Anthocyanins are a class of dietary polyphenols that exhibit technological and bioactive-relevant properties. C3G is absorbed in its unmodified molecular form in the upper digestive tract, goes through the extended first-passage metabolism and its metabolites enter the bloodstream. The C3G metabolites possess health benefits such as antioxidant, cardio-protective, anti-inflammatory, neuroprotective, anti-cancer, anti-diabetic, and anti-thrombotic activities. However, the efficacy and distribution of C3G in the human body are restricted due to its low stability and bioaccessibility. Inspiringly, the lipid-, polysaccharide-, protein-, and nanocapsule-associated conjugates have achieved targeted delivery with enhanced bioaccessibility and controlled release. In this review, the absorption and transportation modes, decomposition and metabolism processes, functional activity mechanisms, and improved methods for enhancing the bioavailability of C3G are summarized. Moreover, the aspects of the gut microbiota regulation, C3G-mediated cytoprotection and different biocompatible materials applications are briefly discussed.