Many unique chemical compounds and nanomaterials are being developed, and each one requires a considerable range of in vitro and/or in vivo toxicity screening in order to evaluate their safety. The current methodology of in vitro toxicological screening on cells is based on well-plate assays that require time-consuming manual handling or expensive automation to gather enough meaningful toxicology data. Cost reduction; access to faster, more comprehensive toxicity data; and a robust platform capable of quantitative testing, will be essential in evaluating the safety of new chemicals and nanomaterials, and, at the same time, in securing the confidence of regulators and end-users. Microfluidic chips offer an alternative platform for toxicity screening that has the potential to transform both the rates and efficiency of nanomaterial testing, as reviewed here. The inherent advantages of microfluidic technologies offer high-throughput screening with small volumes of analytes, parallel analyses, and low-cost fabrication.