Ruan Shaobo, Wan Jingyu, Fu Yao, Han Ke, Li Xiang, Chen Jiantao, Zhang Qianyu, Shen Shun, He Qin, Gao Huile
Key Laboratory of Drug Targeting and Drug Delivery Systems, West China School of Pharmacy, Sichuan University , No. 17, Block 3, Southern Renmin Road, Chengdu 610041, China.
Bioconjug Chem. 2014 Jun 18;25(6):1061-8. doi: 10.1021/bc5001627. Epub 2014 May 22.
Fluorescent carbon nanoparticles (CNP) have gained much attention due to their unique fluorescent properties and safety. In this study, we evaluated the potential application of CNP and PEGylated CNP (PEG-CNP) in noninvasive heart imaging. CNP was prepared by hydrothermal treatment of silk. The particle size and zeta potential of CNP were 121.8 nm and -3.7 mV, respectively, which did not change significantly after PEGylation with a PEG density of 4.43 ± 0.02 μg/mg CNP. FTIR and XPS showed that CNP possessed several functional groups, such as -COOH, -OH, and NH2, which could be utilized for PEGylation and other modifications. CNP displayed strong blue fluorescence after excitation at the wavelength of 375 nm. PEG-CNP displayed better serum stability compared to CNP. The hemolysis rate of PEG-CNP was lower than that of CNP, suggesting PEGylation could enhance the hemocompatibility of CNP. Both CNP and PEG-CNP showed higher uptake capacity by H9c2 cells (a heart cell line) than that by human umbilical vein endothelial cells (HUVEC), suggesting the particles tend to be selectively taken up by heart cells. Both CNP and PEG-CNP were proven to be taken up through endosome-mediated pathway, and the colocalization of nanoparticles with mitochondria was also observed. In vivo results demonstrated that CNP could target heart with much higher fluorescent intensity than liver and spleen. Although PEGylation could decrease the distribution in heart, it remained high for PEG-CNP. In conclusion, CNP could be used for heart imaging, and moreover, PEGylation could improve the stability and biocompatibility of CNP.
荧光碳纳米颗粒(CNP)因其独特的荧光特性和安全性而备受关注。在本研究中,我们评估了CNP和聚乙二醇化碳纳米颗粒(PEG-CNP)在无创心脏成像中的潜在应用。通过对丝绸进行水热处理制备了CNP。CNP的粒径和zeta电位分别为121.8 nm和-3.7 mV,在用密度为4.43±0.02 μg/mg CNP的聚乙二醇进行聚乙二醇化后,其粒径和zeta电位没有显著变化。傅里叶变换红外光谱(FTIR)和X射线光电子能谱(XPS)表明,CNP具有多个官能团,如-COOH、-OH和NH2,可用于聚乙二醇化和其他修饰。在375 nm波长激发后,CNP发出强烈的蓝色荧光。与CNP相比,PEG-CNP表现出更好的血清稳定性。PEG-CNP的溶血率低于CNP,这表明聚乙二醇化可以提高CNP的血液相容性。CNP和PEG-CNP对H9c2细胞(一种心脏细胞系)的摄取能力均高于人脐静脉内皮细胞(HUVEC),这表明这些颗粒倾向于被心脏细胞选择性摄取。CNP和PEG-CNP均被证明是通过内吞体介导的途径被摄取的,并且还观察到纳米颗粒与线粒体的共定位。体内结果表明,CNP能够靶向心脏,其荧光强度远高于肝脏和脾脏。虽然聚乙二醇化会减少在心脏中的分布,但PEG-CNP在心脏中的分布仍然很高。总之,CNP可用于心脏成像,此外,聚乙二醇化可以提高CNP的稳定性和生物相容性。