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Published on: February 27, 2019
PEGylated chitosan nanoparticles potentiate repurposing of ormeloxifene in breast cancer therapy
Satish Agrawal1, Hafsa Ahmad1, Monika Dwivedi1
1Pharmaceutics Division, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India.
Aim:
Development and optimization of ormeloxifene-loaded PEGylated chitosan nanoparticles (CNPs) for enhancing its literature profound therapeutic activity against breast cancer.
Methods:
CNPs were prepared by ionotropic gelation method and characterized.
Results:
Optimized formulation (CNPs10) had average 304 nm particle size with 0.247 polydispersity index and spherical shape with +31 mV surface charge. CNPs10 had 88.37% entrapment efficiency and 20.93% loading efficiency. CNPs10 demonstrated dose-dependent enhancement in cytotoxicity, cellular uptake, apoptosis, disruption of mitochondrial membrane potential and activation of caspase-3 in breast cancer MDA-MB-231 and MCF-7 cells over free ormeloxifene. In vivo studies divulged improved pharmacokinetic parameters, reduced toxicity, suppressed tumor burden and increased survival in CNPs10-treated female Sprague-Dawley rats.
Conclusion:
PEGylated CNPs enhanced anticancer activity of ormeloxifene.
