There are several requirements for the safe and effective delivery of therapeutic agents for human use. Drug permeation to the normal regions of the body is the main drawback of conventional Drug delivery system. To avoid unwanted side effects of drug the approach like targeted drug delivery is preferred. In particular, carrier drug delivery system posses some structures which are attached the drug molecule for targeted delivery. Layer-by-Layer approach also offers a delivery of drug in a targeted fashion to avoid its unintentional effects on normal tissue. LbL self-assembly systems involve simple alternative adsorption of oppositely charged polyelectrolytes on core materials. Here, in this review we have discussed the latest findings from research into LbL systems, with special emphasis on drug delivery systems.