Preparation ， <> in Vitro Release and Pharmacokinetics of Paclitaxel Lipid Nanoparticles for Intravenous Injection

LIU Dn;LI Shu-in;O Jie;GUO Zhi-fu;LI Ming-hui;YU N

Chinese Pharmaceutical Journal ›› 2009, Vol. 44 ›› Issue (17) : 1320-1326.

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Chinese Pharmaceutical Journal ›› 2009, Vol. 44 ›› Issue (17) : 1320-1326.
Article

Preparation ， <> in Vitro Release and Pharmacokinetics of Paclitaxel Lipid Nanoparticles for Intravenous Injection

  • LIU Dan ， LI Shu-bin* ， BAO Jie ， GUO Zhi-fu ， LI Ming-hui ， YU Na
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Abstract

OBJECTIVE To prepare paclitaxel lipid nanoparticles for intravenous injection and investigate its release characteristics in vitro and its pharmacokinetics in rats. METHODS Paclitaxel lipid nanoparticles for intravenous injection were prepared by high-pressure homogenization and lyophilization. The shape of lipid nanoparticles，particles size，drug-loading capability were evaluated．Entrapment efficiency was determined by filtration-centrifugal ultrafiltration．Stability and hemolysis reaction were evaluated. The in vitro release and its pharmacokinetics in rats were investigated by comparison with paclitaxel injection at the same time．RESULTS The mean particle size，entrapment efficiency and drug-loading capability were 25.6 nm, （99.55±0.25）% and（1.37±0.78）%, respectively. Paclitaxel lipid nanoparticles after being diluted by 5％ glucose solution and 0.9% NaCl solution was stable within 8 h. It had no hemolysis reaction. The in vitro cumulative released in 0.8 mol·L-1 sodium salicylate solution reached about 99.8% and 99.9% in 24 h. The profile was described by first-class equation. The mean residence time and the area under the curve of concentration versus time from zero to the last time point of paclitaxel injection and lipid nanoparticles were 1.10 and 1.85 h, and 6.78 and 33.6 mg·h·L-1，respectively．CONCLUSION Paclitaxel lipid nanoparticles was prepared by high-pressure homogenization and lyophilization. It showed high drug-loading capability and high encapsulation efficiency. And lipid nanoparticles showed sustained release in vitro compared with injection.

Key words

paclitaxel lipid nanoparticles / entrapment efficiency / in vitro release / pharmacokinetics

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LIU Dn;LI Shu-in;O Jie;GUO Zhi-fu;LI Ming-hui;YU N . Preparation ， <> in Vitro Release and Pharmacokinetics of Paclitaxel Lipid Nanoparticles for Intravenous Injection[J]. Chinese Pharmaceutical Journal, 2009, 44(17): 1320-1326

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（ 收稿日期 ： 2009-04-07 ）


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