A lung-targeting liposomal docetaxel was developed to improve therapeutic index and to reduce side effects. Docetaxel proliposomes composed of docetaxel/Tween-80/Phospholipon 90H/cholesterol/citric acid at molar ratio of 0.18:0.09:3.78:3.78:91.17 were prepared by solid dispersion technique, and then were hydrated with NaHCO₃ solution to obtain docetaxel liposomes by effervescent technique. The stability of proliposomes containing docetaxel, characterization and evaluation of lung-targeting effect of docetaxel liposomes in rabbit were studied. Docetaxel proliposomes were stable at 6 ± 2°C for at least 12 months. The particle size, zeta-potential, and entrapment efficiency of the resulted liposomes were 1011 ± 22 nm, −23.7 ± 0.26 mv, and 90.12 ± 0.36%, respectively. As far as the targeting parameters are concerned, the relative intake rate (R_e) and the ratio of peak concentration (C_e) of lung were 28.91 and 74.28, respectively. Compared with liver, spleen, and kidney, the ratios of targeting efficacy (T_e)_liposomes to (T_e)_injection of lung were increased by a factor of 3.16, 23.00, and 27.83, respectively. In conclusion, the negatively charged docetaxel liposomes with diameter of about 1 µm described in this study have favorable lung-targeting effect and are a promising lung-targeting carrier.

Herein, a series of Ru(arene) complexes, [(η⁶-p-cymene)Ru(bpy)(X)]²⁺ complexes (bpy = 2,2′-bipyridine, X = pyridine, diazine, pyrimidine, and pyrazine) was synthesized, and its photochemical and photobiological properties were carefully compared. It has been found that the basicity of the monodentate ligand has a significant impact on the ligand photodissociation and photobinding DNA abilities of the complexes. A decrease in the basicity of the monodentate ligand leads to a decrease in the electron donating ability of the monodentate ligand; this enhances the photoinduced DNA covalent binding capabilities of 1–4. The CCK8 assay suggests that 4 exhibits the most potent phototoxicity against human lung carcinoma A549 cells among the examined complexes. By changing the basicity of the monodentate ligand, the photobinding abilities increases from the complexes 1 to 4; this provides a good strategy for the development of more efficient metallodrugs with photoactivity.

An efficient and facile synthesis for 2-aminobenzimidazoles and 2-aminobenzoxazoles has been reported. Thioureas prepared from the reaction of o-phenylenediamines or 2-aminophenols and isothiocyanate derivatives, underwent desulfurization reaction smoothly under mild conditions in the presence of Cu(OAc)₂, and afforded a variety of N-heterocyclic compounds in moderate to good yields. Graphical Abstract