Increased Bioavailability of Rifampicin from Stimuli-Responsive Smart Nano Carrier

Abstract

Stimuli responsive polymeric nanocarrier (RCOP-2) functionalized with frontline anti tuberculosis drug (rifampicin) is demonstrated for the sustained release. Bioavailability of rifampicin is taken care by conjugating it through a acylhydrazine linker to the polymeric backbone. PEG motif is introduced in the copolymer architecture for the water solubility. Releasing retinal along with rifampicin is hypothesized to reduce the risk of side effects due to rifampicin. The self-assembly of RCOP-2, due to the amphiphilicity present in the copolymer, is explored in detail. The pH responsiveness of RCOP-2 is demonstrated in mild acidic environment as well as in cell lines. 4T cell line, due to acidic nature, shows time dependent cellular internalization. Based on the results, our unique design is expected to provide an increased bioavalaibility of rifampicin with reduced side effects. From the flow cytometery results on A549 cell lines, it is clear that the newly designed copolymer RCOP-2, can internalize efficiently and serve as effective rifampicin delivery system.