Albumin microspheres for oral delivery of iron

作者：Shivakumar H N; Vaka Siva Ram Kiran; Murthy S Narasimha^*

来源：Journal of Drug Targeting, 2010, 18(1): 36-44.

DOI：10.3109/10611860903156393

• Oral iron
• Peyer's patch
• M-cell
• albumin microsphere
• ferric pyrophosphate
• serum iron

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 mu g/dL) and increased AUC(0-16h) (647.44 +/- 52.33 mu g.h/dL) for these microspheres which significantly differed (P < 0.05) from FPP solution indicating a higher iron repletion potential of the BSA microspheres.

• 出版日期2010-1