The present work is devoted to the preparation of novel self-assembled nanoparticles by conjugating different bioactive compounds. CS–PLA is blended with polyethylene glycol (PEG) and gelatin (G) by emulsion solvent evaporation technique. Theemulsion solvent evaporation method is the widely used one among various encapsulation techniques. Various drugs are successfully retained within particles prepared by this method. Manytypes of pharmaceuticals and biopharmaceuticals with different physico-chemical properties have been formulated into particles by emulsion method. The emulsion method has been considered better since the method is relatively simple, convenient in controlling process parameters, and has the ability to produce with simple instrument. The advantages of the bioactivityof CS–PLA–PEG–G matrix along with the attractive properties of matrix have been presented. The developed compositenanoparticles have been characterized and evaluated for in vitrostudies, cell inhibition studies and instrumental characteristics.The developed composite nanoparticle is a soft matrix materialand can be utilized for tuberculosis treatment and drug deliv-ery. The results obtained have been discussed in detail in this paper.