scholarly journals Synthesis of Biocompatible and Environmentally Nanofibrous Mats Loaded with Moxifloxacin as a Model Drug for Biomedical Applications

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1029
Author(s):  
Mahmoud H. Teaima ◽  
Fatma A. Abdelnaby ◽  
Maha Fadel ◽  
Mohamed A. El-Nabarawi ◽  
Kamel R. Shoueir
Keyword(s):  
Pathogenic Bacteria ◽  
Guest Molecule ◽  
Pure Water ◽  
Electrospun Nanofibers ◽  
In Vitro Cytotoxicity ◽  
Total Antioxidant ◽  
Synthetic Routes ◽  
Model Drug ◽  
Mcf 7

Biopolymeric chitosan structure (Cs) is rationally investigated owing to its potentiality in pharmaceutical applications. The synthetic routes of biomimetic Cs-based blend electrospun nanofibers were studied. Herein, biocompatible crosslinked electrospun polyvinyl alcohol (PVA)/Cs-reduced gold nanoparticles (Cs(Rg))/β-CD (beta-cyclodextrin) in pure water were fabricated. To this end, supportive PVA as a carrier, Cs bio modifier, and gold reductant and β-CD as smoother, inclusion guest molecule, and capping agent exhibit efficient entrapment of moxifloxacin (Mox) and consequently accelerate release. Besides, PVA/Cs(Rg)/β-CD paves towards controlled drug encapsulation-release affinity, antimicrobial, and for wound dressing. Without losing the nanofiber structure, the webs prolonged stability for particle size and release content up to 96.4%. The synergistic effect of the nanoformulation PVA/Cs(Rg)/β-CD against pathogenic bacteria, fungus, and yeast, including Staphylococcus aureus, Escherichia coli, Candida albicans, and Aspergillus niger, posed clear zones up to 53 φmm. Furthermore, a certain combination of PVA/Cs (Rg)/β-CD showed a total antioxidant capacity of 311.10 ± 2.86 mg AAE/g sample. In vitro cytotoxicity assay of HePG2 and MCF-7 NF6 can eradicate 34.8 and 29.3 µg/mL against selected cells.

Formulation, Characterization and In vitro Cytotoxicity of 5-Fluorouracil Loaded Polymeric Electrospun Nanofibers for the Treatment of Skin Cancer

2019 ◽  
Vol 13 (2) ◽  
pp. 114-128 ◽  
Author(s):  
Gayatri Patel ◽  
Bindu K.N. Yadav
Keyword(s):  
Skin Cancer ◽  
Basal Cell Carcinoma ◽  
Cell Viability ◽  
Cell Carcinoma ◽  
Basal Cell ◽  
Fiber Diameter ◽  
Electrospun Nanofibers ◽  
In Vitro Cytotoxicity ◽  
Fractional Factorial

Background: The purpose of this study was to formulate, characterize and conduct in vitro cytotoxicity of 5-fluorouracil loaded polymeric electrospun nanofibers for the treatment of skin cancer. The patents on electrospun nanofibers (US9393216B2), (US14146252), (WO2015003155A1) etc. helped in the selection of polymers and method for the preparation of nanofibers. Methods: In the present study, the fabrication of nanofibers was done using a blend of chitosan with polyvinyl alcohol and processed using the electrospinning technique. 5-fluorouracil with known chemotherapeutic potential in the treatment of skin cancer was used as a drug carrier. 24-1 fractional factorial screening design was employed to study the effect of independent variables like the concentration of the polymeric solution, applied voltage (kV), distance (cm), flow rate (ml / hr) on dependent variables like % entrapment efficiency and fiber diameter. Results: Scanning electron microscopy was used to characterize fiber diameter and morphology. Results showed that the fiber diameter of all batches was found in the range of 100-200 nm. The optimized batch results showed the fiber diameter of 162.7 nm with uniform fibers. The tensile strength obtained was 190±37 Mpa. Further in vitro and ex vivo drug release profile suggested a controlled release mechanism for an extended period of 24 hr. The 5-fluorouracil loaded electrospun nanofibers were found to decrease cell viability up to ≥50% over 24 hr, with the number of cells dropping by ~ 10% over 48 hr. As the cell viability was affected by the release of 5-fluorouracil, we believe that electrospun nanofibers are a promising drug delivery system for the treatment of Basal Cell Carcinoma (BCC) skin cancer. Conclusion: These results demonstrate the possibility of delivering 5-Fluorouracil loaded electrospun nanofiber to skin with enhanced encapsulation efficiency indicating the effectiveness of the formulation for the treatment of basal cell carcinoma type of skin cancer.

