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.
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Acknowledgments
This work was financially supported of by the National Natural Science Foundation of China (81101678), the Key Program of the Scientific Research Foundation of the Education Department of Sichuan Province (11ZZ024; 12ZZ020; 12ZB066), the Scientific Research Foundation of the Administration of Traditional Chinese of Sichuan Province (2012-F-026) and the Key Program of the Scientific Research Foundation of Bureau of Science and Technology of Luzhou City (2011-S-32(1/4)) and Produce-learn-research Projects of Luzhou medical college (2012CXY-01).
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All authors report no conflicts of interest. These authors alone are responsible for the content and writing of the paper.
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Wei, Y., Xue, Z., Ye, Y. et al. Paclitaxel targeting to lungs by way of liposomes prepared by the effervescent dispersion technique. Arch. Pharm. Res. 37, 728–737 (2014). https://doi.org/10.1007/s12272-013-0181-8
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DOI: https://doi.org/10.1007/s12272-013-0181-8