Impact of defibrillation technique on the rheological, thermo-mechanical, and nutritional properties of nanosuspensions produced from multiple fractions of pinhão seed (Araucaria angustifolia (Bertol.) Kuntze).

This work aimed to evaluate the influence of the mechanical defibrillation technique on the pinhão nanosuspensions production obtained from the whole pinhão, its coat, and almond. The nanosuspensions were characterized concerning their composition, morphology, thermal stability, rheological behavior, compound profiling, and cytotoxicity. The results revealed a significant fiber content in pinhão coat nanosuspension (63.12 ± 0.52 %) and non-fiber carbohydrates in whole pinhão (59.00 ± 0.13 %) and almond (74.39 ± 0.23 %) nanosuspensions. The defibrillation process led to micro/nano-sized fibers in pinhão coat nanosuspensions and small-size starch granules in almond nanosuspensions. The nanosuspensions containing pinhão coat exhibited a gel-like behavior, while almond nanosuspensions displayed liquid-like characteristics. Pinhão coat nanosuspensions presented a significant content of flavonoids and phytosterols, whereas almond-based nanosuspensions contained substantial sugar amounts. No cytotoxicity was observed at the concentrations evaluated. These findings demonstrated that the defibrillation technique impacted the properties of pinhão constituents, allowing their application in new product development.

Characterization of Potent ABCG2 Inhibitor Derived from Chromone: From the Mechanism of Inhibition to Human Extracellular Vesicles for Drug Delivery.

Inhibition of ABC transporters is a promising approach to overcome multidrug resistance in cancer. Herein, we report the characterization of a potent ABCG2 inhibitor, namely, chromone 4a (C4a). Molecular docking and in vitro assays using ABCG2 and P-glycoprotein (P-gp) expressing membrane vesicles of insect cells revealed that C4a interacts with both transporters, while showing selectivity toward ABCG2 using cell-based transport assays. C4a inhibited the ABCG2-mediated efflux of different substrates and molecular dynamic simulations demonstrated that C4a binds in the Ko143-binding pocket. Liposomes and extracellular vesicles (EVs) of Giardia intestinalis and human blood were used to successfully bypass the poor water solubility and delivery of C4a as assessed by inhibition of the ABCG2 function. Human blood EVs also promoted delivery of the well-known P-gp inhibitor, elacridar. Here, for the first time, we demonstrated the potential use of plasma circulating EVs for drug delivery of hydrophobic drugs targeting membrane proteins.