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α3β1 Integrin-Targeting Polymersomal Docetaxel as an Advanced Nanotherapeutic for Nonsmall Cell Lung Cancer Treatment
journal contribution
posted on 2020-03-18, 18:03 authored by Yan Zou, Yinping Sun, Beibei Guo, Yaohua Wei, Yifeng Xia, Zhenyuan Huangfu, Fenghua Meng, Jan C. M. van Hest, Jiandong Yuan, Zhiyuan ZhongDocetaxel
(DTX) widely used for treating nonsmall cell lung cancer
(NSCLC) patients is associated with dose-limiting side effects, especially
neurotoxicity and myelosuppression. Here, we have developed cyclic
cNGQGEQc peptide-directed polymersomal docetaxel (cNGQ-PS-DTX) as
a targeted and multifunctional formulation for NSCLC. cNGQ-PS-DTX
carrying 8.1 wt % DTX had a size of 93 nm, neutral surface charge,
high stability, and glutathione-triggered DTX release behavior. Cytotoxicity
studies demonstrated a clearly better antitumor activity of cNGQ-PS-DTX
in α3β1 integrin overexpressing
A549 human lung cancer cells than free DTX and nontargeted PS-DTX.
cNGQ-PS-DTX showed a remarkably high tolerability (over 8 times better
than free DTX) and slow elimination in mice. Importantly, cNGQ-PS-DTX
exhibited greatly improved tumor accumulation and higher suppression
of subcutaneous and orthotopic A549 xenografts as compared to PS-DTX
and free DTX controls. α3β1 integrin-targeting
polymersomal docetaxel emerges as an advanced nanotherapeutic for
NSCLC treatment.
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Cytotoxicity studiesmultifunctional formulationcyclic cNGQGEQc peptide-directed polymersomal docetaxel549 xenograftsα 3 β 1 integrin overexpressingglutathione-triggered DTX release behaviorα 3 β 1 Integrin-Targeting Polymersomal Docetaxeltumor accumulationantitumor activityNonsmall Cell Lung Cancer Treatment Docetaxelα 3 β 1 integrin-targeting polymersomal docetaxelsurface chargeNSCLC treatmentAdvanced Nanotherapeuticnonsmall cell lung cancerlung cancer cellsnontargeted PS-DTXdose-limiting side effects93 nmDTX controls8 timescNGQ-PS-DTX
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