Design of N-acetylcysteine vesicles as a potential chemopreventive tool in lung cancer: Characterization, Tc-99 m radiolabeling and in vivo evaluation

Abstract

Lung cancer is a type of cancer which is characterized by high incidence and elevated mortality rate. In an attempt to counteract the carcinogens’ load and prevent the development of lung cancer especially in heavy smokers, chemoprevention has emerged as a promising strategy in this regard. Among the popular chemopreventive agents is N-acetyl cysteine (NAC), which prevents the progression of lung damage by virtue of its antioxidant and anti-inflammatory properties. In order to increase the amount of NAC reaching the lung following intravenous administration, the current work explored its formulation in transcutol-containing liposomes. The vesicles prepared using the ethanol injection method were characterized in vitro for their particle size, zeta potential, polydispersity, entrapment efficiency, storage stability, drug release, antioxidant and anti-inflammatory properties, safety and morphology. Their in vivo biodistribution was assessed in body organs after radiolabeling with technetium-99 m. Results showed that the transcutol-containing liposomes exhibited a particle size of 250 ± 17 nm, a zeta potential of −18.90 ± 2.30, entrapment efficiency 41 % ± 3.4, sustained release, and they preserved the antioxidant and anti-inflammatory properties of the encapsulated NAC. The biodistribution study delineated that NAC was deposited about three-fold higher in the lung when administered in transcutol-containing liposomes compared to the solution form. Therefore, it can be concluded that transcutol-containing liposomes is a promising lung-targeting modality for delivering NAC, which is worthy of further exploration with other drugs targeting pulmonary diseases.