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

Abstract

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(HO)K(HBTC)(HO)](HBTC)·2HO, where HBTC = 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.

Recent advances in metallopolymer-based drug delivery systems

“…157 For the delivery of small-molecule chemotherapeutic agents, such as 5-uorouracil (5-FU), one-dimensional (1D) zinc CP based on benzene-1,3,5-tricarboxylic acid (trimesic acid) was used. 158 The 5-FUloaded CP exhibited a time-dependent cytotoxicity effect against breast cancer cell lines MCF-7 and 4T1. The intratumor treatment with 5-FU-loaded CP showed favorable antitumor efficacy by inhibiting tumor growth.…”

A new 2D cadmium coordination polymer based on hydroxyl‐substituted benzenedicarboxylic acid as an effective heterogeneous catalyst for Knoevenagel condensation

“…[1] There have been several efforts to design innovative structures in recent years to apply them for diverse applications, such as molecular sensing, [2][3][4] gas storage and separation, [5,6] dye adsorption, [7] catalysis, [8] magnetism, [9] and drug delivery. [10] Low-dimensional structures have been of considerable attention in comparison with the 3D porous frameworks, due to their easily available and accessible active sites. For instance, it has been reported that 2D nanosheets of MOF-5 remarkably enhance the catalytic performance in Knoevenagel condensation, in comparison with 3D structure of MOF, including large pores and high surface area.…”

A novel core-shell nanofiber drug delivery system intended for the synergistic treatment of melanoma

“…Despite this, the adverse effects of 5-FU on normal health cells (e.g. hair loss, liver disorders) should not be neglected (Rezaei et al, 2018). Hence, extra recovery therapy following 5-FU treatment to minimize long term side-effects and impairment of normal heath tissue cells around the targeting is critical on synergism skin cancer treatments.…”