Novel drug delivery systems have previously never been used in the formulation of any crude unfractionated traditional Chinese medicine. In the present study, a multi-unit drug delivery system (MUDDS) for a Chinese medicine Niuhuang Xingxiao Wan (NXW) was prepared using micro/nanotechnologies to enhance the bioavailability and efficacy. NXW was formulated into four units, that is, realgar, frankincense and myrrh oil (FMO), musk, and bezoar. The four units were processed using the wet ball milling, high-pressure homogenization, liquid nitrogen freezing-ultracentrifugation trituration, and dry grinding methods, respectively. After formulation, the four independent units prepared were encapsulated together to obtain the final NXW-MUDDS. Pharmacokinetic studies showed that the area under the plasma concentration-time curve (AUC), terminal half-life (T1/2), and time to reach the peak plasma concentration (Tmax) following administration of NXW-MUDDS were 5.21, 1.96, and 1.99 times higher, respectively, than that of NXW. The in vivo antitumor activity assay showed that the efficacy of NXW-MUDDS was significantly higher (P<0.05) than that of NXW. Collectively, these results reveal the feasibility of applying micro/nanotechnologies in formulating Chinese medicines.