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ACS Appl Mater Interfaces. 2017 Sep 6;9(35):29505-29514. doi: 10.1021/acsami.7b07565. Epub 2017 Aug 25.

Construction of a Supramolecular Drug-Drug Delivery System for Non-Small-Cell Lung Cancer Therapy.

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School of Chemistry and Chemical Engineering, State Key Laboratory of Metal Matrix Composites, Shanghai Jiao Tong University , 800 Dongchuan Road, Shanghai 200240, People's Republic of China.


Nanoscale drug delivery systems (DDSs) are generally considered to be an effective alternative to small molecular chemotherapeutics due to improved accumulation in the tumor site and enhanced retention in blood. Nevertheless, most DDSs have low loading efficiency or even pose a high threat to normal organs from severe side effects. Ideally, a supramolecular drug-drug delivery system (SDDDS) composed of pure drugs via supramolecular interaction provides a hopeful approach for cancer treatment. Herein we propose a facile method to construct SDDDS via coassembly of gefitinib (GEF) and tripeptide tyroservatide (YSV), two kinds of chemotherapeutic pharmaceuticals for non-small-cell lung cancer (NSCLC) via multiple intermolecular interactions, including hydrogen bonding and π-π stacking. As shown through transmission electron microscopy (TEM) and dynamic light scattering (DLS), GEF and YSV self-assemble into nanoparticles with regular morphology and uniform size, which facilitates the delivery of both drugs. In vitro studies demonstrate that the SDDDS is much more efficient in entering cancer cells and inhibiting the proliferation of cancer cells compared with single GEF, YSV, or GEF/YSV drug mixture. In vivo experiments show that the SDDDS can selectively accumulate in tumor tissue, resulting in much better drug efficacy without evident side effects. Considering the advantages of the SDDDS, we believe this strategy provides a promising route for enhanced anticancer therapy in nanomedicine.


chemotherapy; drug delivery; nanoparticles; non-small-cell lung cancer; self-assembly

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