Cyclophosphamide Loaded Albumin Microspheres: Liver Entrapment and Fate in Mice

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Abstract
Microspheres offer the possibility of target selectivity through choice of appropriate size or surface charecteristics, slow release of drug and also minimize systemic toxicity. The active substance of this investigation, cyclophosphamide (CP), interferes with the growth of cancer cells which are eventually destroyed. Since side effects of CP are frequently dose related, by incorporating low dose of CP to human serum albumin (HSA) microspheres, the normal body cells are not affected while the tumour cells are destroyed. Cyclophosphamide microspheres were prepared by the modification of the method of Scheffel et al and Gürkan et al. 2,3-butanedione was used as a cross-linking agent. The albumin microspheres containing CP were labelled by 99mTc by incorporating SnC12.2H20 at a concentration of 5% of the matrix material. All the microspheres used in this study ranged between 1–5 μm. A suspension of 99mTc labelled cyclophosphamide microspheres was injected into swiss albino mice intravenously. At 15 min, 30 rain, 6 h and 24 h mice were killed and the organs assayed for radioactivity accumulated in each organ. 1 hour later the radioactivity in the liver increased to 4.73 percent. By 24 hours, 2.68 percent of the radioactivity was found in the liver. Whereas the percentage of free cyclophosphamide at 1 and 24 hours was 2.22 and 2.57 percent, respectively. Based on the evidence obtained from these results, the application of CP loaded HSA microspheres seems advantages in accumulation in liver.