Three-Dimensional Covalent Organic Frameworks with pts Topology for Controlled Anticancer Drug Delivery

03 April 2023, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

Noted for their unique structural and functional attributes including especially high surface areas, open interconnected nanochannels and rich active sites, three-dimensional (3D) covalent organic frameworks (COFs) have emerged as frontier materials for energy, environmental and biomedical research. However, the limited options of 3D organic building blocks, poor reversibility in covalent linkage formation and highly complicated crystal structure analysis raise several challenges to the construction of new 3D COFs for which the number of 3D COF structures is still restricted to a few. In this contribution, we report the designed synthesis of two new 3D COFs, namely TUS-440 and TUS-441, with two- and three-fold interpenetrated pts topology, respectively, by combining a Td-symmetric tetrahedral vertex with two C2-symmetric rectangular linkers. The resulting COFs demonstrate well-defined crystalline porous structures and Brunauer−Emmett−Teller surface areas of 1320 and 940 m2 g-1. In vitro drug delivery studies substantiate these COFs as efficient nanocarriers with good loading and sustained release of anticancer drugs (cytarabine and 5-fluorouracil), showing great potential for increasing therapeutic efficacy and reducing dosing frequency.

Keywords

covalent organic framework
three-dimensional
topology
drug delivery
controlled release

Supplementary materials

Title
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Title
Three-Dimensional Covalent Organic Frameworks with pts Topology for Controlled Anticancer Drug Delivery
Description
In this contribution, we report the designed synthesis of two new 3D COFs, namely TUS-440 and TUS-441, with two- and three-fold interpenetrated pts topology, respectively, by combining a Td-symmetric tetrahedral vertex with two C2-symmetric rectangular linkers. The resulting COFs demonstrate well-defined crystalline porous structures and Brunauer−Emmett−Teller surface areas of 1320 and 940 m2 g-1. In vitro drug delivery studies substantiate these COFs as efficient nanocarriers with good loading and sustained release of anticancer drugs (cytarabine and 5-fluorouracil), showing great potential for increasing therapeutic efficacy and reducing dosing frequency.
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