Liao Dehua, Liu Xinyi, Dai Wei, Tang Tiantian, Ou Ge, Zhang Kai, Han Meng, Kang Rongrong, Yang Sufang, Xiang Daxiong
Department of Pharmacy, The Second Xiangya Hospital of Central South University , Changsha , China .
Drug Deliv. 2015;22(4):516-21. doi: 10.3109/10717544.2013.879398. Epub 2014 Jan 27.
The aim of this research was to increase the oral bioavailability of puerarin by N-trimethyl chitosan-modified microemulsions (TMC-MEs) loaded with puerarin. Different concentrations of TMC-modified microemulsions were prepared in our study, and then evaluated for particle size, zeta potential, morphological observation and changes of the microenvironment polarity of inner oil core. It was shown that the zeta potential of the microemulsion was increased with the increasing concentration of TMC, and the peak value was achieved when the concentration of TMC was 3.0 mg/mL. The enhancement of the ratio of I(1)/I(3) (the ratio between the first band and the third band of the emission fluorescence spectrum of pyrene, I(1) = 373 nm, I(3) = 384 nm) indicated that polarity of the inner core of TMC-MEs was increased with the addition of the modifier. Pharmacokinetic studies demonstrated that after oral administration of puerarin N-trimethyl chitosan (TMC)-modified microemulsions (PUE-TMEs) and puerarin microemulsions (PUE-MEs) to rats at a dose of 100 mg/kg, relative bioavailability was enhanced about 6.8- and 1.2-fold, respectively, compared to puerarin suspension (PUE-SUS) as control. It indicated that the TMC-MEs could be used as an effective formulation for enhancing the oral bioavailability of puerarin.
本研究的目的是通过负载葛根素的N-三甲基壳聚糖修饰微乳（TMC-MEs）提高葛根素的口服生物利用度。本研究制备了不同浓度的TMC修饰微乳，然后对其粒径、ζ电位、形态观察以及内部油核微环境极性变化进行了评估。结果表明，微乳的ζ电位随TMC浓度的增加而升高，当TMC浓度为3.0 mg/mL时达到峰值。芘发射荧光光谱第一峰与第三峰的比值I(1)/I(3)（I(1) = 373 nm，I(3) = 384 nm）增大，表明添加改性剂后TMC-MEs内核的极性增加。药代动力学研究表明，以100 mg/kg的剂量给大鼠口服葛根素N-三甲基壳聚糖（TMC）修饰微乳（PUE-TMEs）和葛根素微乳（PUE-MEs）后，与作为对照的葛根素混悬液（PUE-SUS）相比，相对生物利用度分别提高了约6.8倍和1.2倍。这表明TMC-MEs可作为提高葛根素口服生物利用度的有效制剂。
