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

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posted on 2022-11-23, 09:56 authored by Vishwas P Pardhi, Teeja Suthar, Ankita Sharma, Keerti Jain
<p>Aim: Bedaquiline fumarate (BQF), an antitubercular drug, shows limited bioavailability due to solubilitylimited</p> <p>intestinal absorption. In this research, the authors formulated a BQF-loaded microemulsion</p> <p>to improve BQF’s oral bioavailability. Methods: Microemulsion was prepared by a spontaneous</p> <p>emulsification method and evaluated for thermodynamic stability, size, dispersibility, transmittance,</p> <p>rheology, microrheology, drug release, cytotoxicity and cellular uptake. Results: Microemulsion showed</p> <p>an average globule size of 26.50 ± 6.29 nm with spherical geometry and revealed gel-sol-gel behavior</p> <p>in microrheological studies. Cytotoxicity and cell uptake studies in Caco-2 cells showed that BQF</p> <p>microemulsion was cytocompatible at the highest concentration of 500 μg/ml with significantly higher</p> <p>cellular uptake than control. Conclusion: The present study indicates that BQF microemulsion could be</p> <p>explored further for effective treatment of multidrug-resistant tuberculosis.</p>

Funding

Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, India, (Grant / Award Number: )

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