Vitamin E D‐alpha‐tocopheryl polyethylene glycol 1000 succinate‐conjugated liposomal docetaxel reverses multidrug resistance in breast cancer cells

2019 ◽  
Vol 71 (8) ◽  
pp. 1243-1254 ◽  
Author(s):  
Na Li ◽  
Tingting Fu ◽  
Wenling Fei ◽  
Tianyan Han ◽  
Xiangshuai Gu ◽  
...  
2020 ◽  
Vol 16 (7) ◽  
pp. 492-499
Author(s):  
Gamal A. Shazly ◽  
Gehan M. Elossai ◽  
Mohamed A. Ibrahim ◽  
Omar S. Aljohani ◽  
Usama A. Fahmy ◽  
...  

Author(s):  
Arehalli S. Manjappa ◽  
Popat S. Kumbhar ◽  
Rohini Kasabe ◽  
Sonali K. Diwate ◽  
John I. Disouza

Abstract Background Methotrexate (MTX), a folate anti-metabolite, has been used widely in the treatment of plenty of malignancies. However, the clinical use is limited because of its poor water solubility (BCS class II drug), nonspecific distribution, drug resistance, short circulation half-life, and toxicity. The objective of the present research was to synthesize the ester prodrug of MTX with d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) and characterize for in vitro anticancer efficacy. Results The FTIR and NMR results revealed the successful synthesis of the prodrug. The assay and saturation solubility of the prodrug is found to be 23 ± 2.5% and 6.7 ± 1.3 mg/mL (MTX equivalent) respectively. The CMC of the prodrug in distilled water at room temperature is found to be 36.9 ± 2.6 μg/mL. The prepared prodrug micelles showed a mean particle size of 166 ± 10 nm (PDI, 0.325 ± 0.09). Further, the TEM results confirmed the self-assembling character of the prodrug into micelles with a nearly spherical shape. The prodrug caused the significantly (p < 0.01) less hemolysis (16.8 ± 1.5%) when compared to plain MTX solution and significantly higher (p < 0.01) in vitro cytotoxicity, cell cycle arresting, and apoptosis against human breast cancer cells (MCF-7 and MDA-MB-231). Conclusion Our study results revealed the remarkable in vitro anticancer activity of MTX following its esterification with TPGS. However, further, in vivo studies are needed to prove its efficacy against different cancers.


2018 ◽  
Vol 15 (2) ◽  
pp. 227-234 ◽  
Author(s):  
Aliny Aparecida Lopes Ribeiro ◽  
Fabiana Helen da Silva ◽  
Aron Carlos de Melo Cotrim ◽  
Alessandra Lima Deluque ◽  
Patricia Gelli Feres de Marchi ◽  
...  

2018 ◽  
Vol 18 (8) ◽  
pp. 1138-1147 ◽  
Author(s):  
Esra Metin ◽  
Pelin Mutlu ◽  
Ufuk Gündüz

Background: Although conventional chemotherapy is the most common method for cancer treatment, it has several side effects such as neuropathy, alopecia and cardiotoxicity. Since the drugs are given to body systemically, normal cells are also affected, just like cancer cells. However, in recent years, targeted drug delivery has been developed to overcome these drawbacks. Objective: The aim of this study was targeted co-delivery of doxorubicin (Dox) which is an anticancer agent and D-α-Tocopherol polyethylene glycol 1000 succinate (vitamin E TPGS or simply TPGS) to breast cancer cells. For this purpose, Magnetic Nanoparticles (MNPs) were synthesized and coated with Oleic Acid (OA). Coated nanoparticles were encapsulated in Poly Lactic-co-Glycolic Acid (PLGA) and TPGS polymers and loaded with Dox. The Nanoparticles (NPs) were characterized by Fourier Transform Infrared (FTIR) spectroscopy, zetapotential analysis, Dynamic Light Scattering (DLS) analysis, Thermal Gravimetric Analysis (TGA) and Scanning Electron Microscope (SEM) analysis. Results: The results showed that NPs were spherical, superparamagnetic and in the desired range for use in drug targeting. The targetability of NPs was confirmed. Moreover, TPGS and Dox loading was shown by TGA and FTIR analyses. NPs were internalized by cells and the cytotoxic effect of drug loaded NPs on sensitive (MCF-7) and drug-resistant (MCF-7/Dox) cells were examined. It was seen that the presence of TPGS increased cytotoxicity significantly. TPGS also enhanced drug loading efficiency, release rate, cellular internalization. In MCF- 7/Dox cells, the drug resistance seems to be decreased when Dox is loaded onto TPGS containing NPs. Conclusion: This magnetic PLGA nanoparticle system is important for new generation targeted chemotherapy and could be used for breast cancer treatment after in vivo tests.


2008 ◽  
Vol 47 (6) ◽  
pp. 436-445 ◽  
Author(s):  
Pei Wang ◽  
Weiping Yu ◽  
Zhanzhi Hu ◽  
Li Jia ◽  
Vishwanath R. Iyer ◽  
...  

2000 ◽  
Vol 91 (1) ◽  
pp. 9-14 ◽  
Author(s):  
Tracy Heisler ◽  
Shirin Towfigh ◽  
Natalie Simon ◽  
David W. McFadden

2020 ◽  
Vol 7 ◽  
pp. 20-20
Author(s):  
Aparna Kalyanaraman ◽  
Dhanavathy Gnanasampanthapandian ◽  
Prasad Shanmughan ◽  
Puneet Kishore ◽  
Satish Ramalingam ◽  
...  

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