Mizuhara Tsukasa, Saha Krishnendu, Moyano Daniel F, Kim Chang Soo, Yan Bo, Kim Young-Kwan, Rotello Vincent M
Department of Chemistry, University of Massachusetts Amherst, 710 North Pleasant Street, Amherst, MA 01003 (USA).
Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501 (Japan).
Angew Chem Int Ed Engl. 2015 May 26;54(22):6567-70. doi: 10.1002/anie.201411615. Epub 2015 Apr 14.
A nanoparticle design featuring pH-responsive alkoxyphenyl acylsulfonamide ligands is reported herein. As a result of ligand structure, this nanoparticle is neutral at pH 7.4, becoming positively charged at tumor pH (<6.5). The particle uptake and cytotoxicity increase over this pH range. This pH-controlled uptake and toxicity makes this particle a promising tool for tumor selective therapy.
本文报道了一种具有pH响应性烷氧基苯基酰基磺酰胺配体的纳米颗粒设计。由于配体结构,这种纳米颗粒在pH 7.4时呈中性,在肿瘤pH值(<6.5)时带正电荷。在这个pH范围内,颗粒的摄取和细胞毒性增加。这种pH控制的摄取和毒性使这种颗粒成为肿瘤选择性治疗的一个有前途的工具。