scholarly journals Synthesis and In Vitro Antitumor Activity of Novel Bivalent β-Carboline-3-carboxylic Acid Derivatives with DNA as a Potential Target

2018 ◽  
Vol 19 (10) ◽  
pp. 3179 ◽  
Author(s):  
Hongling Gu ◽  
Na Li ◽  
Jiangkun Dai ◽  
Yaxi Xi ◽  
Shijun Wang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Cell Apoptosis ◽  
Docking Studies ◽  
In Vitro Cytotoxicity ◽  
Dependent Manner ◽  
Cycle Arrest ◽  
Dna Binding Affinity ◽  
Dose Dependent ◽  
Mcf 7

A series of novel bivalent β-carboline derivatives were designed and synthesized, and in vitro cytotoxicity, cell apoptosis, and DNA-binding affinity were evaluated. The cytotoxic results demonstrated that most bivalent β-carboline derivatives exhibited stronger cytotoxicity than the corresponding monomer against the five selected tumor cell lines (A549, SGC-7901, Hela, SMMC-7721, and MCF-7), indicating that the dimerization at the C3 position could enhance the antitumor activity of β-carbolines. Among the derivatives tested, 4B, 6i, 4D, and 6u displayed considerable cytotoxicity against A549 cell line. Furthermore, 4B, 6i, 4D, and 6u induced cell apoptosis in a dose-dependent manner, and caused cell cycle arrest at the S and G2/M phases. Moreover, the levels of cytochrome C in mitochondria, and the expressions of bcl-2 protein, decreased after treatment with β-carbolines, which indicated that 6i and 6u could induce mitochondria-mediated apoptosis. In addition, the results of UV-visible spectral, thermal denaturation, and molecular docking studies revealed that 4B, 6i, 4D, and 6u could bind to DNA mainly by intercalation.

scholarly journals Evaluation of phytochemical, antioxidant and cytotoxic potential of Sesbania grandiflora Linn.

2018 ◽  
Vol 7 (2) ◽  
pp. 191-198
Author(s):  
Shruti Gupta ◽  
◽  
Kishori G Apte ◽  
◽  
Keyword(s):  
Brine Shrimp ◽  
Reducing Power ◽  
In Vitro Cytotoxicity ◽  
Total Phenolic ◽  
Asian Countries ◽  
Leaf Extracts ◽  
Sesbania Grandiflora ◽  
Total Antioxidant ◽  
Potent Drug

Sesbania grandiflora Linn. is perennial branching, small erect quick-growing short-lived soft-wooded tree, mostly cultivated in southeast Asian countries including India and grows primarily in hot, humid environments. This study investigated on phytochemical values- total phenolic flavonoid, tannins and saponin contents for Sesbania grandiflora leaf extracts. The total antioxidant capacity, DPPH, reducing power, superoxide scavenging and Iron chelating effects were examined by established methods. In-vitro cytotoxicity by brine shrimp bioassay. Both the extracts of Sesbania grandiflora were found to possess moderate to high amounts of phytochemical contents. The total phenolic, flavonoid and saponin contents were found significantly higher in EQSG whereas tannins were more in AQSG. The EQSG and AQSG possessed low IC50 for H2O2 Scavenging (32.9, 27.3µg/ml), TAC (35.6, 41.8µg/ml) and moderate for DPPH (114.9, 113µg/ml) and reducing power (176.3, 181.6µg/ml) respectively. The Brine shrimp lethality bioassay showed a significantly high LC50 value with EQSG (10313µg/ml) and AQSG (12773µg/ml) compared to cyclophosphamide (110µg/ml) in cytotoxic assay. The results evidenced the potential of Sesbania grandiflora Linn. as potent drug with antioxidant and cytotoxic activity and could be useful for preparation of nutraceuticals for pharmaceutical use in the treatment of various human diseases and its complications

scholarly journals Perillaldehyde 1,2-epoxide Loaded SLN-Tailored mAb: Production, Physicochemical Characterization and In Vitro Cytotoxicity Profile in MCF-7 Cell Lines

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 161 ◽  
Author(s):  
Eliana B. Souto ◽  
Selma B. Souto ◽  
Aleksandra Zielinska ◽  
Alessandra Durazzo ◽  
Massimo Lucarini ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cetyltrimethylammonium Bromide ◽  
Physicochemical Characterization ◽  
Thiobarbituric Acid ◽  
In Vitro Cytotoxicity ◽  
Solid Lipid Nanoparticle ◽  
Mab Production ◽  
Epithelial Growth ◽  
Mcf 7

