Yu Chao, Xiao Yun-Zhi, Xun Ping-Hua, Dai Ling, Han Jin, Yuan Hai-Long
Zhongguo Zhong Yao Za Zhi. 2014 May;39(10):1799-804.
A novel drug delivery system combining oral fast dissolving film with sodium deoxycholate/phospholipid mixed micelles was prepared to increase the absorption of cucurbitacin B that is a poor aqueous solubility substance. Encapsulation efficiency, particle size, zeta potential, polydispersity coefficient, investigated the morphology, disintegration time of oral fast dissolving film and the pharmacodynamic properties of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles before and after solidified in mice were evaluated and compared. The oral fast dissolving film prepared in this study showed a homogeneous pale yellow and could completely disintegrated in the 30 s. It could meet the requirements of rapidly disintegrating fully. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles loaded in oral fast dissolving film were (43.36 +/- 2.12)%, (108.82 +/- 5.2) nm, (-34.18 +/- 1.07) mV, 0.088 +/- 0.012, respectively. The encapsulation efficiency, particle size, zeta potential, polydispersity coefficient of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles in solution were (41.26 +/- 2.22)%, (181.82 +/- 4.48) nm, (-30.67 +/- 0.81) mV, 0.092 +/- 0.012, respectively. The difference of pharmacodynamics among film of cucurbitacin B-loaded micelles, cucurbitacin B-loaded micelles and free cucurbitacin B in vivo was compared. Solubility of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles has also been greatly improved. The tumor inhibition rate of cucurbitacin B loaded in sodium deoxycholate/phospholipid-mixed micelles was significantly improved and did not change significantly before and after solidified. These showed that the sodium deoxycholate/phospholipid-mixed micelles could enhance the antitumor activities of cucurbitacin B and the stability of cucurbitacin B sodium deoxycholate/phospholipid-mixed micelles was improved significantly after solidified by oral fast dissolving film technology without pharmacodynamic properties changed significantly.
制备了一种将口服速溶膜与脱氧胆酸钠/磷脂混合胶束相结合的新型药物递送系统，以提高难溶性物质葫芦素B的吸收。评估并比较了包封率、粒径、zeta电位、多分散系数，研究了口服速溶膜的形态、崩解时间以及葫芦素B脱氧胆酸钠/磷脂混合胶束在小鼠体内固化前后的药效学性质。本研究制备的口服速溶膜呈均匀淡黄色，能在30 s内完全崩解，可完全满足快速崩解的要求。载于口服速溶膜中的葫芦素B脱氧胆酸钠/磷脂混合胶束的包封率、粒径、zeta电位、多分散系数分别为(43.36±2.12)%、(108.82±5.2)nm、(-34.18±1.07)mV、0.088±0.012。溶液中葫芦素B脱氧胆酸钠/磷脂混合胶束的包封率、粒径、zeta电位、多分散系数分别为(41.26±2.22)%、(181.82±4.48)nm、(-30.67±0.81)mV、0.092±0.012。比较了载有葫芦素B的胶束膜、载有葫芦素B的胶束和游离葫芦素B在体内的药效学差异。载于脱氧胆酸钠/磷脂混合胶束中的葫芦素B的溶解度也有很大提高。载于脱氧胆酸钠/磷脂混合胶束中的葫芦素B的抑瘤率显著提高，固化前后无明显变化。这些结果表明，脱氧胆酸钠/磷脂混合胶束可增强葫芦素B的抗肿瘤活性，口服速溶膜技术固化后，葫芦素B脱氧胆酸钠/磷脂混合胶束的稳定性显著提高，且药效学性质无明显改变。
