Bedaquiline fumarate microemulsion: formulation optimization, rheological characterization and in vitro studies - Supplementary data

Aim: Bedaquiline fumarate (BQF), an antitubercular drug, shows limited bioavailability due to solubilitylimited

intestinal absorption. In this research, the authors formulated a BQF-loaded microemulsion

to improve BQF’s oral bioavailability. Methods: Microemulsion was prepared by a spontaneous

emulsification method and evaluated for thermodynamic stability, size, dispersibility, transmittance,

rheology, microrheology, drug release, cytotoxicity and cellular uptake. Results: Microemulsion showed

an average globule size of 26.50 ± 6.29 nm with spherical geometry and revealed gel-sol-gel behavior

in microrheological studies. Cytotoxicity and cell uptake studies in Caco-2 cells showed that BQF

microemulsion was cytocompatible at the highest concentration of 500 μg/ml with significantly higher

cellular uptake than control. Conclusion: The present study indicates that BQF microemulsion could be

explored further for effective treatment of multidrug-resistant tuberculosis.