We have developed a new cationic solid lipid nanoparticle (SLN) formulation, composed of Compritol ATO 888, poloxamer 188 and cetyltrimethylammonium bromide (CTAB), to load perillaldehyde 1,2-epoxide, and surface-tailored with a monoclonal antibody for site-specific targeting of human epithelial growth receptor 2 (HER2). Perillaldehyde 1,2-epoxide-loaded cationic SLN (cPa-SLN), with a mean particle size (z-Ave) of 275.31 ± 4.78 nm and polydispersity index (PI) of 0.303 ± 0.081, were produced by high shear homogenization. An encapsulation efficiency of cPa-SLN above 80% was achieved. The release of perillaldehyde 1,2-epoxide from cationic SLN followed the Korsemeyer–Peppas kinetic model, which is typically seen in nanoparticle formulations. The lipid peroxidation of cPa-SLN was assessed by the capacity to produce thiobarbituric acid-reactive substances, while the antioxidant activity was determined by the capacity to scavenge the stable radical DPPH. The surface functionalization of cPa-SLN with the antibody was done via streptavidin-biotin interaction, monitoring z-Ave, PI and ZP of the obtained assembly (cPa-SLN-SAb), as well as its stability in phosphate buffer. The effect of plain cationic SLN (c-SLN, monoterpene free), cPa-SLN and cPa-SLN-SAb onto the MCF-7 cell lines was evaluated in a concentration range from 0.01 to 0.1 mg/mL, confirming that streptavidin adsorption onto cPa-SLN-SAb improved the cell viability in comparison to the cationic cPa-SLN.

New binuclear Ni(ii) metallates containing ONS chelators: synthesis, characterisation, DNA binding, DNA cleavage, protein binding, antioxidant activity, antimicrobial and in vitro cytotoxicity

2017 ◽  
Vol 41 (7) ◽  
pp. 2543-2560 ◽  
Author(s):  
G. Kalaiarasi ◽  
Ruchi Jain ◽  
H. Puschman ◽  
S. Poorna Chandrika ◽  
K. Preethi ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Dna Binding ◽  
Protein Binding ◽  
Hela Cell ◽  
Antiproliferative Activity ◽  
Dna Cleavage ◽  
In Vitro Cytotoxicity ◽  
Hela Cell Lines ◽  
Mcf 7

Four new binuclear nickel(ii) metallates showed promising antiproliferative activity against MCF-7 and HeLa cell lines and were much less toxic against HaCaT.

CYTOTOXIC ACTIVITY OF LUVUNGA SCANDENS AGAINST HUMAN CANCER CELL LINES

2016 ◽  
Vol 78 (10) ◽  
Author(s):  
Putri Nur Hidayah Al-Zikri ◽  
Muhammad Taher ◽  
Deny Susanti ◽  
Solachuddin Jauhari Arief Ichwan
Keyword(s):  
Cytotoxic Activity ◽  
Cell Line ◽  
Cell Lines ◽  
A549 Cell ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Breast Adenocarcinoma ◽  
Human Cancer Cell Lines ◽  
Mcf 7

Luvunga scandens belongs to the family of Rutaceae which usually inhabit tropical and moist environment. This plant is known as ‘Mengkurat Jakun’ among locals and used traditionally to treat fever and fatigue via decoction. The aim of this study was to investigate the cytotoxic activity of the leaves and stems extracts of L. scandens extract. Extracts of the leaves and stems were obtained from sequential extraction procedures by various organic solvents. All extracts were subjected to cytotoxic study by 3-(4, 5-dimethylthaizol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. In in vitro cytotoxicity assay, all L. scandens extracts exhibited cytotoxicity against human breast adenocarcinoma (MCF-7) and human lung adenocarcinoma (A549) cell lines. The IC50 values of dichloromethane and methanol extracts from the leaves of L. scandens against MCF-7 cell line were 62.5 µg/mL and 88.0 µg/mL, respectively, whereas IC50 of methanol extract from stem was 81.0 µg/mL. All extracts were less active against A549 cell line where IC50 value were not be determined. The present findings revealed the potential of L. scandens as a cytotoxic agent against MCF-7 cell line. However, further studies should be planned to evaluate role of the plant in cytotoxic activity.

scholarly journals Assessment of Intracellular Delivery Potential of Novel Sustainable Poly(δ-decalactone)-Based Micelles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 726
Author(s):  
Kuldeep Kumar Bansal ◽  
Ezgi Özliseli ◽  
Gaurav Kumar Saraogi ◽  
Jessica M. Rosenholm
Keyword(s):  
Drug Delivery ◽  
Folic Acid ◽  
Folate Receptor ◽  
In Vitro Cytotoxicity ◽  
Uptake Efficiency ◽  
Drug Delivery Carrier ◽  
Intracellular Drug Delivery ◽  
Copolymer Micelles ◽  
Model Drug

