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

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. Graphical Abstract.

Surface-functionalised polymeric nanoparticles for breast cancer treatment: processes and advances.

The World Health Organization (WHO) reported that of all the non-communicable diseases, cancer is considered the second cause of death worldwide. This has driven the big pharma companies to prioritise anticancer products in their pipeline. In addition, research has focused on exploration of new anticancer molecules and design of suitable dosage forms to achieve effective drug delivery to the tumour site. Nanotechnology is a valuable tool to build nano delivery systems with controlled and targeted drug release properties. Nanoparticles can be fabricated by robust, scalable and economic techniques using various polymers. Moreover, specific functional groups can be introduced to the surface of nanoparticles enabling targeting to a specific tissue; besides, they exhibit versatile drug release patterns according to the rate of polymer degradation. This review outlines the processes and advances in surface functionalisation of nanoparticles employed for treatment of breast cancer. The therapeutic molecules, the polymers used to fabricate nanoparticles, the techniques used to prepare the nanoparticles have been reviewed with a focus on the processes employed to functionalise these nanoparticles with suitable ligands to target different types of breast cancer.

In Situ Hexosomal Gel as a Promising Tool to Ameliorate the Transnasal Brain Delivery of Vinpocetine: Central Composite Optimization and In Vivo Biodistribution.

Vascular dementia is a condition characterized by a wretched cerebral circulation which can lead to memory loss. Vinpocetine showed ability to promote the cerebral circulation and depict neuroprotective impacts. However, it suffers from poor bioavailability and requires frequent daily dosing which is not suitable for dementia patients. In our study, these limitations were overcome by the prolonged direct delivery of vinpocetine to the brain utilizing an intranasal in situ hexosomal gel. A central composite design was utilized and the optimum dispersion (consisting of 15% w/w of oleic acid and 5% w/w of pluronic F127) was loaded in an in situ gel system using gellan gum with 1% w/v. The optimized Formulae achieved a controlled drug release over 24 h and the pharmacokinetic data revealed that the Cmax and AUC0-24 in the rats' brain after the intranasal application of the dispersion and in situ gel were significantly higher relative to the vinpocetine solution applied intravenously at the same dose. The potential of both formulae to deliver vinpocetine to the brain directly through the intranasal route was confirmed by the high BTE% of 370.97% and 480.70% and the high DTP% of 73.04% and 79.19% for the dispersion and in situ gel, respectively.