Evaluation of long-circulating nanoparticles using biodegradable ABA triblock copolymers containing of poly(l-lactic acid) A-blocks attached to central poly(oxyethylene) B-blocks in vivo |
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| Institution: | 1. Pharmaceutical Research and Development Center, Kanebo Ltd, 5-9 Tomobuchi-cho, 1-chome, Miyakojimaku, Osaka 534-8666, Japan;2. Research and Development Center, Kanebo Ltd, 5-9 Tomobuchi-cho, 1-chome, Miyakojimaku, Osaka 534-8666, Japan;1. King Abdullah Institute for Nanotechnology, King Saud University, Riyadh, Saudi Arabia;2. Department of Medical Physics and Astronomy, College of Science, King Saud University, Riyadh, Saudi Arabia;3. Nanomedicine Research Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia;4. Department of Biochemistry, College of Science, King Saud University, Riyadh, Saudi Arabia;1. Department of Life Sciences and Biotechnology, University of Ferrara, I-44121 Ferrara, Italy;2. BIMF/Soft Matter Electronmicroscopy, University of Bayreuth, Germany;3. Department of Life and Environmental Sciences and CNISM, Università Politecnica delle Marche, I-60100 Ancona, Italy;1. Department of Chemistry, Faculty of Sciences, University of Guilan, P.O. Box 41335-1914, Rasht, Iran;2. Department of Chemistry, Islamic Azad University, Rasht Branch, Iran;1. College of Life Sciences and Agricultural Engineering, Nanyang Normal University, Nanyang, 473061, PR China;2. Collaborative Innovation Center of Water Security for the Water Source Region of the Mid-line of the South-to-North Diversion Project of Henan Province, Nanyang Normal University, Nanyang, 473061, PR China;1. Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt;2. Department of Pharmaceutics, Faculty of Pharmacy, University of Tabuk, Tabuk, Saudi Arabia |
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| Abstract: | The nanoparticles (mean diameter 152–377 nm) consisting of the ABA triblock copolymers (Mw 29 000–147 000) containing poly(l-lactic acid) (PLA) A-blocks attached to central poly(oxyethylene) (PEG) B-blocks (PEG Mw 6600, 20 000) (PLA-PEG-PLA) were prepared, and the effects of the polymer characteristics on the pharmacokinetics of the nanoparticles and the biodistribution of the nanoparticles were studied. Progesterone was used as a model drug. We could make the long-circulating nanoparticles using the triblock copolymer. The degree of burst in early phase, which was estimated by the Co values (Progesterone concentration at time 0) and the circulating-time were affected by the total Mw, the PEG content, the PEG Mw and the Mw/Mn (Mn: where Mn is the number average molecular weight) ratio. The purification of the polymer was an important factor for the control of the burst. These triblock copolymer nanoparticles induced reduction in the liver and spleen uptake of the nonoparticles. These phenomena are probably explained by the avoidence of adsorption of opsonin to the particles as a result of the orientation of PEG on the surface of the particles. |
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