Oral drug delivery is a dynamic research area, yet associated with multiple issues in its using: enzymatic degradation, hydrolysis, low permeability of intestinal epithelium. The review presents a research papers analysis on the development of targeted drug delivery using a biodegradable polymer chitosan. Chitosan application, singly or in composites, is suitable for various drug delivery systems. Upon oral delivery, chitosan serves as a mucoadhesive polymer with controlled and targeted release. During the last five years, various approaches to the delivery of insulin and other drugs had been reported in literature. The main technological strategy for insulin delivery was its protection against intestinal pH, as well as increasing of permeability via transcellular and/or paracellular pathways. It is observed that application of the biopolymer and its derivatives has a controlled absorption profile. In publications on the drugs delivery, most of the research is focused on development and modification of methods for their producing. According to the presented experimental data, there were obtained particles with well-defined spherical shapes and microparticles capacity of 85-97%. A number of research articles provide data on the chitosan application as a mucoadhesive coating for various nano- or microparticles. It was also noted that application of chitosan microparticles contributed to diminishing adverse side effects.