in five different cell lines. The results indicate relatively low cytotoxic effects of NAC in comparison to RLs and UA. In addition, NAC inhibited bacterial growth for all strains, while RLs showed overall lower inhibition and UA inhibited only the growth of Gram-positive bacteria. Even though tested substances did not remove the biofilms, NAC represents a promising tool in biofilm prevention.

scholarly journals Chemical Composition and Cytotoxicity of Kalanchoe pinnata Leaves Extracts prepared using Accelerated System Extraction (ASE)

2018 ◽  
Vol 13 (2) ◽  
pp. 1934578X1801300
Author(s):  
Kassia M. F. Pereira ◽  
Simone S. Grecco ◽  
Carlos R. Figueiredo ◽  
Jorge K. Hosomi ◽  
Mari U. Nakamura ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Organic Acids ◽  
Folk Medicine ◽  
Extraction Methods ◽  
In Vitro Cytotoxicity ◽  
Human Leukemia ◽  
Crude Extracts ◽  
Kalanchoe Pinnata ◽  
The Impact

Kalanchoe pinnata (Crassulaceae) is a medicinal plant distributed in several areas of the World. Their leaves have been used, in folk medicine, for anxiety and sleep disorders among other proposes. Chemically, this plant is composed by organic acids, flavonoids, bufadienolides, triterpenoids and some ubiquitous compounds. In this study, the fresh leaves of K. pinnata were extracted in an accelerated solvent extraction (ASE) system using H2O (cold and hot) as well as with EtOH:H2O 1:1. The obtained crude extracts were analyzed by HPLC-UV-MS. As a result, were identified organic acids and flavonoids, these being quercetin-3- O-α-L-arabinopyranosyl-(1→2)-α-L-rhamnopyranoside, kaempferol-3- O-α-L-arabinopiranosyl-(1→2)-α-L-rhamnopyranoside, quercitrin, and trans- p-coumaryl glutaric acid the main compounds in the studied extracts. Obtained results revealed the predominance of flavonoids in extracts prepared using hot H2O (70 26 α 2.19%) or EtOH:H2O 1:1 (74.65 α 5.39%) while a reduction in the amount of these compounds was observed in the extracts prepared using cold H2O (54.41 α 2.93%). Additionally, crude extracts from leaves of K. pinnata extracted with hot H2O and EtOH:H2O 1:1 showed in vitro cytotoxicity on five tested cancer cell lines: murine melanoma (B16F10), human melanoma (A2058), human cervical carcinoma (HeLa), human leukemia (HL-60), and human glioblastoma (U87-MG), with IC50 values in the range of 10.6 α 2.5-91.3 α 7.2 μg/mL. On the other hand, the extract prepared using cold H2O displayed reduced potential. These crude extracts were also tested against human foreskin fibroblasts (non-tumorigenic cells) showing IC50 values ranging from 79.5 to 90.2 μg/mL. In conclusion, our results showed the impact that different extraction methods have on the chemical composition and pharmacological activity, which are notable for the anticancer activity associated to flavonoids.

scholarly journals Development and Evaluation of Lyophilized Methotrexate Nanosuspension using Quality by Design Approach

2021 ◽  
Vol 68 (4) ◽  
pp. 861-881
Author(s):  
Trupti Powar ◽  
Ashok Hajare ◽  
Ravindra Jarag ◽  
Sopan Nangare
Keyword(s):  
Central Composite Design ◽  
Quality By Design ◽  
Average Particle Size ◽  
In Vitro Cytotoxicity ◽  
Average Particle ◽  
Formulation Development ◽  
Process Factors ◽  
The Impact ◽  
Central Composite

With the application of the quality by design (QbD) approach, a high-pressure homogenizer (HPH) methodology was employed to develop methotrexate nanosuspension (MTX-NS) to boost bioavailability. The Ishikawa diagram was used to analyze potential risk factors in formulation development. To screen and study the impact of various formulation and process factors on the critical quality attributes (CQA), the Placket–Burman design and central composite design were utilized. The number of HPH cycles, poloxamer 188 concentration, and tween 80 concentration were shown to be significant parameters (P<0.05), that were further optimized using Central Composite Design. The zeta potential of optimized lyophilized MTX-NS was determined to be –11.6 ± 7.52 mV and the average particle size was 260 ± 0.25 nm. In vitro cytotoxicity experiments revealed a greater than 80% inhibition, with apoptotic cells shrinking, fragmentation, and cell death. Furthermore, the Cmax and AUC0-t were increased by 2.53 and 8.83 folds, respectively. The relative bioavailability of MTX-NS was found to be 8.83 times higher than that of MTX-aqueous dispersion. As a result, the QbD method resulted in the development of a lyophilized MTX-NS with process understanding and control based on quality risk management.

scholarly journals In vitro cytotoxicity assessment of ferulic, caffeic and p-coumaric acids on human renal cancer cells

2020 ◽  
Vol 17 (1) ◽  
pp. 1-12
Author(s):  
Rita Caparica ◽  
André Rolim Baby ◽  
Tânia Almeida ◽  
João Guilherme Costa
Keyword(s):  
Cancer Cells ◽  
Renal Cancer ◽  
Biological Effects ◽  
Biological Properties ◽  
In Vitro Cytotoxicity ◽  
Hydroxycinnamic Acids ◽  
Therapeutic Uses ◽  
Cytotoxicity Assessment ◽  
The Impact

