Maedeh Koohi Moftakhari Esfahani1,
Seyed Ebrahim Alavi1,
Azim Akbarzadeh2,
Soheil Ghassemi2,
Zahra Saffari2,
Maryam Farahnak2,
Mohsen Chiani2 
For correspondence:- Mohsen Chiani Email: chiani110@yahoo.com Tel:+982166968856
Received: 5 October 2013 Accepted: 27 June 2014 Published: 18 August 2014
Citation: Esfahani MK, Alavi SE, Akbarzadeh A, Ghassemi S, Saffari Z, Farahnak M, et al. Pegylation of Nanoliposomal Paclitaxel Enhances its Efficacy in Breast Cancer. Trop J Pharm Res 2014; 13(8):1195-1198 doi: 10.4314/tjpr.v13i8.1
© 2014 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
Purpose: To encapsulate paclitaxel into nanoliposomes, followed by pegylatation, in order to improve its therapeutic index and reduce side effects in breast cancer.
Methods: In order to prepare nanoliposomal paclitaxel, varying ratios of phosphatidylcholine, cholesterol and paclitaxel were mixed and the formulations pegylated with poly-ethylene glycol 2000 (PEG 2000) to enhance stability, efficiency, as well as solubility. The mean diameter of nanoliposomal paclitaxel and pegylated nanoliposomal paclitaxel were measured by Zeta sizer device and release of paclitaxel from both formulations was determined within 28 h by dialysis method. The cytotoxicity of nanoliposomal and pegylated nanoliposomal paclitaxel was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay.
Results: The mean diameter of nanoliposomal paclitaxel and pegylated nanoliposomal paclitaxel was 421.4 and 369.1 nm, respectively, while encapsulation efficiency was 91.3 ± 5.7 and 95.2 ± 6.3 %, respectively. Paclitaxel released from both formulations in 28 h was 5.53 and 5.02 %, respectively. The cytotoxicity of pegylated nanoliposomal paclitaxel was significantly (p F6; 0.05) greater than that of nanoliposomal paclitaxel (their IC50 = 79.8±2.9 and 86.25±3.4 µg/ml, respectively).
Conclusion: The release pattern and cytotoxicity of pegylated nanoliposomal paclitaxel show that the formulation is superior to nanoliposomal paclitaxel. Furthermore, the mean particle size of pegylated nanoliposome is smaller than that of the non-pegylated preparation.
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