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Open AccessArticle

Enhanced Efficacy of PEGylated Liposomal Cisplatin: In Vitro and In Vivo Evaluation

1
Department of Chemical Engineering, Shahrood Branch, Islamic Azad University, Shahrood 36155-163, Iran
2
Department of Pilot Nanobiotechnology, Pasteur Institute of Iran, Tehran 1316943551, Iran
3
Department of Microbiology, School of Medicine, Rafsanjan University of Medical Sciences, Rafsanjan 7717933777, Iran
4
School of Pharmacy, The University of Queensland, Woolloongabba 4102, Australia
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(2), 559; https://doi.org/10.3390/ijms21020559
Received: 19 December 2019 / Revised: 9 January 2020 / Accepted: 12 January 2020 / Published: 15 January 2020
(This article belongs to the Special Issue Development of Responsive Nanoparticles for Cancer Therapy)
This study aims to evaluate the potency of cisplatin (Cispt)-loaded liposome (LCispt) and PEGylated liposome (PLCispt) as therapeutic nanoformulations in the treatment of bladder cancer (BC). Cispt was loaded into liposomes using reverse-phase evaporation method, and the formulations were characterized using dynamic light scattering, scanning electron microscopy, dialysis membrane, and Fourier-transform infrared spectroscopy (FTIR) methods. The results showed that the particles were formed in spherical monodispersed shapes with a nanoscale size (221–274 nm) and controlled drug release profile. The cytotoxicity effects of LCispt and PLCispt were assessed in an in vitro environment, and the results demonstrated that PLCispt caused a 2.4- and 1.9-fold increase in the cytotoxicity effects of Cispt after 24 and 48 h, respectively. The therapeutic and toxicity effects of the formulations were also assessed on BC-bearing rats. The results showed that PLCispt caused a 4.8-fold increase in the drug efficacy (tumor volume of 11 ± 0.5 and 2.3 ± 0.1 mm3 in Cispt and PLCispt receiver rats, respectively) and a 3.3-fold decrease in the toxicity effects of the drug (bodyweight gains of 3% and 10% in Cispt and PLCispt receiver rats, respectively). The results of toxicity were also confirmed by histopathological studies. Overall, this study suggests that the PEGylation of LCispt is a promising approach to achieve a nanoformulation with enhanced anticancer effects and reduced toxicity compared to Cispt for the treatment of BC. View Full-Text
Keywords: cisplatin; drug delivery; nanoparticle; PEG; PEGylated liposome; polyethylene glycol; liposome cisplatin; drug delivery; nanoparticle; PEG; PEGylated liposome; polyethylene glycol; liposome
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Ghaferi, M.; Asadollahzadeh, M.J.; Akbarzadeh, A.; Ebrahimi Shahmabadi, H.; Alavi, S.E. Enhanced Efficacy of PEGylated Liposomal Cisplatin: In Vitro and In Vivo Evaluation. Int. J. Mol. Sci. 2020, 21, 559.

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