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. 2019 Jan;27(1):49-55.
doi: 10.1016/j.jsps.2018.07.018. Epub 2018 Jul 20.

Formulation and evaluation of docetaxel nanosuspensions: In-vitro evaluation and cytotoxicity

Mohamed A Ibrahim  1   2 , Gamal A Shazly  1   3 , Fadilah S Aleanizy  1 , Fulwah Y Alqahtani  1 , Gehan M Elosaily  4   5
Affiliations

Formulation and evaluation of docetaxel nanosuspensions: In-vitro evaluation and cytotoxicity

Mohamed A Ibrahim et al. Saudi Pharm J. 2019 Jan.

Abstract

Objective: The aim of the present study was to formulate the anticancer drug; docetaxel (DOX) as nanoparticles to enhance its biological activity.

Methodology: Solvent precipitation method was used to prepare DOX-loaded nanoparticles and was stabilized by different concentrations of hydroxypropyl methylcellulose (HPMC, E5) and sodium deoxycholate (SDC).

Results: The results showed that the particle size of the prepared DOX nanoparticles stabilized by SDC was small in comparison to those stabilized by the corresponding HPMC concentrations. The smallest particle size (83.97 nm) was obtained by using SDC as stabilizer at 5% level with zeta potential of -13.6 mV. It was concluded that increasing the stabilizer concentration resulted in increase in both initial and overall cumulative drug release. The release rate in case of nanoparticles stabilized by 5% SDC was 33% and 87% after 1 and 24 h respectively. The results showed that a significant reduction in the viability of FRO cells was observed at all tested time intervals in case of nanoparticles stabilized by 5% SDC at concentrations of 100 and 1000 μM/ml. In contrast, no signs of cytotoxicity was observed for nanoparticles stabilized by 5% HPMC at 10 and 100 μM/ml concentrations.

Keywords: Cytotoxicity; Docetaxel; In-vitro release; Nanoparticles; Stabilizers.

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Figures

Fig. 1
Fig. 1
Particle size analysis and zeta potential of DOX nanosuspension stabilized by 5% sodium deoxycholate.
Fig. 2
Fig. 2
XRPD spectra of DOX nanoparticles stabilized by 5% HPMC E5 compared to the individual components.
Fig. 3
Fig. 3
XRPD spectra of DOX nanoparticles stabilized by 5% SDC compared to the individual components.
Fig. 4
Fig. 4
In-vitro release profiles of DOX nanoparticles stabilized by different concentrations of HPMC E5.
Fig. 5
Fig. 5
In-vitro release profiles of DOX nanoparticles stabilized by different concentrations of sodium deoxycholate.
Fig. 6
Fig. 6
Cell viability percentage of FRO cells after incubation with different DOX nanoparticle formulations after 24, 48, and 72 h incubation with three concentrations of each formulation (10, 100, 1000 µM/ml) presented as mean ± SD.
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