Improved cellular uptake, enhanced efficacy and promising pharmacokinetic profile of docetaxel employing glycine-tethered C60-fullerenes

Misra, Charu; Thotakura, Nagarani; Kumar, Rajendra; Singh, Bhupinder; Sharma, Gajanand; Katare, Om Prakash; Raza, Kaisar

doi:10.1016/j.msec.2017.03.073

Cited by 31 publications

(12 citation statements)

References 31 publications

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“…The results of drug loading and conjugation efficiency proved that there was significant capacity of drug loading onto water soluble fullerenols. Such drug payload carrying capability of the nanocarriers is a desired attribute in chemotherapy so as to deliver the desired dose in a sustained manner [21]. As fullerenols and its derivatives are known to possess diameter of %1 nm, hence, molecular depiction is not possible from FE-SEM or TEM.…”

Section: Discussionmentioning

confidence: 99%

“…Reaction was continuously monitored for unreacted DTX using thin layer chromatography. Final conjugate (C 60 -OH-APA-DTX) was collected and washed with THF to remove the unconjugated drug [21].…”

Section: Conjugation Of Dtx With C 60 -Oh-apamentioning

confidence: 99%

“…In this study, the powder sample was mounted on the sample holder and scanned at a wavelength of 1.54 A , using copper Ka, as the X-ray source. X-rays were irradiated at angles ranging from 5 to 60 [21].…”

Section: Powdered X-ray Diffraction (Xrd)mentioning

confidence: 99%

“…In recent past, researchers have made various efforts to deliver anti-cancer drugs like 5-fluro uracil, cyclophosphamide, doxorubicin, paclitaxel and docetaxel by means of C 60 fullerene and derivatives, however, there are no reports of delivering DTX by means of fullerenols. Though, numerous nanotechnology-based attempts other than fullerenols have been made to deliver DTX [20][21][22]. Henceforth, it was envisioned to explore the potential of fullerenols in the delivery of DTX and the influence of this conjugation on the pharmacokinetic profile of the drug.…”

mentioning

confidence: 99%

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Aspartic acid derivatized hydroxylated fullerenes as drug delivery vehicles for docetaxel: an explorative study

Thotakura

Sharma

Singh

et al. 2017

Artificial Cells, Nanomedicine, and Biotechnology

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The objective of the present study was to deliver docetaxel to cancerous cells with enhanced efficacy and safety profile, using aspartic acid linked fullerenols. This aspartic acid derivatized fullerenol conjugate linked with docetaxel was characterized by UV, FT-IR and NMR spectroscopy. Studies for particle size, PDI, zeta potential and FE-SEM were also performed. The conjugate was evaluated for release kinetics, cancer cell cytotoxicity, cellular uptake using confocal laser microscopy and also for pharmacokinetic profile. Cytotoxic studies proved that there was almost 4.3 folds decrease in IC with significantly enhanced cellular uptake of the nanometric conjugates. It was observed that the bioavailability was enhanced by 5.8 folds when compared to that of pure DTX. The developed nanoconstructs were erythrocyte compatible and offered decreased protein binding. The findings are encouraging and offer a novel carrier with enhanced efficacy and safety of a drug, belonging to BCS class IV.

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Section: Discussionmentioning

confidence: 99%

Section: Conjugation Of Dtx With C 60 -Oh-apamentioning

confidence: 99%

Section: Powdered X-ray Diffraction (Xrd)mentioning

confidence: 99%

mentioning

confidence: 99%

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Aspartic acid derivatized hydroxylated fullerenes as drug delivery vehicles for docetaxel: an explorative study

Thotakura

Sharma

Singh

et al. 2017

Artificial Cells, Nanomedicine, and Biotechnology

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“…Taking into consideration that similar effects of C 60 fullerene were already observed by us for C 60 + Dox and C 60 + Cis nanocomplexes, one may conclude that enhancement of drug uptake into tumor cells is the unique feature of C 60 fullerene, which may be of high importance for further pre-clinical trials of the C 60 fullerene-drug nanocomplexes. 25,41 The peculiarity of the biological effect of the watersoluble C 60 fullerenes is their ability to selectively damage of the tumor cells, whereas they do not affect the normal cells. 23,46 On the other hand, C 60 fullerene, as a carrier of antitumor drug, thanks to its powerful antioxidant properties, 5,51 effectively reduces the side (toxic) effects of drug relative to the normal cells.…”

Section: Materials Characterizationmentioning

confidence: 99%

A Novel Nanoconjugate of Landomycin A with C60 Fullerene for Cancer Targeted Therapy: In Vitro Studies

et al. 2018

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Introduction-Landomycins are a subgroup of angucycline antibiotics that are produced by Streptomyces bacteria and possess strong antineoplastic potential. Literature data suggest that enhancement of the therapeutic activity of this drug may be achieved by means of creating specific drug delivery systems. Here we propose to adopt C 60 fullerene as flexible and stable nanocarrier for landomycin delivery into tumor cells. Methods-The methods of molecular modelling, dynamic light scattering and Fourier transform infrared spectroscopy were used to study the assembly of C 60 fullerene and the anticancer drug Landomycin A (LA) in aqueous solution. Cytotoxic activity of this nanocomplex was studied in vitro towards two cancer cell lines in comparison to human mesenchymal stem cells (hMSCs) using 3-(4,5-dimethyl-2thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) test and a live/dead assay. The morphology of the cells incubated with fullerene-drug nanoparticles and their uptake into target cells were studied by scanning electron microscopy and fluorescence light microscopy. Results-The viability of primary cells (hMSCs, as a model for healthy cells) and cancer cell lines (human osteosarcoma cells, MG-63, and mouse mammary cells, 4T1, as models for cancer cells) was studied after incubation with water-soluble C 60 fullerenes, LA and the mixture C 60 + LA. The C 60 + LA nanocomplex in contrast to LA alone showed higher toxicity towards cancer cells and lower toxicity towards normal cells, whereas the water-soluble C 60 fullerenes at the same concentration were not toxic for the cells. Conclusions-The obtained physico-chemical data indicate a complexation between the two compounds, leading to the formation of a C 60 + LA nanocomposite. It was concluded that immobilization of LA on C 60 fullerene enhances selectivity of action of this anticancer drug in vitro, indicating on possibility of further preclinical studies of novel C 60 + LA nanocomposites on animal tumor models.

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Biomedical Application of Nanocomposites Based on Fullerenes-C60

Bratovčić

2023

Lecture Notes in Networks and Systems

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Improved cellular uptake, enhanced efficacy and promising pharmacokinetic profile of docetaxel employing glycine-tethered C60-fullerenes

Cited by 31 publications

References 31 publications

Aspartic acid derivatized hydroxylated fullerenes as drug delivery vehicles for docetaxel: an explorative study

Aspartic acid derivatized hydroxylated fullerenes as drug delivery vehicles for docetaxel: an explorative study

A Novel Nanoconjugate of Landomycin A with C60 Fullerene for Cancer Targeted Therapy: In Vitro Studies

Biomedical Application of Nanocomposites Based on Fullerenes-C60

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