Zhou Yue, Ning Qing, Yu Dan-Ni, Li Wei-Guang, Deng Jin
Hospital of Traditional Chinese Medicine Affiliated to Nanjing University of Chinese Medicine, Lianyungang, China.
J Pharm Pharmacol. 2014 Jul;66(7):903-11. doi: 10.1111/jphp.12215. Epub 2014 Feb 12.
Breviscapine, a hydrophobic drug used for treating cardiovascular disease, was encapsulated in liposomes to improve its pharmaceutical characteristics. This study describes a novel liposome composition approach to specifically inhibit the P-glycoprotein efflux system.
Breviscapine-loaded Pluronic P85-coated liposomes were prepared by the thin film hydration technique. The particle size, zeta potential and encapsulation efficiency of the formulations were characterized. In-vitro drug release and permeability of Caco-2 cells were investigated. In-vitro characteristics and pharmacokinetics of the liposomes were evaluated in rat studies.
The Pluronic P85-modified liposomes dispersed individually and had an approximate diameter of 118.8 ± 4.9 nm and a zeta potential of -35.4 ± 1.5 mV. Encapsulation efficiency was more than 90%. The use of the P85-coated liposomes resulted in significantly (P<0.05) increased absorption of breviscapine in Caco-2 cells and in 5.6-fold enhancement in its oral bioavailability in rats.
The P85-modified liposomes for the oral delivery of breviscapine were prepared using l-α-phosphatidylcholine (soy-hydrogenated) and cholesterol with a narrow size distribution. This method seems to effectively enhance the bioavailability of breviscapine in rats.
灯盏花素是一种用于治疗心血管疾病的疏水药物，将其包裹于脂质体中以改善其药学特性。本研究描述了一种新型脂质体组成方法，以特异性抑制P-糖蛋白外排系统。
采用薄膜水化技术制备负载灯盏花素的普朗尼克P85包衣脂质体。对制剂的粒径、ζ电位和包封率进行了表征。研究了其体外药物释放及对Caco-2细胞的通透性。通过大鼠研究评估了脂质体的体外特性和药代动力学。
普朗尼克P85修饰的脂质体单独分散，平均直径约为118.8±4.9 nm，ζ电位为-35.4±1.5 mV。包封率超过90%。使用P85包衣脂质体导致灯盏花素在Caco-2细胞中的吸收显著增加（P<0.05），并且其在大鼠体内的口服生物利用度提高了5.6倍。
使用l-α-磷脂酰胆碱（氢化大豆）和胆固醇制备了用于口服递送灯盏花素的P85修饰脂质体，其粒径分布窄。该方法似乎能有效提高灯盏花素在大鼠体内的生物利用度。
