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Design and Synthesis of a Biocompatible 1D Coordination Polymer as Anti-Breast Cancer Drug Carrier, 5-Fu: In Vitro and in Vivo Studies

Rezaei, Mahsa, Abbasi, Alireza, Dinarvand, Rassoul, Jeddi-Tehrani, Mahmood, Janczak, Jan
ACS applied materials & interfaces 2018 v.10 no.21 pp. 17594-17604
animal models, breast neoplasms, carboxylic acids, cell lines, confocal laser scanning microscopy, coordination polymers, cytotoxicity, drug carriers, drug therapy, encapsulation, fluorescein, fluorouracil, hydrogen bonding, isothiocyanates, microparticles, neoplasm cells, staining, zinc
Designable coordination polymers with suitable chemical diversities and biocompatible structures have been proposed as a promising class of vehicles for drug delivery systems. Here, we hydrothermally synthesized a novel one-dimensional (1D) coordination polymer, [Zn(H₂O)₆K₂(H₂BTC)₂(H₂O)₄](H₂BTC)₂·2H₂O, where H₃BTC = benzene-1,3,5-tricarboxylic acid (trimesic acid), cp.1. As the hydrogen bonds stabilized 1D chains in three dimensions, the cp.1 could be a good candidate for delivering small-molecule chemotherapeutics such as 5-fluorouracil (5-Fu). The synthesized cp.1 showed a remarkable 5-Fu loading of 66% with encapsulation efficiency of 98% and almost complete release process. The 5-Fu-loaded cp.1 displayed a time-dependent cytotoxicity effect against breast cancer cell lines MCF-7 and 4T1. The cellular uptake of cp.1 particles was investigated via confocal laser scanning microscopy using fluorescein isothiocyanate and LysoTracker Red staining. Furthermore, the in vivo antitumor impact of 5-Fu-loaded cp.1 was studied on 4T1 breast cancer BALB/c mice model. The intratumor treatment of 5-Fu-loaded cp.1 demonstrated beneficial antitumor efficacy by postponing tumor growth. These results suggest that the 5-Fu-loaded cp.1 microparticles with a great locoregional delivery can be efficient anticancer drug carriers for further clinical treatments.