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. 2011:2011:587604.
doi: 10.1155/2011/587604. Epub 2011 Jun 7.

Poly(amidoamine)-Cholesterol Conjugate Nanoparticles Obtained by Electrospraying as Novel Tamoxifen Delivery System

Affiliations

Poly(amidoamine)-Cholesterol Conjugate Nanoparticles Obtained by Electrospraying as Novel Tamoxifen Delivery System

R Cavalli et al. J Drug Deliv. 2011.

Abstract

A new poly(amidoamine)-cholesterol (PAA-cholesterol) conjugate was synthesized, characterized and used to produce nanoparticles by the electrospraying technique. The electrospraying is a method of liquid atomization that consists in the dispersion of a solution into small charged droplets by an electric field. Tuning the electrospraying process parameters spherical PAA-chol nanoparticles formed. The PAA-cholesterol nanoparticles showed sizes lower than 500 nm and spherical shape. The drug incorporation capacity was investigated using tamoxifen, a lipophilic anticancer drug, as model drug. The incorporation of the tamoxifen did not affect the shape and sizes of nanoparticles showing a drug loading of 40%. Tamoxifen-loaded nanoparticles exhibited a higher dose-dependent cytotoxicity than free tamoxifen, while blank nanoparticles did not show any cytotoxic effect at the same concentrations. The electrospray technique might be proposed to produce tamoxifen-loaded PAA-chol nanoparticle in powder form without any excipient in a single step.

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Figures

Figure 1
Figure 1
Scheme of the apparatus for electrospraying.
Figure 2
Figure 2
Chemical structure of the PAA-cholesterol conjugate.
Figure 3
Figure 3
Surface tension of PAA-cholesterol conjugate in water.
Figure 4
Figure 4
SEM image of blank PAA-cholesterol nanoparticles.
Figure 5
Figure 5
Fluorescent PAA-cholesterol nanoparticles containing Rhodamine B (fluorescent microscopy).
Figure 6
Figure 6
Internalization of fluorescent PAA-cholesterol nanoparticles on Vero cells analysed by confocal laser scanning microscopy.
Figure 7
Figure 7
SEM image of In vitro release of the formulations.
Figure 8
Figure 8
Thermal analysis of tamoxifen and tamoxifen-loaded nanoparticles.
Figure 9
Figure 9
In vitro release of tamoxifen from the formulations.
Figure 10
Figure 10
Cell viability of MCF-7 breast cancer cells incubated for 24, 48, and 72 h (a, b, and c panels, resp.) with free tamoxifen (Tamoxifen), tamoxifen-loaded nanoparticles (tamoxifen-NP), empty nanoparticles (NP), or DMSO. Each bar represents the mean of three samples ± SD.

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