Center for Intelligent NanoBio Materials (CINBM), Division of Nano Science BK 21, Department of Bioinspired Science, Nano Science, Ewha Womans University, 11-1 daehyun-dong, Seodaemun-gu, Seoul 120-750, Republic of Korea.
Int J Pharm. 2010 Dec 15;402(1-2):117-22. doi: 10.1016/j.ijpharm.2010.09.039. Epub 2010 Oct 7.
Delivery of poorly soluble drugs has been problematic due to its low absorption profile and bioavailability. In this work, ursodeoxycholic acid (UDCA), a poorly-soluble drug, was intercalated into inorganic nanovehicle, layered double hydroxides (LDHs), with a molecular level to enhance its solubility in biological fluid. The UDCA-loaded nanovehicle (i.e., UDCA-LDHs) was also coated with an anionic polymer, Eudragit(®) S100, to increase the dissolution rate of UDCA. According to the powder X-ray diffraction (PXRD) patterns of UDCA-LDHs, the gallery height of LDHs was expanded from 3.6Å to 28.3Å, indicating that the UDCA molecules were successfully intercalated into the interlayer space of LDHs. Fourier transform infrared (FT-IR) spectra also revealed that the UDCA molecules were well stabilized in the LDHs through electrostatic interaction. The in vitro dissolution test in a simulated biological fluid (pH=6.8) showed that the total dissolved fraction of UDCA for the first 2h was about 60.2% for the Eudragit(®) S100 coated UDCA-LDHs, which was a dramatic increase as compared with 19.0% dissolution from intact UDCA. It is, therefore, concluded that LDHs nanovehicle coated with an anionic polymer is a promising delivery system for improving aqueous solubility of poorly soluble drugs.
由于其低吸收特性和生物利用度,难溶性药物的递送一直存在问题。在这项工作中,将一种难溶性药物熊去氧胆酸(UDCA)插入无机纳米载体层状双氢氧化物(LDHs)中,达到分子水平以提高其在生物流体中的溶解度。负载 UDCA 的纳米载体(即 UDCA-LDHs)也用阴离子聚合物 Eudragit(®) S100 进行了涂层处理,以提高 UDCA 的溶解速率。根据 UDCA-LDHs 的粉末 X 射线衍射(PXRD)图谱,LDHs 的层间距从 3.6Å 扩展到 28.3Å,表明 UDCA 分子已成功插入 LDHs 的层间空间。傅里叶变换红外(FT-IR)光谱也表明 UDCA 分子通过静电相互作用在 LDHs 中得到了很好的稳定。在模拟生物流体(pH=6.8)中的体外溶解试验表明,对于用阴离子聚合物涂层的 Eudragit(®) S100 涂层的 UDCA-LDHs,在前 2 小时内 UDCA 的总溶解分数约为 60.2%,与完整 UDCA 的 19.0%溶解相比有了显著增加。因此,可以得出结论,用阴离子聚合物涂层的 LDHs 纳米载体是一种提高难溶性药物水溶解度的有前途的给药系统。