School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
J Pharm Pharm Sci. 2011;14(1):46-59. doi: 10.18433/j37w2v.
The aim of the present study was to use a novel protein co-encapsulation method to prepare phenytoin-loaded human erythrocytes with improved loading parameters and release profiles. Carrier erythrocytes were prepared using the hypotonic pre-swelling method. A series of in vitro characterization tests were carried out on the carrier cells, including loading parameters, drug and hemoglobin release, hematological indices, particle size analysis, osmotic fragility, turbulence fragility, and scanning electron microscopy (SEM). Co-encapsulation with bovine serum albumin (BSA) resulted in about 8-times higher drug loading in erythrocytes, with biphasic release trend instead of triphasic in the case of drug alone loading. In comparison to the normal unloaded cells, MCH and MCHC indices were decreased in the case of both drug and drug/protein loading, apparent cell sizes were unchanged, cell shapes were changed to spherical rather than biconcave discoid, and the osmotic as well as turbulence fragilities were higher in the case of drug/protein but were unchanged in the case of drug alone loading. The most profound finding of this study was the possibility of achieving remarkably higher drug loading and more controllable drug release profile in the case of drug/protein loading, with no unwanted in vitro characteristics change.
本研究旨在采用一种新的蛋白质共包封方法，制备载有苯妥英的人红细胞，以改善载药参数和释放特性。采用低渗预溶胀法制备载体红细胞。对载体细胞进行了一系列体外特性测试，包括载药参数、药物和血红蛋白释放、血液学指标、粒径分析、渗透压脆性、湍流脆性和扫描电子显微镜（SEM）。与单独载药相比，与牛血清白蛋白（BSA）共包封可使红细胞中药物的载药量增加约 8 倍，并呈两相释放趋势，而不是三相释放。与正常未载药细胞相比，药物和药物/蛋白质载药后 MCH 和 MCHC 指数降低，细胞大小无明显变化，细胞形状由双凹碟形变为球形，药物/蛋白质载药后的渗透压和湍流脆性增加，但单独载药时无明显变化。本研究最显著的发现是，在药物/蛋白质载药时，有可能实现显著更高的药物载药量和更可控的药物释放特性，而无体外特性的不良变化。
