Pal Sudeshna, Mondal Rajarshi, Das Prasanta Kumar
School of Biological Sciences, Indian Association for the Cultivation of Science, Jadavpur, Kolkata-700032, India.
ACS Med Chem Lett. 2024 Sep 10;15(10):1668-1676. doi: 10.1021/acsmedchemlett.4c00194. eCollection 2024 Oct 10.
The present study reports the development of a novel nanoconjugate, , comprising a positively charged self-assembled nanogel (NG) derived from a peptide amphiphilic hydrogelator and a negatively charged folic acid-functionalized blue-emitting carbon dot (FACD), bound via electrostatic interactions. was developed to combine the advantages of the individual nanocarriers and overcome their drawbacks. The presence of folic acid enables to be successfully used in selective bioimaging and targeted combination therapy against folate receptor-positive (FR+) B16F10 over FR- cells. demonstrated improved riboflavin (RbF) and paclitaxel (PTX) loading compared to individual nanocarriers that made it ∼1.8- and 1.5-fold more cytotoxic toward FR+ B16F10 cells over RbF- and PTX-loaded individual nanocarriers. The concurrent presence of RbF and PTX on displayed ∼1.9-2.8-fold higher cytotoxicity than single drug-loaded individual nanocarriers and ∼3-4.5-fold higher cytotoxicity through RbF-mediated photodynamic therapy and PTX-induced chemotherapy in synergy compared to free drugs against FR+ B16F10 cells.
本研究报告了一种新型纳米共轭物的研发，该共轭物由源自肽两亲性水凝胶剂的带正电荷的自组装纳米凝胶（NG）和带负电荷的叶酸功能化蓝色发光碳点（FACD）组成，二者通过静电相互作用结合。研发该共轭物是为了结合单个纳米载体的优点并克服其缺点。叶酸的存在使该共轭物能够成功用于针对叶酸受体阳性（FR+）B16F10细胞而非FR-细胞的选择性生物成像和靶向联合治疗。与单个纳米载体相比，该共轭物显示出更高的核黄素（RbF）和紫杉醇（PTX）负载量，这使得其对FR+ B16F10细胞的细胞毒性比负载RbF和PTX的单个纳米载体分别高约1.8倍和1.5倍。与游离药物相比，该共轭物上同时存在RbF和PTX时，通过RbF介导的光动力疗法和PTX诱导的化疗协同作用，对FR+ B16F10细胞的细胞毒性比单药负载的单个纳米载体高约1.9 - 2.8倍，比游离药物高约3 - 4.5倍。
