Targeted drug delivery science are rapidly gaining importance, due to the offering of controlled delivery of biologically active agents at specific cells. This strategy is based on the chemical modification of the nanocarriers surfaces avoiding the interaction with healthy tissue. The functionalization of stealth cationic liposomes with cyclic RGD peptide (cRGDfK) is a possible way to enhance the nanocarriers internalization in the cancer cells, because these peptides are able to interact selectively with cellular receptors expressed in cancer cells. However, for the clinical application of these drug delivery systems, effective strategies to develop these nanocarriers are necessary. To overcome this challenge, Microfluidics has been applied. Microfluidics offers unique characteristics to control the mixing of liquids under laminar flow. Its use to promote the assembly of lipids to form the liposomes under controlled conditions. Therefore, the aim of this research project was to develop stealth cationic liposomes functionalized with cRGDfK peptides in a microfluidic device. For this purpose, two crucial steps were followed: (i) phospholipids were chemically modified with cRGDfK with 30% of yield and (ii) stealth cationic liposomes were produced by the lipids (EPC/DOTAP/DOPE/DSPE-PEG) and it exhibited convenient physicochemical properties, as hydrodynamic diameter of 122.22 nm and low polydispersity index (PDI) (PDI ≤ 0.2).