BACKGROUND Cellulose being the first abundant biopolymers in nature has many fascinating properties, including low-cost, good biodegradability, and excellent biocompatibility, which made cellulose a real potential material to create nano-drug delivery systems (nano-DDS). This review aims to present and discuss some remarkable recent advances on the drug delivery applications of cellulosebased prodrugs and nanoparticles. METHODS By searching the research literatures over last decade, a variety featured studies on cellulosebased nano-DDS were summarized and divided into prodrugs, prodrug nanoparticles, solid or derivative nanopartilces, amphiphilic copolymer nanoparticles, and polyelectrolyte complex nanoparticles. Various methods employed for the functionalization, pharmacodynamic actions and applications were described and discussed. RESULTS Many types of cellulose-based nano-DDS can ensure efficient encapsulation of various drugs and then overcome the free drug molecule shortcomings. Among all the method described, cellulosebased amphiphilic nanoparticles are most frequently used. These formulations have the higher drug loading capability, a simple and flexible way to achieve multi-functional. Apart from hydrophilic or hydrophobic modification, cellulose or its derivatives can form nanoparticles with different small molecules and macromolecules, leading to a large spectrum of cellulose-based nano-DDS and providing some unexpected advantages. CONCLUSIONS Thorough physicochemical characterization and profound understanding of interactions of the cellulose-based nano-DDS with cells and tissues is indispensable. Moreover, studies toward technics parameter optimization and scale up from the laboratory to production level should be undertaken. The development of intravenous and orally applicable cellulose-based nano-DDS will be an important research area, and these systems will have more commercial status in the market.