Department of Pharmacy, Shandong University Hospital, Jinan 250012, China.
Drug Deliv. 2011 Nov;18(8):545-54. doi: 10.3109/10717544.2011.595842. Epub 2011 Aug 4.
The purpose of the study is to design and evaluate curcumin loaded gelatin microspheres (C-GMS) for effective drug delivery to the lung. C-GMS was prepared by the emulsification-linkage technique and the formulation was optimized by orthogonal design. The mean encapsulation efficiency and drug loading of the optimal C-GMS were 75.5 ± 3.82 % and 6.15 ± 0.44%, respectively. The C-GMS presented a spherical shape and smooth surface with a mean particle diameter of 18.9 μm. The in vitro drug release behavior of C-GMS followed the first-order kinetics. The tissue distribution showed that the drug concentrations at lung tissue for the C-GMS suspension were significantly higher than those for the curcumin solution, and the Ce for lung was 36.19. Histopathological studies proved C-GMS was efficient and safe to be used as a passive targeted drug delivery system to the lung. Hence, C-GMS has a great potential for the targeted delivery of curcumin to the lung.
本研究旨在设计和评估姜黄素载明胶微球（C-GMS），以实现药物向肺部的有效传递。C-GMS 通过乳化连接技术制备，并通过正交设计优化了配方。最佳 C-GMS 的平均包封效率和载药量分别为 75.5±3.82%和 6.15±0.44%。C-GMS 呈球形，表面光滑，平均粒径为 18.9μm。C-GMS 的体外药物释放行为符合一级动力学。组织分布研究表明，C-GMS 混悬液在肺部组织中的药物浓度明显高于姜黄素溶液，肺部的 Ce 为 36.19。组织病理学研究证明，C-GMS 作为一种被动靶向肺部给药系统具有高效、安全的特点。因此，C-GMS 具有将姜黄素靶向递送至肺部的巨大潜力。
