Department of Pharmacy, Anhui University of Chinese Medicine , Hefei , China.
Ministry of Education, Key Laboratory of Xin'An Medicine , Hefei , China.
Pharm Dev Technol. 2019 Nov;24(9):1155-1163. doi: 10.1080/10837450.2019.1646757. Epub 2019 Aug 8.
Lymphatic formations that effectively eradicate the virus in the lymphatic system will be therapeutically advantagous in hepatitis B virus (HBV) infection. Lipid-based formulation is often used to deliver drug via the lymphatic system. Baicalin nanoemulsion may be a promising drug delivery system for improved treatment of HBV infection. This study aimed to prepare, characterize, and evaluate a lipid-based nanoemulsion containing baicalin for lymphatic system absorption. The presence of a nanoemulsion region was studied by pseudoternary phase diagrams. The physicochemical properties of a baicalin-loaded nanoemulsion were investigated. The oral bioavailability of the baicalin-loaded nanoemulsion was compared to that of a baicalin suspension. A chylomicron flow blocking model was used to examine the extent of lymphatic uptake. The lymph node distribution of baicalin was measured to investigate the lymphatic transport ability of the nanoemulsion compared to the suspension. Compared to the baicalin suspension, the AUC and C values of the baicalin nanoemulsion were increased by 10.5-fold and 3.12-fold, respectively. Compared with the saline-treated rats that were orally administered the baicalin nanoemulsion, the AUC and C values of the nanoemulsion for the rats pretreated with cycloheximide were reduced from 23.076 ± 1.244 mg/L h to 9.236 ± 0.940 mg/L h and from 3.010 ± 0.119 mg/L to 1.567 ± 0.220 mg/L, respectively. In comparing baicalin in W/O nanoemulsion with suspension, the C value was found to be 11.5-fold higher in the lymph nodes of the rats treated with the nanoemulsion. The results indicated that a baicalin-loaded W/O nanoemulsion may be a promising drug delivery system for the treatment of chronic hepatitis B.
在乙型肝炎病毒 (HBV) 感染中，能有效清除淋巴系统中病毒的淋巴形成将具有治疗优势。基于脂质的制剂常用于通过淋巴系统递药。黄芩苷纳米乳可能是改善 HBV 感染治疗的有前途的药物传递系统。本研究旨在制备、表征和评估载黄芩苷的基于脂质的纳米乳，以用于淋巴系统吸收。通过伪三元相图研究纳米乳液区域的存在。研究了载黄芩苷纳米乳的理化性质。比较了载黄芩苷纳米乳的口服生物利用度与黄芩苷混悬液的口服生物利用度。使用乳糜微粒流动阻断模型来检查淋巴摄取程度。测量黄芩苷在淋巴结中的分布，以研究纳米乳与混悬液相比的淋巴转运能力。与黄芩苷混悬液相比，黄芩苷纳米乳的 AUC 和 C 值分别增加了 10.5 倍和 3.12 倍。与用生理盐水处理的经口给予黄芩苷纳米乳的大鼠相比，用环己酰亚胺预处理的大鼠的纳米乳 AUC 和 C 值从 23.076±1.244 mg/L·h 降低至 9.236±0.940 mg/L·h 和从 3.010±0.119 mg/L 降低至 1.567±0.220 mg/L。在比较 W/O 纳米乳中的黄芩苷与混悬液中的黄芩苷时，发现用纳米乳处理的大鼠的淋巴结中 C 值高 11.5 倍。结果表明，载黄芩苷的 W/O 纳米乳可能是治疗慢性乙型肝炎的有前途的药物传递系统。
