Zein, as one of the natural and GRAS proteins in plant, is renewable, nontoxic, biocompatible and biodegradable. Over the past decade, many research efforts have been devoted to zein-based biomaterials for several industrial applications. Combining with research experiences in our research group, the preparation methods, characterizations and pharmaceutical applications of zein-based nanoparticles were summarized in this review. Zein NPs with different particle nanostructures have been prepared by chemical crosslinking, desolvating, dispersing and micromixing strategies. The pharmaceutical applications of zein NPs are mainly focus on the drug delivery. Zein NPs can improve the drug stability, increase the oral bioavailability, control the drug release and enhance the drug targeting, thereby improving the pharmaceutical effect effectively. More efforts are required to analyze the relationship among preparation methods, particle nanostructures and pharmaceutical properties in virtue of quality by design approach, and further promote the scale-up production and clinical application of zein NPs.

Solid multicomponent systems (SMS) are gaining an increasingly important role in the pharmaceutical industry, to improve the physicochemical properties of active pharmaceutical ingredients (APIs). In recent years, various processes have been employed for SMS manufacturing. Control of the particle solid-state properties, such as size, morphology, and crystal form is required to optimize the SMS formulation. By utilizing the unique and tunable properties of supercritical fluids, supercritical anti-solvent (SAS) process holds great promise for the manipulation of the solid-state properties of APIs. The SAS techniques have been developed from batch to continuous mode. Their applications in SMS preparation are summarized in this review. Many pharmaceutical co-crystals and solid dispersions have been successfully produced via the SAS process, where the solid-state properties of APIs can be well designed by controlling the operating parameters. The underlying mechanisms on the manipulation of solid-state properties are discussed, with the help of on-line monitoring and computational techniques. With continuous researching, SAS process will give a large contribution to the scalable and continuous manufacturing of desired SMS in the near future.

Quorum sensing (QS) plays an essential role in virulence factor production, biofilm formation, and antimicrobial resistance. As a potent QS inhibitor, hordenine can inhibit both QS and biofilm formation in Pseudomonas aeruginosa and Serratia marcescens. In this work, we tested the QS inhibitory potential of 27 hordenine analogs against QS and biofilm formation in P. aeruginosa and S. marcescens. Among the tested analogs, seven (12, 28, 27, 26, 2, 23, and 7) exhibited strong QS inhibitory activity against P. aeruginosa, five of which (12, 28, 27, 26, and 2) showed better inhibitory activity than hordenine. In addition, seven analogs (28, 12, 23, 7, 26, 2, and 27) exhibited better biofilm inhibition against P. aeruginosa than hordenine. Four analogs (7, 28, 2, and 12) showed QS inhibitory activity against S. marcescens, two of which (7 and 28) demonstrated better inhibitory activity than hordenine. Furthermore, analog 7 showed similar biofilm inhibition against S. marcescens as hordenine. Structure-activity relationship (SAR) analysis indicated that the inhibitory activities of the analogs were related to four factors, i.e., carbon chain length, presence or absence of an α,β-C <!-- PBM data was replaced with SVG by xgml2pxml: 000000000000 000000000000 000000000000 111111111111 000000000000 111111111111 000000000000 000000000000 000000000000 --> Created by potrace 1.16, written by Peter Selinger 2001-2019 C bond, amino group with/without lipophilic group, such as methyl group, and hydroxyl group in benzene ring.

The objective of this work is to formulate a zein-based nanocomposite for the delivery of natural polyphenols. A proprietary atomizing/antisolvent precipitation (AAP) process was used to prepare carboxymethyl chitosan (CMC)-coated zein/soy lecithin (SL) nanoparticles (ZLC NPs). At a suitable mass ratio of zein/SL/CMC (100 : 30 : 30), ZLC NPs with desirable redispersibility and physicochemical stability were successfully fabricated. After that, resveratrol (Res) as the representative natural polyphenol was encapsulated in ZLC NPs. The optimized Res/ZLC NPs exhibited a spherical morphology, small size (259.43 ± 2.47 nm), large zeta potential (−47.7 ± 0.66 mV), and high encapsulation efficiency (91.32 ± 4.01%) and loading capacity (5.27 ± 0.35%). Further characterization indicated that Res was encapsulated in the hydrophobic core of the ZLC matrix in an amorphous state. Compared to free Res, Res/ZLC NPs showed a 2.55-fold increase in the Res dissolution rate, a 2.27-fold increase in bioaccessibility, and a 1.69-fold increase in ABTS˙⁺ scavenging activity. Also, Res/ZLC NPs showed a higher Res retention rate (>68.0%) than free Res (<35.0%) over 45 days of storage. Therefore, ZLC NPs have promising potential as vehicles for natural polyphenols.