A Comparative Evaluation of Hydroxycamptothecin Drug Nanorods With and Without Methotrexate Prodrug Functionalization for Drug Delivery

• Published in: Nanoscale research letters Vol. 11; no. 1; pp. 384 - 7
• Main Authors: Guo, Fuqiang, Fan, Zhongxiong, Yang, Jinbin, Li, Yang, Wang, Yange, Zhao, Hai, Xie, Liya, Hou, Zhenqing
• Format: Journal Article
• Language: English
• Published: New York Springer US 01.12.2016; Springer Nature B.V
• Subjects: Cancer; Chemistry and Materials Science; Drug delivery systems; Drugs; In vitro testing; Materials Science; Methotrexate; Molecular Medicine; Nano Express; Nanochemistry; Nanoscale Science and Technology; Nanostructure; Nanotechnology; Nanotechnology and Microengineering; Strategy; Uptakes; 10-Hydroxycamptothecin; Self-targeted multi-drug co-delivery system; Controlled and sustained release; Methotrexate
• ISSN: 1931-7573; 1556-276X
• DOI: 10.1186/s11671-016-1599-y

We developed a novel self-targeted multi-drug co-delivery system based on rod-shaped 10-hydroxycamptothecin (CPT) nanoanticancer drug (CPT NRs) followed by a surface functionalization with self-targeting PEGylated lipid-conjugated methotrexate (MTX) pro-anticancer drug. The self-targeting effect and in vitro cell viability of the MTX-PEG-CPT NRs on HeLa cells were demonstrated by comparative cellular uptake and MTT assay of the PEG-CPT NRs. In vitro studies showed the feasibility of using this high drug-loading MTX-PEG-CPT NRs in self-targeted drug delivery, controlled-/sustained-release, and synergistic cancer therapy. More importantly, this work would stimulate interest in the use of PEGylated lipid-conjugated MTX by introducing an early-phase tumor-targeting role and then driving a late-phase anticancer role for the highly convergent design of nanomulti-drug, which may advantageously offer a new and simple strategy for simultaneously targeting and treating FA receptor-overexpressing cancer cells.