title: Paclitaxel targeting to lungs by way of liposomes prepared by the effervescent dispersion technique.
abstract: In order to develop a novel lung targeting drug delivery system (LTDDS) with large-sized liposomes containing paclitaxel (PTX), the liposomes composed of PTX, phosopholipon 90H and tween-80 were prepared by the effervescent dispersion technique with optimal formulation composition. The liposomes were found to be relatively uniform in particle size (8.166 ± 0.459 μm) with a negative zeta-potential (-12.45 ± 1.34 mv), and high entrapment efficiency (92.20 ± 2.56 %). They kept stable for at least 3 months and exhibited a slow release behavior without any hemolysis reaction. Via intravenous administration in rabbits, the PTX liposomes presented a longer mean residence time and elimination half-life, and a much larger area under the plasma drug concentration-time curve compared with its injection; meanwhile, the liposomes altered its biodistribution and exhibited a significant lung targeting characteristic. For example, the relative intake rate (Re) and the ratio of peak concentration (Ce) of lung were 14.87 and 26.44, respectively. Compared with heart, liver, spleen and kidney, the ratios of targeting efficacy (Te)liposomes to (Te)injection of lung were increased by a factor of 20.08, 11.10, 6.97 and 14.41, respectively. To sum up, the liposome could be a promising drug carrier for PTX as LTDDS for lung cancer treatment.
authors.affiliation: Department of Pharmaceutical Sciences, School of Pharmacy, Luzhou Medical College, No. 3-319, Zhongshan Road, Jiangyang District, Luzhou, 646000, Sichuan, China.
authors.forename: Yumeng
authors.initials: Y
authors.lastname: Wei
authors.forename: Zhengkai
authors.initials: Z
authors.lastname: Xue
authors.forename: Yun
authors.initials: Y
authors.lastname: Ye
authors.forename: Yu
authors.initials: Y
authors.lastname: Huang
authors.forename: Ling
authors.initials: L
authors.lastname: Zhao
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000138:chemical synthesis*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004337:Drug Carriers / Q000008:administration & dosage / Q000138:chemical synthesis*; D016503:Drug Delivery Systems / Q000379:methods*; D008081:Liposomes; D008168:Lung / Q000187:drug effects* / Q000378:metabolism; D017239:Paclitaxel / Q000008:administration & dosage / Q000138:chemical synthesis*; D011817:Rabbits; D011897:Random Allocation; D014018:Tissue Distribution / Q000187:drug effects / Q000502:physiology
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D008081:Liposomes; D017239:Paclitaxel