Elham Bagheri Eskolaky1,
Mehdi Ardjmand2,
Azim Akbarzadeh3
1Department of Applied Chemistry, Faculty of Pharmaceutical Chemistry, Pharmaceutical Sciences Branch;
2Chemical Engineering Department, Islamic Azad University, South Tehran Branch, 3Department of Pilot Nanobiotechnology, Pasteur Institute of Iran, Tehran, Iran.
For correspondence:- Azim Akbarzadeh
Email: azimakbarzadeh1326@gmail.com Tel:+982166465406
Received: 25 March 2015
Accepted: 24 June 2015
Published: 30 August 2015
Citation:
Eskolaky EB, Ardjmand M, Akbarzadeh A.
Evaluation of anti-cancer properties of pegylated ethosomal paclitaxel on human melanoma cell line SK-MEL-3. Trop J Pharm Res 2015; 14(8):1421-1425
doi:
10.4314/tjpr.v14i8.14
© 2015 The authors.
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Abstract
Purpose: To prepare pegylated ethosomal Paclitaxel® by reverse phase evaporation technique, and evaluate its cytotoxic effect on SK-MEL-3 cell line.
Methods: Nanodrug was prepared by reverse phase evaporation technique. The characteristics of the nanoparticles were evaluated by a zetasizer and scanning electron microscopy (SEM). Drug loading and encapsulation efficiency as well as paclitaxel® release were determined spectrophotometerically at 227 nm while the cytotoxicity of the pegylated ethosomal nanoencapsulated Paclitaxel® was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on SK-MEL-3 cell line.
Results: The mean diameter and zeta potential of drug-loaded pegylated ethosomal particles and blank pegylated ethosomes were 138.1 ± 2.7 nm and -13.1 mV, and 102.3 ± 2.1 nm and -19.2 mV, respectively, while drug loading and encapsulation efficiency were 2.82 ± 0.27 and 96 ± 1.27 %, respectively. The drug release pattern indicates that the half-life (t1/2) of the nanodrug was approximately twice that of the free drug for both static and dynamic release. Toxicological results indicate approx. 4.5-fold cytotoxicity against SK-MEL-3 cell line compared with the free drug.
Conclusion: This study shows that pegylated ethosomal Paclitaxel® is significantly considerably more toxic than the free drug on SK-MEL-3 cell line, thus making it an potential alternative to the standard therapy. It is, however, necessary to evaluate the nanoformulation in vivo.
Keywords: Paclitaxel®, Ethosome, Reverse phase evaporation, Pegylated, Cytotoxicity, Nanoparticles, Drug release