Electrospun high bioavailable rifampicin–isoniazid-polyvinylpyrrolidone fiber membranes

Rifampicin (RIF) and Isoniazid (INH) are two first-line drugs for tuberculosis treatment. Compared to isoniazid, rifampicin has poor water solubility, which results in low bioavailability. Combining the two drugs can improve the treatment effect of tuberculosis, but thier direct contact may accelerate the degradation of rifampicin, which is also considered to be another reason for RIF’s low bioavailability. In this study, the polyvinylpyrrolidone (PVP) was selected as the carrier and mixed with the loaded drug of rifampicin and isoniazid separately. The quick-released rifampicin/isoniazid-polyvinylpyrrolidone mingled fibers (RIPMF) were fabricated by the electrospinning method to promote the absorption of rifampicin. The results showed that isoniazid-polyvinylpyrrolidone (INH-PVP) nanofibers and rifampicin-polyvinylpyrrolidone (RIF-PVP) microfibers were mixed in RIPMF, instead of two drugs coexisting in one fiber. Rifampicin and isoniazid in the fibers changed from crystalline to amorphous states, which facilitated the release of the rifampicin from the fibers. The hydrophilicity of RIF-PVP fibers was not distinct, but that of RIPMF increased with the addition of INH-PVP fibers. The release rate of rifampicin in rifampicin-loaded fibers was twice as fast as rifampicin powder. Additionally, in vitro antibacterial test showed that RIPMF had an obvious inhibition effect on Staphylococcus aureus. Finally, the rifampicin-loaded fibers enhanced the release rate of rifampicin and improved its bioavailability. Increased bioavailability reduces the waste of rifampicin and prevents damage to the kidneys due to the massive metabolism of rifampicin in biomedicine.