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Controlled Release of Sulfasalazine Release from “Smart” Pectin Gel Microspheres under Physiological Simulated Fluids

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Abstract

Sulfasalazine (SLZ) is a synthetic nonsteroidal anti-inflammatory drug used mainly for the treatment of an inflammatory bowel and other diseases. Two pectins with different methylation degrees were blended to synthesized gel microspheres by ionotropic gelation for SLZ encapsulation. The encapsulation efficiency was found to be around of 99% in all formulations tested. However, different SLZ release profiles related to the methylation degrees of pectin were observed. Mixture of low methylated (LM) and high methylated (HM) pectins in the presence of calcium(II) displayed the best microsphere morphologies among the formulations tested determined by optical and electronic microscopies. The percentage of drug release using a mixture of LM and HM pectins after 255 min in simulated gastric fluid (pH = 1.2), simulated intestinal fluid (pH = 6.8), and phosphate buffer (pH = 7.4) were 15.0%, 47.0%, and 52.2%, respectively.

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Acknowledgments

The present work was supported by the Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET, PIP 297), CIUNT 26/D 409 and the Agencia Nacional de Promoción Científica y Técnica (ANPCyT) of Argentina. We thank CPKelco (Buenos Aires, Argentina) for the donation of pectin samples used in the present work.

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Authors and Affiliations

  1. Planta Piloto de Procesos Industriales Microbiológicos (PROIMI-CONICET), Av. Belgrano y Pasaje Caseros, T4001MVB, Tucumán, Argentina

    Luciana Costas & Licia M. Pera

  2. Lab. de Física de Fluidos y Electroreología, Depto. de Física, Facultad de Ciencias Exactas y Tecnología, Universidad Nacional de Tucumán, Av. Roca 1800, (T4001MVB), Tucumán, Argentina

    Azucena Gómez López & Magdalena Mechetti

  3. CINDEFI (CONICET, CCT La Plata)—School of Sciences, Universidad Nacional de La Plata, Calle 50 # 227, B1900AJL, La Plata, Provincia de Buenos Aires, Argentina

    Guillermo R. Castro

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  1. Luciana Costas
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  2. Licia M. Pera
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  3. Azucena Gómez López
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  4. Magdalena Mechetti
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Correspondence to Guillermo R. Castro.

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Costas, L., Pera, L.M., López, A.G. et al. Controlled Release of Sulfasalazine Release from “Smart” Pectin Gel Microspheres under Physiological Simulated Fluids. Appl Biochem Biotechnol 167, 1396–1407 (2012). https://doi.org/10.1007/s12010-012-9615-x

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  • DOI: https://doi.org/10.1007/s12010-012-9615-x

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