Bioactive compounds from natural sources have been extensively studied as potential therapeutic agents, due to their chemical, structural, and biological properties. Among them, hydroxycinnamic acids emerge with a very interesting pharmacological potential to prevent and treat several diseases, including cancer. However, while some studies support their anticancer activity, other reports indicate otherwise. Since the impact of these compounds on renal cancer is not well established, further studies are needed to better understand their biological effects and their potential therapeutic uses in this cancer. In this work, the cytotoxicity of three hydroxycinnamic acids: ferulic, caffeic and p-coumaric acids, was evaluated on 786-O human renal cancer cells by MTT and CV assays. At concentrations up to 250 µM, none of the studied natural compounds showed cytotoxic effects to 786-O cell line. At higher concentrations (500 and 1000 µM), while ferulic acid also did not significantly influence the cell viability of 786-O cells, p-coumaric and caffeic acids decreased the renal cancer cells viability. Nevertheless, further studies on the biological activity of these compounds, using other methodologies, as well as using other cancer cell models, should be performed.

scholarly journals Is aggregated synthetic amorphous silica toxicologically relevant?

2020 ◽  
Vol 17 (1) ◽  
Author(s):  
Sivakumar Murugadoss ◽  
Sybille van den Brule ◽  
Frederic Brassinne ◽  
Noham Sebaihi ◽  
Jorge Mejia ◽  
...  
Keyword(s):  
Amorphous Silica ◽  
Ad Hoc ◽  
Aggregate Size ◽  
Industrial Applications ◽  
In Vitro Cytotoxicity ◽  
Biologically Active ◽  
Supernatant Fraction ◽  
Synthetic Amorphous Silica ◽  
The Impact

Abstract Background The regulatory definition(s) of nanomaterials (NMs) frequently uses the term ‘agglomerates and aggregates’ (AA) despite the paucity of evidence that AA are significantly relevant from a nanotoxicological perspective. This knowledge gap greatly affects the safety assessment and regulation of NMs, such as synthetic amorphous silica (SAS). SAS is used in a large panel of industrial applications. They are primarily produced as nano-sized particles (1–100 nm in diameter) and considered safe as they form large aggregates (> 100 nm) during the production process. So far, it is indeed believed that large aggregates represent a weaker hazard compared to their nano counterpart. Thus, we assessed the impact of SAS aggregation on in vitro cytotoxicity/biological activity to address the toxicological relevance of aggregates of different sizes. Results We used a precipitated SAS dispersed by different methods, generating 4 ad-hoc suspensions with different aggregate size distributions. Their effect on cell metabolic activity, cell viability, epithelial barrier integrity, total glutathione content and, IL-8 and IL-6 secretion were investigated after 24 h exposure in human bronchial epithelial (HBE), colon epithelial (Caco2) and monocytic cells (THP-1). We observed that the de-aggregated suspension (DE-AGGR), predominantly composed of nano-sized aggregates, induced stronger effects in all the cell lines than the aggregated suspension (AGGR). We then compared DE-AGGR with 2 suspensions fractionated from AGGR: the precipitated fraction (PREC) and the supernatant fraction (SuperN). Very large aggregates in PREC were found to be the least cytotoxic/biologically active compared to other suspensions. SuperN, which contains aggregates larger in size (> 100 nm) than in DE-AGGR but smaller than PREC, exhibited similar activity as DE-AGGR. Conclusion Overall, aggregation resulted in reduced toxicological activity of SAS. However, when comparing aggregates of different sizes, it appeared that aggregates > 100 nm were not necessarily less cytotoxic than their nano-sized counterparts. This study suggests that aggregates of SAS are toxicologically relevant for the definition of NMs.

scholarly journals Cytotoxicity and Microbicidal Activity of Commonly Used Organic Solvents: A Comparative Study and Application to a Standardized Extract from Vaccinium macrocarpon

Toxics ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 92
Author(s):  
Yana Ilieva ◽  
Lyudmila Dimitrova ◽  
Maya Margaritova Zaharieva ◽  
Mila Kaleva ◽  
Petko Alov ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Dimethyl Sulfoxide ◽  
Organic Solvents ◽  
Cell Lines ◽  
In Vitro Cytotoxicity ◽  
International Standards ◽  
Vaccinium Macrocarpon ◽  
Bioactive Molecules ◽  
The Impact

The cytotoxicity and microbicidal capacity of seven organic solvents commonly applied for studying plant extracts and bioactive compounds were systematically investigated based on international standards. Four cell lines of normal (CCL-1, HaCaT) or tumor (A-375, A-431) tissue origin, seven bacterial and one fungal strain were used. The impact of the least toxic solvents in the determination of in vitro cytotoxicity was evaluated using a standardized extract from Vaccinium macrocarpon containing 54.2% v/v proanthocyanidins (CystiCran®). The solvents ethanol, methoxyethanol and polyethylene glycol were the least cytotoxic to all cell lines, with a maximum tolerated concentration (MTC) between 1 and 2% v/v. Ethanol, methanol and polyethylene glycol were mostly suitable for antimicrobial susceptibility testing, with minimum inhibitory concentrations (MICs) ≥ 25% v/v. The MTC values of the solvents dimethyl sulfoxide, dimethoxyethane and dimethylformamide varied from 0.03% to 1.09% v/v. The MICs of dimethyl sulfoxide, methoxyethanol and dimethoxyethane were in the range of 3.125–25% v/v. The cytotoxic effects of CystiCran® on eukaryotic cell lines were directly proportional to the superimposed effect of the solvents used. The results of this study can be useful for selecting the appropriate solvents for in vitro estimation of the cytotoxic and growth inhibitory effects of bioactive molecules in eukaryotic and prokaryotic cells.

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