One out of every three people in the world is infected with Mycobacterium tuberculosis. Approximately two billion people are carriers of tuberculosis (TB) and have the chance to develop the disease [1]. TB infection is a threat in western countries mostly due to the active TB development in HIV positive patients, but it is a burden in poor countries. Rifampicin is a first line drug used for the TB treatment for more than two decades but still there are challenges in improving its poor bioavailability. Major sources of this problem are instability of rifampicin at the acidic pH of the stomach and its low solubility. In our work, we proposed to improve rifampicin bioavailability with new cellulose esters used for oral drug delivery systems. Amorphous solid dispersions were prepared with rifampicin and cellulose derivatives (CAP-Adip, CAB-Seb, CA suberate and commercial polymer CMCAB for control purposes). Particle morphology and size were determined by SEM. In addition, XRD studies showed the amorphous nature of the spray dried particles. Afterwards, dissolution studies showed that these novel cellulose derivatives are successful in preventing rifampicin acid degradation (at stomach pH 1.2). Slow release of the antibiotic in the small intestine (pH 6.8) and rifampicin solubility increase were observed. In some of the formulations, 100% drug release was achieved while in other formulations rifampicin was released slowly without the burst effect. These new cellulose esters have strong ability to generate and stabilize supersaturated drug solutions and, great potential for amorphous solid dispersion applications. Referance 1.         Zumla, A., P. Nahid, and S.T. Cole, Advances in the development of new tuberculosis drugs and treatment regimens. Nature Reviews Drug Discovery, 2013. 12 (5): p. 388-404.

Innovative oral drug delivery vehicles to treat an ancient disease: Tuberculosis

248th National Meeting (2014)

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