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| Pharmacokinetics of rotenone loaded nanostructured lipid carriers and its modifiers in rats |
| LI Ya-nan, MAO Quan-gao |
| (Department of Pharmacy, the People′s Hospital of Rugao, Rugao Jiangsu 226500, China) |
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Abstract ［Abstract］Objective： To observe pharmacokinetical characterization of rotenone loaded nanostructured lipid carriers (RNLC) modified by polyethylene glycol(PEG) in rats. Methods：One hundred and twentythree SD rats were used in the serial tests. Twentyone rats were divided into three groups, each group were injected with rotenone solution, RNLC and PEG modified rotenone nanostructured lipid carriers (PEGRNLC), respectively. Blood were collected at different time points.The remaining 102 SD rats were randomly divided into 17 groups, 5 groups received subcutaneous injection of rotenone solution, 12 groups were given subcutaneous injection of RNLC(6 groups) and PEGRNLC(6 groups), respectively. Tissues of interests were harvested at different time points. HPLC was used to determine and the distribution of rotenone in blood and tissues of different groups were evaluated. Results：The AUC of rotenone solution in tissues from high to low in order was kidneys, liver, brain, spleen, heart and lung. Tmax of rotenone solution was 4 h in blood, while it was 8 h of RNLC and PEGRNLC. The AUC of RNLC and PEGRNLC was 35.99 and 42.03 times higher than rotenone solution respectively. The AUC of RNLC in tissues from high to low in order was brain, liver, kidneys, heart spleen, and lung. The contention of PEGRNLC in tissues was significantly increased in brain (substantia nigra and striatum) and decreased in the peripheral issues. Conclusion：PEGRNLC could increase the contention of rotenone in the striatum and substantia nigra, which further enhanced brain targeting of RNLC.
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Received: 20 April 2016
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2016, Vol. 26 
