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The aim of this study was to investigate human erythrocytes as a carrier fortargeted drug delivery of primaquine (PQ). The process of PQ loading in humanerythrocytes, as well as the effect of PQ loading on the oxidative status oferythrocytes, was also studied. At PQ concentrations of 2, 4, 6, and 8 mg/mLand an incubation time of 2 h, the ratios of the concentrations of PQ entrappedin erythrocytes to that in the incubation medium were 0.515, 0.688, 0.697 and0.788, respectively. The maximal decline of erythrocyte reduced glutathionecontent was observed at 8 mg/mL of PQ compared with native erythrocytes p <0.001. In contrast, malondialdehyde and protein carbonyl were significantlyincreased in cells loaded with PQ (p < 0.001). Furthermore, osmotic fragilityof PQ carrier erythrocytes was increased in comparison with unloaded cells.Electron microscopy revealed spherocyte formation with PQ carrier erythrocytes.PQ-loaded cells showed sustained drug release over a 48 h period. Erythrocyteswere loaded with PQ successfully, but there were some biochemical as well asphysiological changes that resulted from the effect of PQ on the oxidativestatus of drug-loaded erythrocytes. These changes may result in favorabletargeting of PQ-loaded cells to reticulo-endothelial organs. The relativeimpact of these changes remains to be explored in ongoing animal studies.

Biochemically altered human erythrocytes as a carrier for targeted delivery of primaquine: an in vitro study