Co-delivery of docetaxel and gemcitabine using PEGylated self-assembled stealth nanoparticles for improved breast cancer therapy.
作者： Varun Kushwah , Sameer S. Katiyar , Ashish Kumar Agrawal , Ramesh C. Gupta , Sanyog Jain
DOI: 10.1016/J.NANO.2018.04.009
关键词:
摘要: Abstract The present report deals with conjugation of dual drug; docetaxel (DTX) and gemcitabine (GEM) linker poly-ethylene-glycol (PEG) to develop amphiphilic molecule having self-assembled property. synthesized conjugate (DTX-PEG-GEM) demonstrated critical micelle concentration (CMC) in the range 5–10 μg/ml which form NPs size 124.2 ± 5.7. Remarkably higher coumarin-6 (C-6) fluorescence signals observed case C-6 loaded NPs, suggested enhanced cellular uptake via clathrin mediated endocytosis. Developed 4.8-fold AUC(0-∞) value GEM comparison Gemzar®. Tumor growth inhibition study significant reduction tumor volume survival rate NPs. Moreover, significantly lower hepato- nephro-toxicity, evident from both histopathological sections biochemical markers level estimation, hemolytic toxicity. Data hand suggest therapeutic efficacy reduced toxicity developed over conventional drugs, resulting efficient combinatorial chemotherapeutic-regimen patient compliance, is still an unmet task.
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