Biodegradable polymers from renewable resources have attracted much attention in recent years within the biomedical field. Lately, poly(δ-decalactone) based copolymer micelles have emerged as a potential drug delivery carrier material as a sustainable alternative to fossil-based polymers. However, their intracellular drug delivery potential is not yet investigated and therefore, in this work, we report on the synthesis and cellular uptake efficiency of poly(δ-decalactone) based micelles with or without a targeting ligand. Folic acid was chosen as a model targeting ligand and Rhodamine B as a fluorescent tracer to demonstrate the straightforward functionalisation aspect of copolymers. The synthesis of block copolymers was accomplished by a combination of facile ring-opening polymerisation and click chemistry to retain the structure uniformity. The presence of folic acid on the surface of micelles with diameter ~150 nm upsurge the uptake efficiency by 1.6 fold on folate receptor overexpressing MDA-MB-231 cells indicating the attainment of targeting using ligand functionality. The drug delivery capability of these carriers was ascertained by using docetaxel as a model drug, whereby the in vitro cytotoxicity of the drug was significantly increased after incorporation in micelles 48 h post incubation. We have also investigated the possible endocytosis route of non-targeted micelles and found that caveolae-mediated endocytosis was the preferred route of uptake. This work strengthens the prospect of using novel bio-based poly(δ-decalactone) micelles as efficient multifunctional drug delivery nanocarriers towards medical applications.

Paclitaxel-Loaded TPGS-b-PCL Nanoparticles: In Vitro Cytotoxicity and Cellular Uptake in MCF-7 and MDA-MB-231 Cells versus mPEG-b-PCL Nanoparticles and Abraxane®

2016 ◽  
Vol 16 (1) ◽  
pp. 160-170 ◽  
Author(s):  
Ezequiel Bernabeu ◽  
Lorena Gonzalez ◽  
Maria J. Legaspi ◽  
Marcela A. Moretton ◽  
Diego A. Chiappetta
Keyword(s):  
Cellular Uptake ◽  
In Vitro Cytotoxicity ◽  
Mcf 7

scholarly journals Freeze-Drying Ethylcellulose Microparticles Loaded with Etoposide for In Vitro Fast Dissolution and In Vitro Cytotoxicity against Cancer Cell Types, MCF-7 and Caco-2

2021 ◽  
Vol 11 (19) ◽  
pp. 9066
Author(s):  
Ahmed A. H. Abdellatif ◽  
Mashari A. Aldhafeeri ◽  
Waleed H. Alharbi ◽  
Fahad H. Alharbi ◽  
Waleed Almutiri ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Freeze Drying ◽  
Chemical Interaction ◽  
In Vitro Cytotoxicity ◽  
Dissolution Experiment ◽  
Freeze Dried ◽  
Fast Dissolution ◽  
Mcf 7

The aim of this study was to improve the solubility of etoposide–ethylcellulose (ET–ETO) microparticles using the freeze-drying technique. Ethylcellulose (EC) microparticles loaded with etoposide (ETO) were prepared with different drug–polymer molar ratios of 1:1, 1:3, 1:6, and 1:20 by the solvent evaporation method. The size of the prepared microparticles was 0.088 µm. The results showed that the amount of ETO encapsulated into the microparticles was 387.3, 365.0, 350.0, and 250 µg/50 mg microparticles for microparticles with drug–polymer ratios of 1:1, 1:3, 1:6, and 1:20, respectively. The FT-IR spectra showed no chemical interaction between ETO and the polymer in the solid state. The results obtained from the dissolution experiment showed that the freeze-dried microparticles were stable in 0.1 N HCl (gastric pH) for 2 h. At pH 7.4, the ETO release was 60 to 70% within the first 15 min and approximately 100% within 30 min. Results from the application of different dissolution models showed that the equations that best fit the dissolution data for the ET–ETO microparticles at pH 7.4 were the Higuchi and Peppas model equations. The in vitro cytotoxicity assay of free ETO and freeze-dried microspheres prepared in this study with a drug–polymer ratio of 1:1 was performed in two mammalian cancer cell lines, MCF-7 (for bone cancer of the mammary organ) and Caco-2 (for mammalian epithelial colorectal adenocarcinoma). The results showed that the half-maximal inhibitory concentrations (IC50 values) for ETO and freeze-dried ET–ETO microparticles were 18.6 µM and 27.1 µM, respectively. In conclusion, freeze-dried ET–ETO is a promising formulation for developing a fast-dissolving form of ETO with a significant antiproliferative activity against the tested cell lines used in this study. It is a promising formulation for local duodenal area targeting.

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