Hamidi M, Zarrin A H, Foroozesh M, Zarei N, Mohammadi-Samani S
Department of Pharmaceutics, Faculty of Pharmacy, Shiraz University of Medical Sciences, P.O. Box 71345-1583, Shiraz, Iran.
Int J Pharm. 2007 Aug 16;341(1-2):125-33. doi: 10.1016/j.ijpharm.2007.04.001. Epub 2007 Apr 6.
Carrier erythrocytes is one of the most promising systemic drug delivery systems investigated in recent decades. In this study, human erythrocytes have been loaded with interferon-alpha 2b (IFN) with the aim to benefit the reticuloendothelial system (RES) targeting potential of the carrier cells. Hypotonic preswelling method was used for drug loading in erythrocytes and the entire loading procedure was evaluated and validated. The loaded amount, entrapment efficiency and cell recovery of the loading procedure were 2906.33+/-588.35IU/0.1ml, 14.53+/-2.94%, and 83.61+/-0.49%, respectively, all being practically feasible. The carrier erythrocytes were characterized in vitro in terms of their drug release kinetics, hematological indices, particle size distribution, SEM analysis, and osmotic and turbulence fragility. IFN release from carrier cells was a relatively rapid process in comparison to the cell lysis kinetics, which is unusual considering the whole body of data published on this delivery system and other protein drugs, so far. All the tested in vitro characteristics showed significant, sometimes notable changes upon drug loading procedure, both with and without the drug.
携带药物的红细胞是近几十年来研究的最有前景的全身给药系统之一。在本研究中，已将α-2b干扰素（IFN）载入人红细胞，目的是提高载体细胞对网状内皮系统（RES）的靶向潜力。采用低渗预膨胀法将药物载入红细胞，并对整个载入过程进行了评估和验证。载入过程的载药量、包封率和细胞回收率分别为2906.33±588.35IU/0.1ml、14.53±2.94%和83.61±0.49%，均切实可行。对携带药物的红细胞进行了体外表征，包括药物释放动力学、血液学指标、粒度分布、扫描电镜分析以及渗透和湍流脆性。与细胞裂解动力学相比，载体细胞释放IFN是一个相对快速的过程，考虑到迄今为止关于该给药系统和其他蛋白质药物发表的所有数据，这是不寻常的。所有测试的体外特性在载药过程中均显示出显著的、有时是明显的变化，无论有无药物。
