Department of Pharmaceutics, The University of Mississippi, University, Mississippi, USA.
J Drug Target. 2010 Jan;18(1):36-44. doi: 10.3109/10611860903156393.
Bovine serum albumin (BSA) microspheres of ferric pyrophosphate (FPP) intended for passive targeting to the Peyer's patches has been proposed for oral iron supplementation. Microspheres prepared by emulsification chemical cross linking method were characterized for surface topography, entrapment efficiency, particle size, particle charge and in vitro drug release. Microspheres of batch C with FPP to BSA ratio of 1:5 were found to be most suitable for targeting as they exhibited high entrapment (83.88 +/- 4.31), high monodispersity (span = 1.24 +/- 0.01), and least particle size (d(vm) = 4.40 +/- 0.01). In addition the amount of iron retained in these microspheres despite exposure to simulated gastrointestinal conditions for 5 h was found to be 83.72 +/- 4.22%, the highest in the three batches. The in vivo serum iron profiles in normal rats following oral administration displayed a reduced T(max) (2 h), elevated C(max) (106.06 +/- 12.18 mug/dL) and increased AUC (0-16 h) (647.44 +/- 52.33 mug.h/dL) for these microspheres which significantly differed (P <0.05) from FPP solution indicating a higher iron repletion potential of the BSA microspheres.
牛血清白蛋白(BSA)铁焦磷酸(FPP)微球被提议用于被动靶向派尔集合淋巴结,以进行口服铁补充。通过乳化化学交联法制备的微球的特征在于表面形貌、包封效率、粒径、颗粒电荷和体外药物释放。发现 FPP 与 BSA 比例为 1:5 的 C 批微球最适合靶向,因为它们表现出高包封效率(83.88 +/- 4.31)、高单分散性(跨度 = 1.24 +/- 0.01)和最小粒径(d(vm)= 4.40 +/- 0.01)。此外,尽管在模拟胃肠道条件下暴露 5 小时,但这些微球中保留的铁量仍为 83.72 +/- 4.22%,在三批中最高。正常大鼠口服给药后血清铁谱显示,这些微球的 T(max)(2 小时)降低,C(max)(106.06 +/- 12.18 mug/dL)升高,AUC(0-16 小时)(647.44 +/- 52.33 mug.h/dL)增加,与 FPP 溶液显著不同(P <0.05),表明 BSA 微球具有更高的铁补充潜力。