AAPS PharmSciTech

, 20:67 | Cite as

Promising Chitosan-Coated Alginate-Tween 80 Nanoparticles as Rifampicin Coadministered Ascorbic Acid Delivery Carrier Against Mycobacterium tuberculosis

  • Ivana R. Scolari
  • Paulina L. Páez
  • Mariela E. Sánchez-Borzone
  • Gladys E. GraneroEmail author
Research Article


The aim of this study was to design a nanocarrier system for inhalation delivery of rifampicin (RIF) in combination with ascorbic acid (ASC), namely constituted of sodium alginate coated with chitosan and Tween 80 (RIF/ASC NPs) as a platform for the treatment of pulmonary tuberculosis infection. A Box-Behnken experimental design and response surface methodology (RSM) were applied to elucidate and evaluate the effects of several factors on the nanoparticle properties. On the other hand, it was found that RIF/ASC NPs were less cytotoxic than the free RIF, showing a significantly improved activity against nine clinical strains of Mycobacterium tuberculosis (M. tb) in comparison with the free drug. RIF/ASC NPs had an average particle size of 324.0 ± 40.7 nm, a polydispersity index of 0.226 ± 0.030, and a zeta potential of − 28.52 ± 0.47 mV and the surface was hydrophilic. The addition of sucrose (1% w/v) to the nanosuspension resulted in the formation of a solid pellet easily redispersible after lyophilization. RIF/ASC NPs were found to be stable at different physiological pH values. In summary, findings of this work highlight the potential of the RIF/ASC NP-based formulation development herein to deliver RIF in combination with ASC through pulmonary route by exploring a non-invasive route of administration of this antibiotic, increasing the local drug concentrations in lung tissues, the primary infection site, as well as reducing the risk of systemic toxicity and hence improving the patient compliance.


rifampicin ascorbic acid sodium alginate chitosan nanoparticles tuberculosis 



The authors acknowledge the ConsejoNacional de InvestigacionesCientíficas y Técnicas (CONICET), the Secretaría de Ciencia y Técnica de la Universidad Nacional de Córdoba (SECyT-UNC), and the Fondopara la InvestigaciónCientífica y Tecnológica (FONCYT) for providing the support and the facilities for this study and to the Bioq. Norberto Símboli, Servicio de Micobacterias, Instituto Nacional de Enfermedades Infecciosas “DR. CARLOS G. MALBRÁN.”

Supplementary material

12249_2018_1278_MOESM1_ESM.docx (144 kb)
ESM 1 (DOCX 143 kb)


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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Ivana R. Scolari
    • 1
  • Paulina L. Páez
    • 1
  • Mariela E. Sánchez-Borzone
    • 2
  • Gladys E. Granero
    • 1
    Email author
  1. 1.Unidad de Investigación y Desarrollo en Tecnología Farmacéutica (UNITEFA), CONICET and Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Químicas, Universidad Nacional de CórdobaCiudad UniversitariaCórdobaArgentina
  2. 2.Instituto de Investigaciones Biológicas y Tecnológicas (IIByT), CONICET and Cátedra de Química Biológica, Departamento de Química, Facultad de Ciencias de Exactas, Físicas y Naturales, Universidad Nacional de CórdobaCiudad UniversitariaCórdobaArgentina

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