One‐Pot Synthesis of DOX@Covalent Organic Framework with Enhanced Chemotherapeutic Efficacy

Abstract

Covalent organic frameworks (COFs) have attracted great attention across diverse research fields. However, only a few reports about the biomedical application of COFs are found in the literature. Attributed to the highly porous and tunable structure, as well as good thermal stability, COFs show great potential as drug carriers for chemotherapy. In this work, doxorubicin (DOX) was successfully in situ loaded into a COF by a one‐pot method for the first time. The resultant DOX@COF platform exhibited high drug‐loading capacity (32.1 wt %) and pH‐responsive release property. In vitro and in vivo experiments demonstrated its good biocompatibility and enhanced antitumor efficacy.

Covalent Organic Frameworks (COFs) for Cancer Therapeutics

“…Scanning electron micrographs (left) and in vivo antitumor effects (right) of the nanoscale COF are shown. Adapted with permission . Copyright 2019, Wiley‐VCH.…”

“…The third method involves preparing COF nanosheets (e.g., 5‐FU@TpASH‐FA in Figure A) or nanoparticles. For instance, TAPB‐DMTP‐COF particles (Figure C) with an average size of 200 nm were synthesized by a Schiff‐base condensation between 2,5‐dimethoxyterephthaldehyde (DMTP) and 1,3,5‐tris(4‐aminophenyl)benzene (TAPB) . When the NCOF was used as a delivery vehicle for DOX, DOX@COF displayed excellent in vivo antitumor effects owing to enhanced dispersion and cell affinity.…”

BODIPY-Decorated Nanoscale Covalent Organic Frameworks for Photodynamic Therapy

“…As a promising alternative to MOFs, metal-free covalent organic frameworks (COFs) (Bisbey and Dichtel, 2017, Lohse and Bein, 2018) should be more biocompatible and suitable for biomedical treatment because of their pure organic nature (Figure S1, see Normal Tissue Cytotoxicity Test in Transparent Methods for experimental details) (Guan et al., 2018b, Jiang et al., 2019, Ruyra et al., 2015, Tamames-Tabar et al., 2014). Some examples of COF-based biomedical applications have been reported, such as fluorescence bioimaging (Das et al., 2018, Li et al., 2017, Liu et al., 2019b, Wang et al., 2018a), drug delivery (Bai et al., 2016, Fang et al., 2015, Liu et al., 2019a, Mitra et al., 2017, Vyas et al., 2016b, Zhang et al., 2018b), antibacterial therapy (Hynek et al., 2018, Liu et al., 2017, Mitra et al., 2016), enzyme immobilization (Kandambeth et al., 2015, Sun et al., 2018c), biochemical analysis (Liu et al., 2019c, Yan et al., 2019, Zhang et al., 2018e, Zhang et al., 2018f, Zhou et al., 2019), and so on. In addition, some conceptual therapeutic models, such as 1 O 2 generation (Feng et al., 2016, Lin et al., 2017, Nagai et al., 2013), photothermal conversion (Tan et al., 2016), and apoptosis induction (Bhanja et al., 2017), have also been reported.…”

Nanoscale covalent organic frameworks as theranostic platforms for oncotherapy: synthesis, functionalization, and applications

“…The particle size of the obtained TAPB-PDA COF varied from the minimum of 200 nm to the maximum of 500 nm with changes in the initial monomer concentration. This approach has been widely applied to the synthesis of various Schiff-base COFs, [220][221][222][223][224] implying its widespread feasibility.…”

“…Here, we will introduce the different kinds of methods to make the bread: COF-based oncotherapy examples. Till now, COFs have been used as drug delivery carriers, 221,[396][397][398][399][400][401][402][403] phototherapy reagents, 163,216,223,261,[404][405][406][407][408][409][410] and combination therapy platforms 161,162,220,[411][412][413][414][415] for tumor therapeutics ( Table 5).…”