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

PÁEZ, PAULINA L.; SÁNCHEZ-BORZONE, MARIELA E.; SCOLARI, IVANA R.; GRANERO, GLADYS E.

AAPS PHARMSCITECH

SPRINGER

Lugar: Berlin; Año: 2019 vol. 20 p. 1 - 21

1530-9932

The aim of this study was to design a nanocarrier system for inhalation deliveryof rifampicin (RIF) in combination with ascorbic acid (ASC), namely constituted of sodiumalginate coated with chitosan and Tween 80 (RIF/ASC NPs) as a platform for the treatmentof pulmonary tuberculosis infection. A Box-Behnken experimental design and responsesurface methodology (RSM) were applied to elucidate and evaluate the effects of severalfactors on the nanoparticle properties. On the other hand, it was found that RIF/ASC NPswere 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 mVand the surface was hydrophilic. The additionof 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 differentphysiological 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 thisantibiotic, 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.