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Rosuvastatin (RSVS), an anti-lipidemic agent suggested for the treatment of airway remodeling in chronic obstructive pulmonary disease (COPD). It shows a pleiotropic effect on airway smooth muscles and inhibits proliferative activities of physiological mitogens. The aim of the present study was to develop and investigate the targeting potential of rosuvastatin (RSVS) to lung as loaded in nanostructured lipid carrier dry powder for inhalation (RNLC-DPI). RNLC dispersion was converted into respirable particle by lyophilization using 5% mannitol as cryoprotectant-carrier. Targeting efficiency of RNLC-DPI was evaluated in vitro for aerosol performance using 8-stage cascade impactor as well in vivo in Wistar rats for pulmokinetics. In vitro aerosol performance demonstrated mass median aerodynamic diameter of <3 μm with fine particle fraction of >90% at 60 L/min. Improved aerosol performance was observed for RNLC-DPI prepared using l-leucin as anti-static agent. Modified in vivo performance with higher Cmax (1.14-fold), improvement in t1/2 (5-fold) and 35-fold improvement in AUC0-∞ indicated significant improvement in bioavailability of RNLC-DPI. Lipidic nature and smaller size of particles helped in bypassing macrophage clearance leading to higher targeting factor. Thus, study demonstrated potential of RNLC-DPI for lung targeting and further for COPD treatment.