Montmorillonite–Rifampicin Nanohybrid for pH-Responsive Release of the Tuberculostatic

Author:

Damasceno Junior Elmar1,Barbosa Raquel de Melo2ORCID,da Silva Rita de Cássia Dantas1,Costa Felipe dos Santos1,da Silva Djalma Ribeiro1,Viseras César23ORCID,Perioli Luana4ORCID,Fernandes Nedja Suely1

Affiliation:

1. Institute of Chemistry, Federal University of Rio Grande do Norte, Natal 59078-970, RN, Brazil

2. Pharmaceutical Technology Department, University of Granada, 18071 Granada, Spain

3. Andalusian Institute of Earth Sciences, Spanish Research Council, University of Granada–CSIC-UGR, Avenida de las Palmeras 4, Armilla, 18100 Granada, Spain

4. Department of Pharmaceutic Science, University of Perugia, 06123 Perugia, Italy

Abstract

The present work describes the development of a hybrid and pH-responsive system for rifampicin using the clay mineral ‘montmorillonite’ as a nanocarrier. The influence of operational variables on the drug incorporation process was evaluated using 24 factorial designs. Under optimized conditions, the experiment allowed an incorporated drug dose equivalent to 98.60 ± 1.21 mg/g. Hybrid systems were characterized by different characterization techniques (FTIR, XRD, TGA, DSC, and SEM) to elucidate the mechanism of interaction between the compounds used. Through in vitro release studies, it was possible to verify the efficacy of the pH-dependent system obtained, with approximately 70% of the drug released after sixteen hours in simulated intestinal fluid. The adjustment of the experimental release data to the theoretical model of Higuchi and Korsmeyer–Peppas indicated that the release of rifampicin occurs in a prolonged form from montmorillonite. Elucidation of the interactions between the drug and this raw clay reinforces its viability as a novel carrier to develop an anti-TB/clay hybrid system with good physical and chemical stability.

Publisher

MDPI AG

Subject

Pharmaceutical Science

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