In Vitro and in Vivo Study of Two Types of Long-Circulating Solid Lipid Nanoparticles Containing Paclitaxel
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概要
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Paclitaxel (Taxol), a diterpenoid isolated from Taxus brevifolia, is effective against several murine tumors, and is one of the most exciting anticancer molecules currently available. Due to its low solubility in water, it is clinically administered with polyethoxylated castor oil (Cremophor EL), which causes serious side effects. Inclusion of paclitaxel in solid lipid nanoparticles (SLNs) has proved to be a good approach to eliminate the need for Cremophor EL and improve the drug's antitumor efficacy. This paper describes the development of two types of long-circulating SLNs as colloidal carriers for paclitaxel. SLNs are constituted mainly of bioacceptable and biodegradable lipids. In vitro release kinetics showed that the release was very slow, the release of paclitaxel from F_<68>-SLN is linear, and the release of paclitaxel from Brij78-SLN followed the Weibull equation. Pharmacokinetics was evaluated in KM mice after injection of paclitaxel formulated in Cremophor EL or in Brij78-SLN and F_<68>-SLN. Encapsulation of paclitaxel in both SLNs produced marked differences compared with the free drug pharmacokinetics. F_<68>-SLN and Brij78-SLN are long-circulating (t_<1/2>β, 10.06 and 4.88h, respectively) compared with paclitaxel injection (t<1/2>β, 1.36h)
- 公益社団法人日本薬学会の論文
- 2001-11-01
著者
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Zhang Q
Peking Univ. School Of Pharmaceutical Sci. Beijing Chn
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Zhang Qiang
Department of Hepatology, Capital University of Medical Science Affiliated Beijing You An Hospital
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Yang T‐z
Peking Univ. School Of Pharmaceutical Sci. Beijing Chn
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Yang Tian-zhi
Department Of Pharmaceutics Peking University School Of Pharmaceutical Sciences
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CHEN Da-Bing
Department of Pharmaceutics, Peking University, School of Pharmaceutical Sciences
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LU Wang-Liang
Department of Pharmaceutics, Peking University, School of Pharmaceutical Sciences
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Zhang Qiang
Department Of Cardiology Beijing Anzhen Hospital Capital Medical University
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Chen Da-bing
Department Of Pharmaceutics Peking University School Of Pharmaceutical Sciences
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Lu Wang-liang
Department Of Pharmaceutics Peking University School Of Pharmaceutical Sciences
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