Jain Sanyog, Dongave Shesherao M, Date Tushar, Kushwah Varun, Mahajan Rahul R, Pujara Naisarg, Kumeria Tushar, Popat Amirali
Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sec 67, S.A.S. Nagar (Mohali), Punjab 160062, India.
School of Pharmacy, The University of Queensland Brisbane, Queensland 4102, Australia.
ACS Biomater Sci Eng. 2019 Jul 8;5(7):3361-3372. doi: 10.1021/acsbiomaterials.9b00268. Epub 2019 Jun 5.
PEGylation (i.e., attachment of polyethylene-glycol) of carbon nanotubes (CNTs) is one of the most widely used strategies to improve its biocompatibility and aqueous dispersion stability, which are critical for their successful clinical application. However, PEGylation of nanomaterials has recently been associated with production of anti-PEG antibody, low cellular uptake, and degradation. Herein, we explore surface functionalization of CNTs using the bovine-milk-derived protein succinylated β-lactoglobuline (Sblg) as an alternative strategy to PEGylation. The aqueous dispersion stability, in vitro cell uptake and biocompatibility of Sblg-functionalized multiwalled CNTs (Sblg-f-MWCNTs) was compared to PEGylated MWCNTs (PEG-f-MWCNTs). The surface functionalization with Sblg was found to improve the IC50 values of CNTs by ∼5- to 6-fold in comparison with pristine CNTs in various cell lines. Both Sblg-f-MWCNTs and PEG-f-MWCNTs improved the aqueous colloidal stability of CNTs, which remained suspended for a period of one month. Our study concluded that the Sblg provides a cost-effective alternative to the PEG-based CNT functionalization with significant improvement in the biocompatibility and dispersion stability of CNTs.
碳纳米管（CNTs）的聚乙二醇化（即连接聚乙二醇）是提高其生物相容性和水分散稳定性最广泛使用的策略之一，而这对于它们成功的临床应用至关重要。然而，纳米材料的聚乙二醇化最近与抗聚乙二醇抗体的产生、低细胞摄取率和降解有关。在此，我们探索使用源自牛乳的蛋白质琥珀酰化β-乳球蛋白（Sblg）对碳纳米管进行表面功能化，作为聚乙二醇化的替代策略。将Sblg功能化的多壁碳纳米管（Sblg-f-MWCNTs）与聚乙二醇化的多壁碳纳米管（PEG-f-MWCNTs）在水分散稳定性、体外细胞摄取和生物相容性方面进行了比较。结果发现，与原始碳纳米管相比，用Sblg进行表面功能化可使碳纳米管在各种细胞系中的半数抑制浓度（IC50）值提高约5至6倍。Sblg-f-MWCNTs和PEG-f-MWCNTs都提高了碳纳米管的水胶体稳定性，它们在一个月的时间内都保持悬浮状态。我们的研究得出结论，Sblg为基于聚乙二醇的碳纳米管功能化提供了一种经济高效的替代方法，能显著提高碳纳米管的生物相容性和分散稳定性。
