Enhanced in Vitro Anti-Tumor Activity of 5-Azacytidine by Entrapment into Solid Lipid Nanoparticles

Jahanfar, Farhad; Hasani, Akbar; Shanebandi, Dariush; Rahmati, Mohammad; Hamishehkar, Hamed

doi:10.15171/apb.2016.048

Cited by 4 publications

(2 citation statements)

References 46 publications

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“…The nuclear fragmentation and disintegration is a characteristic of apoptosis [42]. There are also several studies which have reported the use of DAPI as early indicator of apoptotic cell death [42][43][44][45]. We do not know the mechanism of action of FMSP-nanoparticles in eliciting cell death, the possibility of apoptotic pathways cannot be ruled.…”

Section: Discussionmentioning

confidence: 96%

Fluorescent magnetic submicronic polymer (FMSP) nanoparticles induce cell death in human colorectal carcinoma cells

Khan

Akhtar

Almohazey

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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Nanoparticles have many advantages such as high biocompatibility, bioavailability and effective therapeutic capabilities. The aim of the present study is to examine whether fluorescent magnetic submicronic polymer nanoparticles (FMSP-nanoparticles) have any impact on human colorectal cancer cells. In the present study, we have tested FMSP-nanoparticles with an average size of 100-200 nm on human colorectal carcinoma cells (HCT-116) to check their cytotoxic and anti-cancer capabilities. The effects of FMSP-nanoparticles on cancer cells were observed after 6 h, 24 h and 48 h intervals. The response of FMSP-nanoparticles-treated cells was evaluated by Trypan Blue, 4lue-diamidino-2-phenylindole (DAPI) and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays. Our MTT analysis results revealed that FMSP-nanoparticles produced dose-dependent effects on cancer cells, FMSP-nanoparticles with dose of 1.25 µg/mL did not decrease cell survivability, whereas dosages of 12.5 µg/mL and 50 µg/mL respectively showed 23.59% and 59.47% decrease in the cancer cell survivability. In conclusion, our results demonstrate FMSP-nanoparticles have a potential anti-cancer capability and hold a great promise for colon cancer treatments.

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Section: Discussionmentioning

confidence: 96%

Fluorescent magnetic submicronic polymer (FMSP) nanoparticles induce cell death in human colorectal carcinoma cells

Khan

Akhtar

Almohazey

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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“…The drug undergoes spontaneous hydrolysis in aqueous solutions, as well as rapid deamination by cytidine deaminase with subsequent degradation. Furthermore, chemical stability of 5-aza is temperature dependent, as the drug decomposition is faster at 37Cº than at 4Cº and 20 Cº indicating more rapid decomposition inside the incubator [31,32] .…”

Section: Discussionmentioning

confidence: 99%

Differentiation of bone marrow-derived mesenchymal stem cells into cardiomyocytes using different regimens of 5- azacytidine

Shkedif

ELsawy

Zoheir

et al. 2019

Egyptian Journal of Histology

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Background: Conventional therapeutic approaches for ischemic heart disease have limited benefit in preventing postischemic heart failure. Therefore, stem cell therapy emerges as a hopeful tool for treatment of ischemic heart disease following myocardial infarction. Aim: To standardize a protocol ensuring the best differentiation of bone marrow mesenchymal stem cells (BM-MSCs) into cardiomyocytes by using 5-azacytidine with minimum toxicity. Materials and Methods: BM-MSCs were isolated from the bone marrow of albino rats, characterized by flow cytometry and then divided into five groups: Group I: control group, group II: exposed to differentiating medium containing 10 μmol/L of 5-azacytidine for 24 h, group III: exposed to the differentiating medium for 72 h, group IV: the differentiating medium was renewed twice weekly, group V: daily renewal of the differentiating medium was done. The experiment was terminated after 3 weeks from the induction time. Morphological changes of the cultured cells were examined under a phase contrast microscope. The effect of different duration of 5-aza exposure on BM-MSCs viability was evaluated by cell counting Kit 8 assay. Expression of cardiac troponin I and connexin 43 was measured using Quantitative reverse transcription-PCR. Transmission electron microscope was used to observe ultrastructural features of the induced cells. Morphometric study for comparing the length of the formed myofilaments in the four treated groups was done. Results: The obtained results from groups II and III showed initial limited signs of differentiation towards cardiac lineage. Groups IV and V showed optimal signs of differentiation with better results regarding group V, yet, this was at the expense of the viability of the cultured cells. Conclusion:The use of 5-aza showed a valuable differentiating effect on MSCs towards cardiomyocytes. Prolonged use resulted in promotion of the differentiation. Yet, it was at the expense of the viability of these cells.

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Multifunctional 99mTc-5-azacitidine Gold Nanoparticles: Formulation, In Vitro Cytotoxicity, Radiosynthesis, and In Vivo Pharmacokinetic Study

Eldin

Rashed

Hassan

et al. 2023

CDD

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Background: 5-azacitidine is a very potent chemotherapeutic agent that suffers from certain limitation. Objective: This study aims to prepare gold nanoparticles as a new nano-formula of 5-azacitidine that can improve its bioavailability and decrease its side effects. Methods: 5-azacytidine loaded GA-AuNPs were prepared and characterized by UV-Vis spectroscopy, infrared (IR) and transmission electronic microscope (TEM). This new platform was characterized in vitro by measuring its zeta potential, particle size, drug loading efficacy and its anti-proliferative effect on MCF-7 cell line was evaluated. In vivo biodistribution studies of 99mTc-5-aza solution and 99mTc-5-aza-gold nano formula were conducted in tumor bearing mice by different routes of administration (Intravenous and Intra-tumor). Results: 5-Aza-GA-AuNPs formula was successfully prepared with optimum particle size of ≈34.66 nm, zeta potential of -14.4 mV and high entrapment efficiency. 99mTc-5-Aza-GA-AuNPs was efficient radiosynthesized (95.4%). Biodistribution studies showed high selective accumulation in tumor and low uptake in non-target organs in case of 5-Aza-GA-AuNPs formula than 99mTc-5-azacitidine solution. Conclusion: 99mTc-5-Aza-GA-AuNPs had succeeded to improve the selectivity and uptake of 5-azacitidine in cancer. Moreover, 99mTc-5-Aza-GA-AuNPs could be used as a hopeful theranostic radiopharmaceutical preparation for cancer.

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Enhanced in Vitro Anti-Tumor Activity of 5-Azacytidine by Entrapment into Solid Lipid Nanoparticles

Cited by 4 publications

References 46 publications

Fluorescent magnetic submicronic polymer (FMSP) nanoparticles induce cell death in human colorectal carcinoma cells

Fluorescent magnetic submicronic polymer (FMSP) nanoparticles induce cell death in human colorectal carcinoma cells

Differentiation of bone marrow-derived mesenchymal stem cells into cardiomyocytes using different regimens of 5- azacytidine

Multifunctional 99mTc-5-azacitidine Gold Nanoparticles: Formulation, In Vitro Cytotoxicity, Radiosynthesis, and In Vivo Pharmacokinetic Study

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