Preparation of NLS-KALA-SA nanoparticles and evaluation of their nuclear targeting properties
Objective To construct a nucleus-targeted nanocarrier(NLS-KALA-SA,NKSN)consisting of fusion peptide KALA,nuclear localization signal(NLS)and stearic acid(SA).Methods The polypeptide nanocarrier NLS-KALA-SA was synthesized by Fmoc solid phase synthesis method.Results The NLS-KALA-SA nanoparticles were spherical shaped with an average size of(76.4±7.6)mm and a Zeta potential of(43.7±5.8)mV.The diameter of nanoparticles follows a normal distribution,with a narrow particle size distribution and a polydispersity index(PI)(PI<0.3).The results of cellular uptake study showed that NLS-KALA-SA nanoparticle loaded with coumarin-6(C6)(C6/NKSN)was predominantly accumulated in the nucleus of A549 cells.The results of cellular toxicity experiments showed that NLS-KALA-SA was almost no cytotoxic to A549 cells at all tested concentrations range of 0.01-1 000 mg/mL.Conclusion The results demonstrate that the NLS-KALA-SA is safe and non-toxic nanocarrier with transmembrane transport and nuclear localization functions,which is expected to become a promising peptide nanocarrier for cancer treatment.
nuclear localization signalKALA peptidenanoparticlesnucleus-targetedlung cancer
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