scholarly journals Delivery of the Radionuclide 131I Using Cationic Fusogenic Liposomes as Nanocarriers

2021 ◽  
Vol 22 (1) ◽  
pp. 457
Author(s):  
Rejhana Kolašinac ◽  
Dirk Bier ◽  
Laura Schmitt ◽  
Andriy Yabluchanskiy ◽  
Bernd Neumaier ◽  
...  
Keyword(s):  
Membrane Fusion ◽  
Cellular Uptake ◽  
Cancer Cell Line ◽  
Drug Carriers ◽  
Cargo Delivery ◽  
Human Blood Cells ◽  
Fusion Ability ◽  
Potential Use

Liposomes are highly biocompatible and versatile drug carriers with an increasing number of applications in the field of nuclear medicine and diagnostics. So far, only negatively charged liposomes with intercalated radiometals, e.g., 64Cu, 99mTc, have been reported. However, the process of cellular uptake of liposomes by endocytosis is rather slow. Cellular uptake can be accelerated by recently developed cationic liposomes, which exhibit extraordinarily high membrane fusion ability. The aim of the present study was the development of the formulation and the characterization of such cationic fusogenic liposomes with intercalated radioactive [131I]I− for potential use in therapeutic applications. The epithelial human breast cancer cell line MDA-MB-231 was used as a model for invasive cancer cells and cellular uptake of [131I]I− was monitored in vitro. Delivery efficiencies of cationic and neutral liposomes were compared with uptake of free iodide. The best cargo delivery efficiency (~10%) was achieved using cationic fusogenic liposomes due to their special delivery pathway of membrane fusion. Additionally, human blood cells were also incubated with cationic control liposomes and free [131I]I−. In these cases, iodide delivery efficiencies remained below 3%.

scholarly journals In vitro cytotoxicity of Aspilia pluriseta Schweinf. extract fractions

2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Sospeter N. Njeru ◽  
Jackson M. Muema
Keyword(s):  
Biological Activities ◽  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Root Extract ◽  
Lack Of Information ◽  
Information Gap ◽  
Diphenyltetrazolium Bromide ◽  
Potential Use

Abstract Objectives We and others have shown that Aspilia pluriseta is associated with various biological activities. However, there is a lack of information on its cytotoxicity. This has created an information gap about the safety of A. pluriseta extracts. As an extension to our recent publication on the antimicrobial activity and the phytochemical characterization of A. pluriseta root extracts, here we report on cytotoxicity of tested solvent fractions. We evaluated the potential cytotoxicity of these root extract fractions on Vero cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results We show that all solvent extract fractions (except methanolic solvent fractions) had cytotoxic concentration values that killed 50% of the Vero cells (CC50) greater than 20 µg/mL and selectivity index (SI) greater than 1.0. Taken together, we demonstrate that, A. pluriseta extract fractions’ earlier reported bioactivities are within the acceptable cytotoxicity and selective index limits. This finding scientifically validates the potential use of A. pluriseta in the discovery of safe therapeutics agents.

Characterization of in vitro migratory properties of anti-CD19 chimeric receptor-redirected CIK cells for their potential use in B-ALL immunotherapy

2006 ◽  
Vol 34 (9) ◽  
pp. 1218-1228 ◽  
Author(s):  
Virna Marin ◽  
Erica Dander ◽  
Ettore Biagi ◽  
Martino Introna ◽  
Grazia Fazio ◽  
...  
Keyword(s):  
Chimeric Receptor ◽  
Cik Cells ◽  
Potential Use

scholarly journals Development and Characterization of Nanoliposomal Hydroxyurea Against BT-474 Breast Cancer Cells

2019 ◽  
Vol 10 (1) ◽  
pp. 39-45 ◽  
Author(s):  
Azam Akbari ◽  
Azim Akbarzadeh ◽  
Morteza Rafiee Tehrani ◽  
Reza Ahangari Cohan ◽  
Mohsen Chiani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Drug Release ◽  
Zeta Potential ◽  
Cancer Cells ◽  
Cellular Uptake ◽  
Breast Cancer Cells ◽  
Drug Carriers ◽  
Diffusion Method ◽  
Diphenyl Tetrazolium Bromide

Purpose: Hydroxyurea (HU) is a well-known chemotherapy drug with several side effects which limit its clinical application. This study was conducted to improve its therapeutic efficiency against breast cancer using liposomes as FDA-approved drug carriers. Methods: PEGylated nanoliposomes-containing HU (NL-HU) were made via a thin-film hydration method, and assessed in terms of zeta potential, size, morphology, release, stability, cellular uptake, and cytotoxicity. The particle size and zeta potential of NL-HU were specified by zeta-sizer. The drug release from liposomes was assessed by dialysis diffusion method. Cellular uptake was evaluated by flow cytometry. The cytotoxicity was designated by methyl thiazolyl diphenyl-tetrazolium bromide (MTT) test. Results: The size and zeta value of NL-HU were gotten as 85 nm and -27 mV, respectively. NL-HU were spherical.NL-HU vesicles were detected to be stable for two months. The slow drug release and Weibull kinetic model were obtained. Liposomes considerably enhanced the uptake of HU into BT-474 human breast cancer cells. The cytotoxicity of NL-HU on BT-474 cells was found to be significantly more than that of free HU. Conclusion: The results confirmed these PEGylated nanoliposomes containing drug are potentially suitable against in vitro model of breast cancer.

scholarly journals Green Strategy to Develop Novel Drug-Containing Poly (ε-Caprolactone)-Chitosan-Silica Xerogel Hybrid Fibers for Biomedical Applications

