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Gemcitabine-loaded chitosan microspheres. Characterization and biological in vitro evaluation

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Abstract

This study investigates the potential of chitosan microspheres as delivery systems for the anticancer drug gemcitabine. The microspheres were obtained by spray-drying chitosan-gemcitabine solutions containing different amounts of the polyanion dextran sulphate. Morphological characterization by SEM and FIB analyses showed the presence of porous spherical particles having sizes ranging from about 1 to 5 μm. Dextran sulphate improves the technological parameters of the systems by producing very high encapsulation efficiency (about 96%, w/w) and by influencing the in vitro release of gemcitabine. The immediate drug release observed in the system prepared without dextrane sulphate (complete drug release within 30 min) was somewhat reduced by the polyanion (immediate release of 70% (w/w) of the encapsulated drug within 30 min, and subsequent continued release of the remaining 30% of the drug for over 4 days). The anti-tumoral efficacy of the various formulations was tested in vitro on human lung cancer cells (A549) comparing the effects with those of the free drug or drug/dextran sulfate complex. The carriers improved the cytotoxic activity of the drug, particularly the formulation containing the lowest amount of dextran sulphate after 72 h incubation.

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Acknowledgments

This work was partially supported by the University of Messina (Ricerca di Ateneo). The authors are grateful to Antonio Sangrigoli of STMicroelectronics s.r.l. for technical support to SEM and FIB analysis and to Lynn Whitted for her revision of the language.

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Authors and Affiliations

  1. Pharmacochemistry Department, Faculty of Pharmacy, University of Messina, V.le Annunziata, 98168, Messina, Italy

    Cinzia Anna Ventura, Carmela Cannavà, Rosanna Stancanelli & Silvana Tommasini

  2. Department of Experimental and Clinical Medicine, Faculty of Medicine, University “Magna Graecia” of Catanzaro, 88021, Catanzaro, Italy

    Donatella Paolino

  3. Pharmacobiological Department, Building of Biosciences, University “Magna Græcia” of Catanzaro, 88021, Catanzaro, Italy

    Donato Cosco

  4. Failure & Material Analysis Laboratory Mgr., STMicroelectronics s.r.l., Stradale Primo Sole, 50, 95121, Catania, Italy

    Antonio La Mantia

  5. Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Catania, 95125, Catania, Italy

    Rosario Pignatello

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  1. Cinzia Anna Ventura
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  2. Carmela Cannavà
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  3. Rosanna Stancanelli
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  4. Donatella Paolino
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  5. Donato Cosco
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  7. Rosario Pignatello
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  8. Silvana Tommasini
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Correspondence to Cinzia Anna Ventura.

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Ventura, C.A., Cannavà, C., Stancanelli, R. et al. Gemcitabine-loaded chitosan microspheres. Characterization and biological in vitro evaluation. Biomed Microdevices 13, 799–807 (2011). https://doi.org/10.1007/s10544-011-9550-6

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  • DOI: https://doi.org/10.1007/s10544-011-9550-6

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