A vast number of biologically active compounds await efficient delivery to become therapeutic agents. Lipidation has been demonstrated to be a convenient and useful approach to improve the stability and transport across biological membranes of potential drug molecules. The lipid core peptide (LCP) system has emerged as a promising lipidation tool because of its versatile features. This review discusses the progress in the development of the LCP system to improve cell permeability of nucleotides, physicochemical properties of potential drugs, and vaccine immunogenicity. Emphasis was put on the application of the LCP system to deliver antigens for the prevention of group A streptococcus infection, novel techniques of conjugation of target molecules to the LCP, and new alterations of the LCP system itself.