NON-SMALL CELL LUNG CANCER IS THE LEADING CAUSE OF CANCER-RELATED DEATHS WORLDWIDE. GEMCITABINE (GEM) IS AN EFFECTIVE CHEMOTHERAPEUTIC AGENT FOR TREATING THIS AND OTHER CANCERS. HOWEVER, THE NON-SPECIFIC TOXICITY OF GEM HAS PROMPTED A SEARCH FOR NOVEL CHEMOTHERAPEUTIC STRATEGIES. THE MAIN OBJECTIVE OF THIS WORK WAS TO OBTAIN MICROENCAPSULATED SYSTEMS LOADED WITH GEM, NANOMAGNETITE AND MICROZEOLITE IN CHITOSAN MATRIX BY SPRAY DRYING IN ORDER TO CHARACTERISE THEM AND TEST THEIR ACTIVITY ON LUNG CANCER CELLS. CAPSULE CHARACTERIZATIONS SHOWED SPHERICAL NANO-IN-MICROPARTICLES MEASURING 1.91 ?M ON AVERAGE WITH A ROUGH SURFACE AND CHARACTERISTIC SIGNS OF MATERIAL INTERACTION BY TEM AND FESEM-EDS. THE INTERACTION AND LOADING OF NANO- AND MICROPARTICLES IN THE CHITOSAN MATRIX WAS EVIDENCED BY FT-IR. % E.E. WERE OBTAINED. GREATER THAN 99.00 % IN ALL MICROENCAPSULES AND THE RELEASE OF THE GEM WAS SLOW AND CONTROLLED AT PH 7.4 AND 5.0 UP TO 24 H. MAGNETIC MOBILITY WAS DEPENDENT ON THE CONCENTRATION OF NANOMAGNETITE IN THE FORMULATION AND CELL VIABILITY WAS LOWER THAN THE PURE GEM CONTROL (1 MG/ML) IN BOTH CELL LINES (A549 AND H1299). NANO-IN-MICROENCAPSULATED SYSTEMS SHOW GREAT POTENTIAL FOR INHALED DELIVERY OF GEMS FOR THE TREATMENT OF NON-SMALL CELL LUNG CANCER.