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Gemcitabine hydrochloride-loaded functionalised carbon nanotubes as potential carriers for tumour targeting.

Das S, Desai JL, Thakkar HP - Indian J Pharm Sci (2013)

Bottom Line: Gemcitabine hydrochloride release from carbon nanotubes was found to follow Korsmeyer-Peppas kinetic model with non-Fickian diffusion pattern.Cytotoxic activity of formulation on A549 cells was found to be higher in comparison to free gemcitabine hydrochloride.Thus carbon nanotubes can be promising carrier for the anticancer drug gemcitabine hydrochloride.

View Article: PubMed Central - PubMed

Affiliation: Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Vadodara-390 001, India.

ABSTRACT
The objective of the present work was to formulate gemcitabine hydrochloride loaded functionalised carbon nanotubes to achieve tumour targeted drug release and thereby reducing gemcitabine hydrochloride toxicity. Multiwalled carbon nanotubes were functionalised using 1,2-distearoylphosphatidyl ethanolamine-methyl polyethylene glycol conjugate 2000. Optimised ratio 1:2 of carbon nanotubes:1,2-distearoylphosphatidyl ethanolamine-methyl polyethylene glycol conjugate 2000 was taken for loading of gemcitabine hydrochloride. The formulation was evaluated for different parameters. The results showed that maximum drug loading efficiency achieved was 41.59% with an average particle size of 188.7 nm and zeta potential of -10-1 mV. Scanning electron microscopy and transmission electron microscopy images confirmed the tubular structure of the formulation. The carbon nanotubes were able to release gemcitabine hydrochloride faster in acidic pH than at neutral pH indicating its potential for tumour targeting. Gemcitabine hydrochloride release from carbon nanotubes was found to follow Korsmeyer-Peppas kinetic model with non-Fickian diffusion pattern. Cytotoxic activity of formulation on A549 cells was found to be higher in comparison to free gemcitabine hydrochloride. Stability studies indicated that lyophilised samples of the formulation were more stable for 3 months under refrigerated condition than at room temperature. Thus carbon nanotubes can be promising carrier for the anticancer drug gemcitabine hydrochloride.

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Mentions: The cytotoxicity of GEM HCl-loaded in f-CNTs against A549 lung cancer cells were determined by using MTT dye reduction assay and was compared with that of plain GEM HCl. The results obtained are shown in fig. 6. There was no cytotoxic effect found in A549 cells treated with blank f-CNTs. With increasing concentrations, the percent cell viability was found to be decreasing. IC50 value of GEM HCl-loaded was found to be 10.4 μM and of GEM HCl loaded f-CNTs was found to be 9.1 μM. Although, GEM HCl-loaded f-CNTs exhibited a little more cytotoxicity as compared to free GEM HCl, there were no significant difference (P>0.05) between both at equal GEM HCl concentrations. Hence, the activity of GEM HCl was not adversely influenced during formulation step and cytotoxicity of main active component from GEM HCl loaded f-CNTs were GEM HCl. Moreover, no cytotoxicity found by f-CNTs at these concentrations suggests their safe biological applications at these concentrations[33].


Gemcitabine hydrochloride-loaded functionalised carbon nanotubes as potential carriers for tumour targeting.

Das S, Desai JL, Thakkar HP - Indian J Pharm Sci (2013)

© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3928735&req=5

Mentions: The cytotoxicity of GEM HCl-loaded in f-CNTs against A549 lung cancer cells were determined by using MTT dye reduction assay and was compared with that of plain GEM HCl. The results obtained are shown in fig. 6. There was no cytotoxic effect found in A549 cells treated with blank f-CNTs. With increasing concentrations, the percent cell viability was found to be decreasing. IC50 value of GEM HCl-loaded was found to be 10.4 μM and of GEM HCl loaded f-CNTs was found to be 9.1 μM. Although, GEM HCl-loaded f-CNTs exhibited a little more cytotoxicity as compared to free GEM HCl, there were no significant difference (P>0.05) between both at equal GEM HCl concentrations. Hence, the activity of GEM HCl was not adversely influenced during formulation step and cytotoxicity of main active component from GEM HCl loaded f-CNTs were GEM HCl. Moreover, no cytotoxicity found by f-CNTs at these concentrations suggests their safe biological applications at these concentrations[33].

Bottom Line: Gemcitabine hydrochloride release from carbon nanotubes was found to follow Korsmeyer-Peppas kinetic model with non-Fickian diffusion pattern.Cytotoxic activity of formulation on A549 cells was found to be higher in comparison to free gemcitabine hydrochloride.Thus carbon nanotubes can be promising carrier for the anticancer drug gemcitabine hydrochloride.

View Article: PubMed Central - PubMed

Affiliation: Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Vadodara-390 001, India.

ABSTRACT
The objective of the present work was to formulate gemcitabine hydrochloride loaded functionalised carbon nanotubes to achieve tumour targeted drug release and thereby reducing gemcitabine hydrochloride toxicity. Multiwalled carbon nanotubes were functionalised using 1,2-distearoylphosphatidyl ethanolamine-methyl polyethylene glycol conjugate 2000. Optimised ratio 1:2 of carbon nanotubes:1,2-distearoylphosphatidyl ethanolamine-methyl polyethylene glycol conjugate 2000 was taken for loading of gemcitabine hydrochloride. The formulation was evaluated for different parameters. The results showed that maximum drug loading efficiency achieved was 41.59% with an average particle size of 188.7 nm and zeta potential of -10-1 mV. Scanning electron microscopy and transmission electron microscopy images confirmed the tubular structure of the formulation. The carbon nanotubes were able to release gemcitabine hydrochloride faster in acidic pH than at neutral pH indicating its potential for tumour targeting. Gemcitabine hydrochloride release from carbon nanotubes was found to follow Korsmeyer-Peppas kinetic model with non-Fickian diffusion pattern. Cytotoxic activity of formulation on A549 cells was found to be higher in comparison to free gemcitabine hydrochloride. Stability studies indicated that lyophilised samples of the formulation were more stable for 3 months under refrigerated condition than at room temperature. Thus carbon nanotubes can be promising carrier for the anticancer drug gemcitabine hydrochloride.

No MeSH data available.


Related in: MedlinePlus