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Hydrophilic albumin microspheres as cytarabine carriers

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Abstract

The surface of cytarabine-entrapped albumin microspheres was modified by coupling with glycine. Compared with conventionally prepared albumin microspheres, the surface modified albumin microspheres showed remarkably increased hydrophilicity, good dispersability in aqueous medium and reduced aggregation during storage which met the requirements of injectable drug carriers in aqueous vehicle.In vitro cytarabine release from hydrophilic albumin microspheres (HAM) was a function of the cytarabine to albumin ratio, whereas no significant difference in the releasing capacity was observed between surface modified HAM within the small size range (2 to 5 μ) studied. HAM containing 15–23% drug were gradually degraded by protease and continuously released up to 60% of the total entrapped cytarabine for 6 h. These results thus suggest that HAM is a suitable cytarabine carrier which may be injected intraveneously with the benefits of a reduced risk of blood embolism induced by aggregates and prolonged cytarabine release.

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Kim, CK., Chung, MH., Oh, YK. et al. Hydrophilic albumin microspheres as cytarabine carriers. Arch. Pharm. Res. 16, 123–128 (1993). https://doi.org/10.1007/BF03036859

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