The Second Affiliated Hospital of Guangzhou Medical University, Guangzhou, People's Republic of China.
Int J Nanomedicine. 2013;8:933-40. doi: 10.2147/IJN.S39349. Epub 2013 Mar 4.
Puerarin has multiple pharmacological effects and is widely prescribed for patients with cardiovascular diseases including hypertension, cerebral ischemia, myocardial ischemia, diabetes mellitus, and arteriosclerosis. We have successfully prepared puerarin-loaded solid lipid nanoparticles (Pue-SLNs) for oral administration. Pue-SLNs are prepared using monostearin, soya lecithin, and poloxamer 188. SLNs may alter the course of puerarin absorption predominantly to and through lymphatic routes and regions, presumably following a transcellular path of lipid absorption, especially by enterocytes and polar epithelial cells of the intestine. The alteration of absorption might influence the metabolic profile of puerarin when incorporated into SLNs. In the present study, we investigated the metabolic profile of puerarin in rat plasma and urine using rapid resolution liquid chromatography-tandem mass spectrometry after a single-dose intragastric administration of Pue-SLNs in comparison with puerarin suspension. Two glucuronidated metabolites of puerarin, puerarin-4'-O-glucuronide and puerarin-7-O-glucuronide, were detected in rat plasma and urine after intragastric administration of Pue-SLNs, with the latter acting as the major metabolite. Similar results were found in rat plasma and urine after intragastric administration of puerarin suspension. The results suggest that incorporation of puerarin into SLNs does not change either the position of glucuronidation or the metabolic pathway of puerarin in rats.
葛根素具有多种药理作用，广泛用于治疗高血压、脑缺血、心肌缺血、糖尿病和动脉硬化等心血管疾病患者。我们已经成功地制备了葛根素负载的固体脂质纳米粒（Pue-SLNs）用于口服给药。Pue-SLNs 是使用单硬脂酸甘油酯、大豆卵磷脂和泊洛沙姆 188 制备的。SLNs 可能会改变葛根素的吸收过程，主要通过淋巴途径和区域，推测是通过脂质吸收的细胞旁路，特别是通过肠上皮细胞和极性上皮细胞。当葛根素被包裹在 SLNs 中时，吸收的改变可能会影响其代谢谱。在本研究中，我们通过快速分辨液相色谱-串联质谱法在大鼠血浆和尿液中研究了单次灌胃 Pue-SLNs 后葛根素的代谢谱，与葛根素混悬液进行了比较。在大鼠灌胃 Pue-SLNs 后，在血浆和尿液中检测到两种葛根素的葡萄糖醛酸代谢物，葛根素-4'-O-葡萄糖醛酸苷和葛根素-7-O-葡萄糖醛酸苷，后者为主要代谢物。在大鼠灌胃葛根素混悬液后也在血浆和尿液中发现了类似的结果。结果表明，将葛根素包裹在 SLNs 中不会改变其葡萄糖醛酸化的位置或葛根素在大鼠体内的代谢途径。
