Quercitrin loaded cyclodextrin based nanosponge as a promising approach for management of lung cancer and COVID-19

Sally Abou Taleb; Yassmin Moatasim; Mohamed GabAllah; Marwa Hasanein Asfour

doi:10.1016/j.jddst.2022.103921

Quercitrin loaded cyclodextrin based nanosponge as a promising approach for management of lung cancer and COVID-19

J Drug Deliv Sci Technol. 2022 Nov:77:103921. doi: 10.1016/j.jddst.2022.103921. Epub 2022 Oct 28.

Authors

Sally Abou Taleb¹, Yassmin Moatasim², Mohamed GabAllah², Marwa Hasanein Asfour¹

Affiliations

¹ Pharmaceutical Technology Department, National Research Centre, El-Buhouth Street, Dokki, Cairo, 12622, Egypt.
² Center of Scientific Excellence for Influenza Viruses, National Research Centre, El-Buhouth Street, Dokki, Cairo, 12622, Egypt.

Abstract

Lung cancer and pandemic acute respiratory disease, COVID-19, are examples of the most worldwide widespread diseases. The aim of the current study is to develop cyclodextrin based nanosponge (CD-NS) for loading the flavonoid drug, quercitrin (QCT). This is to improve its solubility in an attempt to enhance its activity against lung cancer as well as SARS-CoV-2 virus responsible for COVID-19. Preparation of CD-NS was performed by ultrasound-assisted synthesis method. Two CDs were employed, namely, β cyclodextrin (βCD) and 2-hydroxy propyl-β-cyclodextrin (2-HPβCD) that were crosslinked with diphenyl carbonate, one at a time. QCT loaded CD-NS revealed entrapment efficiency and particle size ranged between 94.17 and 99.03% and 97.10-325.90 nm, respectively. QCT loaded 2-HPβCD-NS revealed smaller particle size compared with that of QCT loaded βCD-NS. Zeta potential absolute values of the prepared formulations were >20 mV, indicating physically stable nanosystems. The selected formulations were investigated by Fourier transform infrared spectroscopy, X-ray powder diffraction and scanning electron microscopy which proved the formation of QCT loaded CD-NS exhibiting porous structure. QCT exhibited partial and complete amorphization in βCD-NS and 2-HPβCD-NS, respectively. In vitro release revealed an improved release of QCT from CD-NS formulations. The biological activity of free QCT and QCT loaded CD-NS was investigated against lung cancer cell line A549 as well as SARS-CoV-2 virus. The results revealed that IC₅₀ values of free QCT against lung cancer cell line A549 and SARS-CoV-2 were higher than those exhibited by QCT loaded CD-NS by 1.57-5.35 and 5.95-26.95 folds, respectively. QCT loaded 2-HPβCD-NS revealed enhanced in vitro release and superior biological activity compared with QCT loaded βCD-NS.

Keywords: A549 lung cancer cell line; COVID-19; Cyclodextrins; Nanosponge; Quercitrin; SARS-CoV-2.