Department of Chemistry and Nano Science and Division of Life and Pharmaceutical Sciences, Department of Bioinspired Science, Ewha Womans University, Seoul, Korea.
Bioconjug Chem. 2010 Aug 18;21(8):1473-8. doi: 10.1021/bc100066k.
Dendritic amine and guanidinium group-modified nanoparticles were investigated for the delivery of model peptide drug into primary osteoclast precursor cells (bone marrow macrophages; BMMs). The model peptide drug was encapsulated into the nanoparticle by dropping the drug/carrier dissolved in dimethylsulfoxide/methylene chloride cosolvent into water containing poly(vinyl alcohol) as a stabilizer. Flow cytometry and spectrofluorimetry analysis indicated that the model drug itself was not taken up by the BMMs; however, nanoparticle systems underwent significant cellular uptake. In particular, guanidinium group-modified nanoparticles were taken up more efficiently than amine group-modified ones. Cell viability studies showed that both amine and guanidinium group-modified nanoparticles exhibited no significant cytotoxicity up to 100 microg/mL against the cells.
树突状胺和胍基改性纳米颗粒被用于将模型肽药物递送至原代破骨细胞前体细胞（骨髓巨噬细胞；BMMs）中。将药物/载体溶解在二甲基亚砜/二氯甲烷共溶剂中滴加到含有聚乙烯醇作为稳定剂的水中，从而将模型肽药物包封到纳米颗粒中。流式细胞术和荧光光谱分析表明，模型药物本身不会被 BMMs 摄取；然而，纳米颗粒系统经历了显著的细胞摄取。特别是，胍基改性纳米颗粒的摄取效率高于胺基改性纳米颗粒。细胞活力研究表明，在 100μg/mL 浓度下，两种胺基和胍基改性纳米颗粒对细胞均无明显的细胞毒性。
