Allam Ahmed N, Komeil Ibrahim A, Fouda Mohamed A, Abdallah Ossama Y
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Egypt.
R&D Pharmacist at Medizen Pharmaceutical Industries, Alexandria, Egypt.
Int J Pharm. 2015 Jul 15;489(1-2):117-23. doi: 10.1016/j.ijpharm.2015.04.067. Epub 2015 Apr 29.
The aim of this study was to examine the efficacy of self-nano phospholipid dispersions (SNPDs) based on Phosal(®) to improve the oral bioavailability of curcumin (CUR). SNPDs were prepared with Phosal(®) 53 and Miglyol 812 at different surfactant ratio. Formulations were evaluated for particle size, polydispersity index, zeta potential, and robustness toward dilution, TEM as well as in vitro drug release. The in vivo oral absorption of selected formulations in comparison to drug suspension was evaluated in rats. Moreover, formulations were assessed for in vitro characteristic changes before and after storage. The SNPDs were miscible with water in any ratio and did not show any phase separation or drug precipitation. All the formulas were monodisperse with nano range size from 158±2.6 nm to 610±6.24 nm. They passed the pharmacopeial tolerance for CUR dissolution. No change in dissolution profile and physicochemical characteristics was detected after storage. CUR-SNPDs are found to be more bioavailable compared with suspension during an in vivo study in rats and in vitro release studies failed to imitate the in vivo conditions. These formulations might be new alternative carriers that enhance the oral bioavailability of poorly water-soluble molecules, such as CUR.
本研究的目的是考察基于Phosal（®）的自纳米磷脂分散体（SNPDs）提高姜黄素（CUR）口服生物利用度的效果。用Phosal（®）53和Miglyol 812以不同的表面活性剂比例制备SNPDs。对制剂进行粒径、多分散指数、zeta电位、稀释稳定性、透射电子显微镜（TEM）以及体外药物释放等方面的评估。在大鼠中评估所选制剂与药物混悬液相比的体内口服吸收情况。此外，还对制剂储存前后的体外特性变化进行了评估。SNPDs可与水以任何比例混溶，未出现任何相分离或药物沉淀现象。所有配方均为单分散，纳米尺寸范围为158±2.6 nm至610±6.24 nm。它们通过了药典对CUR溶出度的耐受性标准。储存后未检测到溶出曲线和理化特性的变化。在大鼠体内研究中发现，与混悬液相比，CUR-SNPDs具有更高的生物利用度，且体外释放研究未能模拟体内情况。这些制剂可能是提高难溶性分子如CUR口服生物利用度的新型替代载体。
