Department of Chemistry and Chemical Biology, Rutgers University, Piscataway, NJ, USA.
Nanoscale. 2022 Mar 24;14(12):4456-4462. doi: 10.1039/d2nr00777k.
We demonstrate the use of water-soluble C-β-cyclodextrin conjugates to encapsulate and deliver doxorubicin to the cell nucleus. The behaviour of the fullerene aggregates inside cells is dictated by the functionalization of the C cage. While both the C conjugates are taken up by lysosomes upon cellular entry, only the one with a hydroxylated cage rapidly escaped the lysosome. The drug delivery system (DDS) with a hydroxylated C cage showed significantly enhanced doxorubicin delivery to the cell nucleus, whereas the DDS with a hydrophobic C cage was trapped in the lysosome for a longer time and showed significantly reduced doxorubicin delivery to the nucleus. This study opens new paths towards advanced fullerene-based DDSs for small molecule drugs.
我们展示了水溶性 C-β-环糊精缀合物在将阿霉素包封并递送至细胞核中的应用。富勒烯聚集体在细胞内的行为取决于 C 笼的功能化。虽然这两种 C 缀合物在进入细胞时都被溶酶体摄取，但只有具有羟基化笼的那一种能够迅速从溶酶体中逃逸。具有羟基化 C 笼的药物传递系统（DDS）显著增强了阿霉素向细胞核的传递，而具有疏水性 C 笼的 DDS 则在溶酶体中被捕获更长时间，并且向细胞核传递的阿霉素明显减少。这项研究为基于富勒烯的小分子药物的先进药物传递系统开辟了新的途径。
