Drug development often relies on high-throughput cell-based screening of large compound libraries. However, the lack of miniaturized and parallelized methodologies in chemistry as well as strict separation and incompatibility of the synthesis of bioactive compounds from their biological screenings makes this process expensive and inefficient. Here, we demonstrate an on-chip platform that combines solution-based synthesis of compound libraries with high-throughput biological screenings (chemBIOS). The chemBIOS platform is compatible with both organic solvents required for the synthesis and aqueous solutions necessary for biological screenings. We use the chemBIOS platform to perform 75 parallel, three-component reactions to synthesize a library of lipidoids, followed by characterization via MALDI-MS, on-chip formation of lipoplexes, and on-chip cell screening. The entire process from the library synthesis to cell screening takes only 3 days and about 1 mL of total solutions, demonstrating the potential of the chemBIOS technology to increase efficiency and accelerate screenings and drug development.

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Light‐based microfabrication techniques constitute an indispensable approach to fabricate tissue assemblies, benefiting from noncontact spatially and temporarily controlled manipulation of soft matter. Light‐triggered degradation of soft materials, such as hydrogels, is important in tissue engineering, bioprinting, and related fields. The photoresponsiveness of hydrogels is generally not intrinsic and requires complex synthetic procedures wherein photoresponsive crosslinking groups are incorporated into the hydrogel. This paper demonstrates a novel biocompatible and inherently photodegradable poly(ethylene glycol) methacrylate (PEGMA)‐based gelatin‐methacryloyl (GelMA)‐containing hydrogel that can be used to culture cells in 3D for at least 14 d. These gels are conveniently and quickly degraded via UV irradiation for 10 min to produce structured hydrogels of various geometries, sizes, and free‐standing cell‐laden hydrogel particles. These structures can be flexibly produced on demand. In particular, photodegradation can be temporarily delayed from photopolymerization, offering an alternative to hydrogel array production via photopolymerization with a photomask. The paper investigates the influences of hydrogel composition and swelling liquid on both its photodegradability and biocompatibility.

Stimuli‐responsive materials find wide applications in different biological and medical settings. Traditionally, stimuli‐responsive materials are synthesized and evaluated individually one‐by‐one. The drawback of this approach is the scarceness of possible combinations that can be practically tested for the purpose of saving time, consumables, and manpower. High‐throughput methods are therefore important to accelerate the discovery of stimuli‐responsive materials and to screen for biological interactions of interest in parallel. The objective of this article is to provide an overview of the successful employment of combinatorial high‐throughput synthesis and screening of stimuli‐responsive materials. In particular, these include thermoresponsive and hydroresponsive materials. Advantages of a combinatorial approach as well as of utilizing high‐throughput methodologies in the development of stimuli‐responsive materials are reviewed. Possible evolution trends of stimuli‐responsive materials, advanced by high‐throughput methodologies, are discussed.