State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
Int J Pharm. 2011 May 30;410(1-2):169-74. doi: 10.1016/j.ijpharm.2011.03.003. Epub 2011 Mar 21.
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(1/2β) and AUC(0→∞) between them and liposome lengthened T(1/2β) and AUC(0→∞) values. The mean T(1/2β) value of PEGylated liposomal honokiol and free honokiol were 26.09 min and 13.46 min, respectively. The AUC(0→∞) ratio of PEGylated liposomal honokiol to free honokiol was about 1.85-fold (219.24 μg/mL min/118.68 μg/mL min) (P=0.000). Examination of protein binding ability showed that honokiol with 0.5, 8.0 and 20 μg/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%.
PEG 化脂质体厚朴酚的研制目的是提高其与游离厚朴酚相比的溶解度和药代动力学特性。还研究了厚朴酚在人血浆中的蛋白结合能力。采用薄膜蒸发-超声法制备 PEG 化脂质体厚朴酚。其平均粒径为 98.68nm，平均 zeta 电位为-20.6mV，包封率为 87.68±1.56%。在 Balb/c 小鼠中静脉给药后研究了 PEG 化脂质体厚朴酚的药代动力学。与脂质体延长 T(1/2β)和 AUC(0→∞)值相比，它们之间的参数 T(1/2β)和 AUC(0→∞)有显著差异。PEG 化脂质体厚朴酚和游离厚朴酚的平均 T(1/2β)值分别为 26.09min 和 13.46min。PEG 化脂质体厚朴酚与游离厚朴酚的 AUC(0→∞)比值约为 1.85 倍(219.24μg/mL min/118.68μg/mL min)(P=0.000)。蛋白结合能力研究表明，人血浆中浓度为 0.5、8.0 和 20μg/mL 的厚朴酚达到了 60%65%的结合率。结果表明，PEG 化脂质体厚朴酚提高了溶解度，增加了血浆中的药物浓度，抵抗了清除。此外，厚朴酚在人血浆中的蛋白结合率在 60%65%之间。
