Improved solubility and pharmacokinetics of PEGylated liposomal honokiol and human plasma protein binding ability of honokiol
Improved solubility and pharmacokinetics of PEGylated liposomal honokiol and human plasma protein binding ability of honokiol
复制标题
改善聚乙二醇化和厚朴酚脂质体的溶解度和药代动力学以及和厚朴酚的人血浆蛋白结合能力
DOI：
10.1016/j.ijpharm.2011.03.003
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发表时间：
2011-05-30
影响因子：
5.8
通讯作者：
Chen, Li-Juan
中科院分区：
文献类型：
--
作者：
Wang, Xian-Huo;Cai, Lu-Lu;Chen, Li-Juan
PEGylated liposomal honokiol had been developed with the purpose of improving the solubility and pharmacokinetics compared with free honokiol. Human plasma protein binding ability of honokiol was also investigated. PEGylated liposomal honokiol was prepared by thin film evaporation-sonication method. Its mean particle size was 98.68 nm, mean zeta potential was -20.6 mV and encapsulation efficiency were 87.68 +/- 1.56%. The pharmacokinetics of PEGylated liposomal honokiol was studied after intravenous administration in Balb/c mice. There were significant differences of parameters T-1/2 beta and AUC(0 ->infinity) between them and liposome lengthened T-1/2 beta and AUC(0 ->infinity) values. The mean T-1/2 beta value of PEGylated liposomal honokiol and free honokiol were 26.09 min and 13.46 min, respectively. The AUC(0 ->infinity) ratio of PEGylated liposomal honokiol to free honokiol was about 1.85-fold (219.24 mu g/mL min/118.68 mu g/mL min) (P = 0.000). Examination of protein binding ability showed that honokiol with 0.5, 8.0 and 20 mu g/mL concentrations in human plasma achieved the percent of bound between 60% and 65%. The results suggested that PEGylated liposomal honokiol improved the solubility, increased the drug concentration in plasma, and withstanded the clearance. Besides, the percent of protein bound of honokiol in human plasma was between 60% and 65%. (C) 2011 Elsevier B.V. All rights reserved.
