Hyaluronic Acid Modified 2D Covalent Organic Framework for Targeted and Sustainable Drug Delivery.

The high surface area to volume ratio of covalent organic frameworks (COFs) provides higher surface energy, which makes them fascinating for studying the rapid adsorption of biomolecules followed by their sustained cellular delivery. Besides their many scopes of application, the therapeutic efficacy of these materials has been less explored. These hurdles are overcome herein by the surface modification of perylene-porphyrin based COF (P) with hydrophilic hyaluronic acid (HA) as confirmed by the UV, FTIR spectra, and fluorescence microscopy analyses. The resulting HA modification is shown to increase the cellular uptake of nanoparticles into CD44 expressing MDA MB231 breast cancer lines with minimum inherent toxic effects. Further, the chemotherapeutic agent doxorubicin loaded HA-P nanoparticles showed significant antitumor activity in killing the MDA MB-231 breast cancer lines at higher drug concentration (more than 80% cell death at 5 μM Dox) and even at lower ranges of Dox concentration as compared to P compound and free Dox. In summary, the developed fluorescence active multifunctional drug delivery system demonstrated superior cellular internalization with a maximum antitumor activity.