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Polyanionic carbohydrate doxorubicin-dextran nanocomplex as a delivery system for anticancer drugs: in vitro analysis and evaluations.

Yousefpour P, Atyabi F, Farahani EV, Sakhtianchi R, Dinarvand R - Int J Nanomedicine (2011)

Bottom Line: Thermal analysis of DOX-DS complexation by ITC revealed that each DOX molecule binds with 3 DS glycosyl monomers.Drug release profile of nanocomplexes showed a fast DOX release followed by a slow sustained release, leading to release of 32% of entrapped DOX within 15 days.DOX-DS nanocomplexes may serve as a drug delivery system with efficient drug encapsulation and also may be taken into consideration in designing DOX controlled-release systems.

View Article: PubMed Central - PubMed

Affiliation: Nanotechnology Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

ABSTRACT
This study deals with the preparation and investigation of a nanoscale delivery system for the anticancer drug doxorubicin (DOX) using its complexation with polyanionic carbohydrate dextran sulfate (DS). Dynamic light scattering, SEM, and zeta potential determination were used to characterize nanocomplexes. DOX-DS complexation was studied in the presence of ethanol as a hydrogen-bond disrupting agent, NaCl as an electrostatic shielding agent, and chitosan as a positively charged polymer. Thermodynamics of DOX-DS interaction was studied using isothermal titration calorimetry (ITC). A dialysis method was applied to investigate the release profile of DOX from DOX-DS nanocomplexes. Spherical and smooth-surfaced DOX-DS nanocomplexes (250-500 nm) with negative zeta potential were formed at a DS/DOX (w/w) ratio of 0.4-0.6, with over 90% drug encapsulation efficiency. DOX when complexed with DS showed lower fluorescence emission and 480 nm absorbance plus a 15 nm bathometric shift in its visible absorbance spectrum. Electrostatic hydrogen bonding and π-π stacking interactions are the main contributing interactions in DOX-DS complexation. Thermal analysis of DOX-DS complexation by ITC revealed that each DOX molecule binds with 3 DS glycosyl monomers. Drug release profile of nanocomplexes showed a fast DOX release followed by a slow sustained release, leading to release of 32% of entrapped DOX within 15 days. DOX-DS nanocomplexes may serve as a drug delivery system with efficient drug encapsulation and also may be taken into consideration in designing DOX controlled-release systems.

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A) In vitro cumulative release and B) in vitro release rate of doxorubicin (DOX) from doxorubicin–dextran sulfate (DOX-DS) nanocomplexes (DOX: 60 μg/mL, DS/DOX [w/w]: 0.6) (n = 3). C) In vitro release of free DOX in phosphate buffer solution (pH 7.4), 37°C.
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f5-ijn-6-1487: A) In vitro cumulative release and B) in vitro release rate of doxorubicin (DOX) from doxorubicin–dextran sulfate (DOX-DS) nanocomplexes (DOX: 60 μg/mL, DS/DOX [w/w]: 0.6) (n = 3). C) In vitro release of free DOX in phosphate buffer solution (pH 7.4), 37°C.

Mentions: A dialysis method was applied to investigate the release profile of DOX from DOX-DS nanocomplexes. Figure 5A shows that 14% of DOX was released during the first 24 hours followed by slow release of 32% over a time span of 15 days. Figure 5B presents a clearer view of release behavior of DOX-DS nanocomplexes. Furthermore, a controlled release study of free DOX revealed complete diffusion of drug through dialysis membrane within 10 hours (Figure 5C).


Polyanionic carbohydrate doxorubicin-dextran nanocomplex as a delivery system for anticancer drugs: in vitro analysis and evaluations.

Yousefpour P, Atyabi F, Farahani EV, Sakhtianchi R, Dinarvand R - Int J Nanomedicine (2011)

A) In vitro cumulative release and B) in vitro release rate of doxorubicin (DOX) from doxorubicin–dextran sulfate (DOX-DS) nanocomplexes (DOX: 60 μg/mL, DS/DOX [w/w]: 0.6) (n = 3). C) In vitro release of free DOX in phosphate buffer solution (pH 7.4), 37°C.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3141874&req=5

f5-ijn-6-1487: A) In vitro cumulative release and B) in vitro release rate of doxorubicin (DOX) from doxorubicin–dextran sulfate (DOX-DS) nanocomplexes (DOX: 60 μg/mL, DS/DOX [w/w]: 0.6) (n = 3). C) In vitro release of free DOX in phosphate buffer solution (pH 7.4), 37°C.
Mentions: A dialysis method was applied to investigate the release profile of DOX from DOX-DS nanocomplexes. Figure 5A shows that 14% of DOX was released during the first 24 hours followed by slow release of 32% over a time span of 15 days. Figure 5B presents a clearer view of release behavior of DOX-DS nanocomplexes. Furthermore, a controlled release study of free DOX revealed complete diffusion of drug through dialysis membrane within 10 hours (Figure 5C).

Bottom Line: Thermal analysis of DOX-DS complexation by ITC revealed that each DOX molecule binds with 3 DS glycosyl monomers.Drug release profile of nanocomplexes showed a fast DOX release followed by a slow sustained release, leading to release of 32% of entrapped DOX within 15 days.DOX-DS nanocomplexes may serve as a drug delivery system with efficient drug encapsulation and also may be taken into consideration in designing DOX controlled-release systems.

View Article: PubMed Central - PubMed

Affiliation: Nanotechnology Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

ABSTRACT
This study deals with the preparation and investigation of a nanoscale delivery system for the anticancer drug doxorubicin (DOX) using its complexation with polyanionic carbohydrate dextran sulfate (DS). Dynamic light scattering, SEM, and zeta potential determination were used to characterize nanocomplexes. DOX-DS complexation was studied in the presence of ethanol as a hydrogen-bond disrupting agent, NaCl as an electrostatic shielding agent, and chitosan as a positively charged polymer. Thermodynamics of DOX-DS interaction was studied using isothermal titration calorimetry (ITC). A dialysis method was applied to investigate the release profile of DOX from DOX-DS nanocomplexes. Spherical and smooth-surfaced DOX-DS nanocomplexes (250-500 nm) with negative zeta potential were formed at a DS/DOX (w/w) ratio of 0.4-0.6, with over 90% drug encapsulation efficiency. DOX when complexed with DS showed lower fluorescence emission and 480 nm absorbance plus a 15 nm bathometric shift in its visible absorbance spectrum. Electrostatic hydrogen bonding and π-π stacking interactions are the main contributing interactions in DOX-DS complexation. Thermal analysis of DOX-DS complexation by ITC revealed that each DOX molecule binds with 3 DS glycosyl monomers. Drug release profile of nanocomplexes showed a fast DOX release followed by a slow sustained release, leading to release of 32% of entrapped DOX within 15 days. DOX-DS nanocomplexes may serve as a drug delivery system with efficient drug encapsulation and also may be taken into consideration in designing DOX controlled-release systems.

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