Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19

Abstract

Investigating bicelles as an oral drug delivery system and exploiting their structural benefits can pave the way to formulate hydrophobic drugs and potentiate their activity. Herein, the ability of non-ionic surfactants (labrasol®, tween 80, cremophore EL and pluronic F127) to form curcumin loaded bicelles with phosphatidylcholine, utilizing a simple method, was investigated. Molecular docking was used to understand the mechanism of bicelles formation. The % transmittance and TEM exhibited bicelles formation with labrasol® and tween 80, while cremophor EL and pluronic F127 tended to form mixed micelles. The surfactant-based nanostructures significantly improved curcumin dissolution (99.2 ± 2.6% within 10 min in case of tween 80-based bicelles) compared to liposomes and curcumin suspension in non-sink conditions. The prepared formulations improved curcumin ex vivo permeation over liposomes and drug suspension. Further, the therapeutic antiviral activity of the formulated curcumin against SARS-CoV-2 was potentiated over drug suspension. Although both Labrasol® and tween 80 bicelles could form bicelles and enhance the oral delivery of curcumin when compared to liposomes and drug suspension, the mixed micelles formulations depicted superiority than bicelles formulations. Our findings provide promising formulations that can be utilized for further preclinical and clinical studies of curcumin as an antiviral therapy for COVID-19 patients.

Formulation of Chitosan-Coated Brigatinib Nanospanlastics: Optimization, Characterization, Stability Assessment and In-Vitro Cytotoxicity Activity against H-1975 Cell Lines

“…Moreover, the Span-60:EA ratio 3:2 showed larger vesicles’ size than those of 4:1 ratio and this may be due to the higher EA concentration that led to the larger vesicles’ size. Both Tween ® 80 and Pluronic F127 are hydrophilic nonionic surfactants [ 35 ] that impart flexibility to the bilayer membranes of NSPs [ 36 ] and, thus, increase the elasticity of the vesicles and water uptake so leading to an increase in the vesicles’ size. PDI is an indicator of the vesicles’ size distribution and its value ranges from 0.0 (for completely uniform vesicles’ size distribution) to 1.0 (for highly polydispersed vesicles).…”

Anticoagulants as Potential SARS-CoV-2 Mpro Inhibitors for COVID-19 Patients: In Vitro, Molecular Docking, Molecular Dynamics, DFT, and SAR Studies

“…The X-ray composition of the M pro receptor of SARS-CoV-2 was attained by downloading from Protein Data Bank (PDB code: 6Y2G) [ 31 ]. Hence, the target protein became ready for the docking studies after considering the following steps: the backbones and side chains of the target protein were protonated with respect to their 3D geometry, the corrections were automatically utilized for the atom’s connection and type to check for any errors, and the receptor potential was fixed as discussed before [ 62 , 63 , 64 , 65 ]. CHARMM27 was implemented as the selected force field, and the native co-crystallized inhibitor active pocket was selected, as displayed before [ 66 , 67 , 68 , 69 ].…”

Design, synthesis, biological evaluation, and SAR studies of novel cyclopentaquinoline derivatives as DNA intercalators, topoisomerase II inhibitors, and apoptotic inducers

“…Docking of the synthesized compounds to human topoisomerase II-DNA complex target protein. The docking process was conducted and the general docking protocol was used following the default methodology described in detail previously, [111][112][113][114][115] thus poses with the best binding interaction scores, RMSD values, and key amino acids and nucleobases interactions were revealed.…”