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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.

No MeSH data available.


Related in: MedlinePlus

Drug content in stability study of functionalized carbon nanotubes.Stability study of optimised batch of GEM HCl-loaded functionalised carbon nanotubes as per % drug retention at room temperature (□) and at refrigerated condition (▥).
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Figure 7: Drug content in stability study of functionalized carbon nanotubes.Stability study of optimised batch of GEM HCl-loaded functionalised carbon nanotubes as per % drug retention at room temperature (□) and at refrigerated condition (▥).

Mentions: Lyophilisation of formulation helps in keeping the product stable during long-term storage. This can be achieved by using cryoprotectant such as trehalose, sucrose, mannitol and dextrose. Therefore for stability studies, the formulation was lyophilised using sucrose as cryoprotectant, which is widely used in industry because of its easy availability and low cost. The results in terms of percent drug retained and particle size are shown graphically in figs. 7 and 8, respectively. There were no changes in physical properties of f-CNTs. At the end of 3 months, the particle size and percent drug retained of lyophilised formulation kept at room temperature were found to be 241 nm and 87.66%, respectively, while it was found to be 210 nm and 96.72%, respectively for sample kept as 5±3°. It indicated that the particle size of the rehydrated lyophilised GEM HCl-loaded f-CNTs was not altered significantly and also no significant reduction in the percent drug retained after rehydration of lyophilised f-CNTs when stored at 5±3° temperature, as compared with 30±2°/ 60±5% RH over a period of 3 months. Hence after lyophilisation storage at 5±3° provides the better stability to the f-CNTs.


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

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

Drug content in stability study of functionalized carbon nanotubes.Stability study of optimised batch of GEM HCl-loaded functionalised carbon nanotubes as per % drug retention at room temperature (□) and at refrigerated condition (▥).
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 7: Drug content in stability study of functionalized carbon nanotubes.Stability study of optimised batch of GEM HCl-loaded functionalised carbon nanotubes as per % drug retention at room temperature (□) and at refrigerated condition (▥).
Mentions: Lyophilisation of formulation helps in keeping the product stable during long-term storage. This can be achieved by using cryoprotectant such as trehalose, sucrose, mannitol and dextrose. Therefore for stability studies, the formulation was lyophilised using sucrose as cryoprotectant, which is widely used in industry because of its easy availability and low cost. The results in terms of percent drug retained and particle size are shown graphically in figs. 7 and 8, respectively. There were no changes in physical properties of f-CNTs. At the end of 3 months, the particle size and percent drug retained of lyophilised formulation kept at room temperature were found to be 241 nm and 87.66%, respectively, while it was found to be 210 nm and 96.72%, respectively for sample kept as 5±3°. It indicated that the particle size of the rehydrated lyophilised GEM HCl-loaded f-CNTs was not altered significantly and also no significant reduction in the percent drug retained after rehydration of lyophilised f-CNTs when stored at 5±3° temperature, as compared with 30±2°/ 60±5% RH over a period of 3 months. Hence after lyophilisation storage at 5±3° provides the better stability to the f-CNTs.

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