聚乙二醇化多壁碳纳米管作为多功能载体，用于肿瘤特异性细胞内触发释放，提高抗癌效率：长度和聚乙二醇化程度的优化。
PEGylated multi-walled carbon nanotubes as versatile vector for tumor-specific intracellular triggered release with enhanced anti-cancer efficiency: Optimization of length and PEGylation degree.
机构信息
State Key Laboratory of Applied Organic Chemistry and Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, China.
State Key Laboratory of Applied Organic Chemistry and Key Laboratory of Nonferrous Metal Chemistry and Resources Utilization of Gansu Province, College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, China.
出版信息
Colloids Surf B Biointerfaces. 2018 Aug 1;168:43-49. doi: 10.1016/j.colsurfb.2018.02.041. Epub 2018 Feb 20.
PEGylated multi-walled carbon nanotubes (PEG-MWCNTs) were optimized as versatile vector for tumor-specific intracellular triggered release of doxorubicin (DOX), based on the effect of their length and PEGylation degree on the cytotoxicity and DOX-loading capacity. The length and surface carboxyl groups of the carboxylated multi-walled carbon nanotubes (CMWCNTs) were easily tailored by adjusting the oxidation time. The longer CMWCNTs or those with high carboxyl group content showed obvious cytotoxicity, while the PEG-MWCNTs ≤ 300 nm showed better cytocompatibility. The PEG-MWCNTs-3 of about 300 nm was selected as drug delivery vector, possessing a high drug-loading capacity of 0.55 mg/mg. They released DOX rapidly under lower pH media mimicking the tumor microenvironment with cumulative release of 57% within 24 h, while the premature leakage under the simulated physiological condition was only 10%. The WST-1 assays demonstrated the DOX-loaded PEG-MWCNTs-3 exhibited the enhanced inhibitory efficiency against HepG2 cells, in comparison with free DOX.
聚乙二醇化多壁碳纳米管（PEG-MWCNTs）被优化为用于肿瘤特异性细胞内触发释放阿霉素（DOX）的多功能载体，这是基于其长度和聚乙二醇化程度对细胞毒性和 DOX 载药能力的影响。通过调整氧化时间，可以轻松调整羧基化多壁碳纳米管（CMWCNTs）的长度和表面羧基含量。较长的 CMWCNTs 或具有高羧基含量的 CMWCNTs 表现出明显的细胞毒性，而长度≤300nm 的 PEG-MWCNTs 表现出更好的细胞相容性。选择约 300nm 的 PEG-MWCNTs-3 作为药物输送载体，具有 0.55mg/mg 的高载药能力。它们在模拟肿瘤微环境的较低 pH 介质中迅速释放 DOX，在 24 小时内累积释放 57%，而在模拟生理条件下的过早泄漏仅为 10%。WST-1 测定表明，与游离 DOX 相比，载 DOX 的 PEG-MWCNTs-3 对 HepG2 细胞表现出增强的抑制效率。
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