2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Hua-Jian Zhou ◽  
Shu-Hua Teng ◽  
Yi-Bo Zhou ◽  
Hai-Sheng Qian
Keyword(s):  
Biomedical Applications ◽  
Average Diameter ◽  
Drug Carriers ◽  
Silica Xerogel ◽  
Hybrid Fibers ◽  
Green Strategy ◽  
Novel Drug ◽  
Potential Use ◽  
Thermal Stability Of

A facile and green method was explored to prepare the tetracycline hydrochloride- (TCH-) loaded poly (ε-caprolactone)-chitosan-silica xerogel (PCL-CS-SiO2) hybrid fibers by using 90% acetic acid as a suitable solvent. The SEM results showed that those fibers exhibited a continuous, bead-free morphology, an average diameter of about 430 nm, and super-hydrophilicity ( θ water ≈ 0 ° ). The presence of SiO2 was found to enhance the thermal stability of the hybrid fibers, and the actual content of SiO2 was obtained by the TG measurement. Moreover, SiO2 xerogel as an important bioceramic endowed the hybrid fibers with good drug release behavior and in vitro bioactivity, suggesting their potential use as novel drug carriers for bone tissue engineering. The present work is expected to offer a green strategy to develop novel, multifunctional hybrid materials.

scholarly journals Preclinical evaluation of new α-radionuclide therapy targeting LAT1: 2-[211At]astato-α-methyl-L-phenylalanine in tumor-bearing model

2020 ◽  
Author(s):  
Yasuhiro OHSHIMA ◽  
Hiroyuki Suzuki ◽  
Hirofumi Hanaoka ◽  
Ichiro Sasaki ◽  
Shigeki Watanabe ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Radionuclide Therapy ◽  
Cancer Cell Line ◽  
Strand Break ◽  
The Body ◽  
Cellular Growth ◽  
Dna Double Strand Break ◽  
Amino Acid Analog

Abstract PURPOSE: Targeted α-radionuclide therapy has growing attention as a promising therapy for refractory cancers. However, the application is limited to certain types of cancer. Since L-type amino acids transporter 1 (LAT1) is highly expressed in various human cancers, we prepared LAT1-selective α-emitting amino acid analog, 2-[211At]astato-α-methyl-L-phenylalanine ([211At]-2-AAMP), and evaluated its potential as a therapeutic agent. METHODS: [211At]-2-AAMP was prepared from the stannyl precursor. Stability of [211At]-2-AAMP was evaluated by both in vitro and in vivo. In vitro studies using LAT1 expressing human ovary cancer cell line, SKOV3, were performed for evaluating cellular uptake and cytotoxicity of [211At]-2-AAMP. Biodistribution and therapeutic studies in SKOV3 bearing mice were performed after intravenous injection of [211At]-2-AAMP. RESULTS: [211At]-2-AAMP was stable in murine plasma in vitro and excreted into urine as intact. Cellular uptake of [211At]-2-AAMP was inhibited by treatment with LAT1-selective inhibitor. After 24 hours of incubation, [211At]-2-AAMP suppressed clonogenic growth at 10 kBq/ml, and induced cell death and DNA double strand break at 25 kBq/ml. When injected to mice, [211At]-2-AAMP exhibited the peak accumulation in the tumor at 30 min postinjection, and the radioactivity levels in the tumor retained up to 60 min. The majority of the radioactivity was rapidly eliminated from the body into the urine as an intact form immediately after injection. [211At]-2-AAMP significantly improved the survival of mice (P<0.05) without serious side effects. CONCLUSION: [211At]-2-AAMP showed α-radiation-dependent cellular growth inhibition after taking up via LAT1. Furthermore, [211At]-2-AAMP provided a beneficial effect on survival in vivo. These findings suggest that [211At]-2-AAMP might be useful for treatment of LAT1-positive cancer.

Preparation and In Vitro Cellular Uptake Assessment of Multifunctional Rubik-Like Magnetic Nano-Assemblies

2019 ◽  
Vol 19 (6) ◽  
pp. 3301-3309
Author(s):  
Xiawen Zheng ◽  
Yuejian Chen ◽  
Zhiming Wang ◽  
Lina Song ◽  
Yu Zhang ◽  
...  
Keyword(s):  
Oleic Acid ◽  
Folic Acid ◽  
Cellular Uptake ◽  
Hela Cells ◽  
Drug Loading ◽  
Superparamagnetic Iron Oxide ◽  
Drug Carriers ◽  
High Drug ◽  
High Drug Loading

Through self-assembly of nanoparticles into high-order and stable structures of cubic clusters, high drug-loading rubik-like magnetic nano-assemblies (MNAs), possessing folic acid targeting and strong magnetism-enhanced cellular uptake capabilities, were built. In this study, the core of the cubic drug assemblies consisted of four monodisperse superparamagnetic iron oxide nanoparticles coated with layers of oleic acid (Fe3O4@OA), simultaneously encapsulating fluorescein, and Paclitaxol (Flu-MNAs and PTX-MNAs) for imaging and therapeutic applications. To enable preferential tumor cellular uptake by the nanocarriers, the outermost layer of Fe3O4 was functionalized with the new dual-oleic acid-polyethylene glycol-folic acid polymer (FA-PEG-Lys-OA2) as a “shell.” The drug carriers exhibited excellent stability and biocompatibility, and showed high drug loading and excellent magnetic response In Vitro. Furthermore, preliminary evaluations of the drug carriers with Hela cells showed effective cellular targeting capability. In addition, the cubic assemblies enhanced anticancer efficiency for Hela cells compared to bare drugs. Especially, the applied external magnetic field further improved the uptake of the vectors, and thereby enhanced the inhibitory effect. In brief, all these results suggested that cubic assemblies could serve as potential strategies for targeted anticancer therapies.

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