Development and evaluation of Captisol®-based inclusion complex of bedaquiline fumarate for enhanced pharmaceutical performance: a proof-of-concept study

Abstract

The beneficial effect of bedaquiline fumarate (BQF) for tuberculosis (TB) is limited by its oral bioavailability, which is very low because of poor aqueous solubility. This research work highlights the organized exploration of the formation and investigation of the inclusion complex (IC) using β-cyclodextrin derivative Captisol^® for improving the solubility of BQF.

The characterizations were performed using FTIR, DSC, and NMR. The findings of the phase solubility analysis highlighted a concentration-dependent increase in the solubility of BQF in the presence of Captisol^®, and the higher apparent solubility constant indicated the formation of a stable IC. In vitro dissolution, cytotoxicity, cell uptake, gut permeability, and pharmacokinetics of the prepared ICs were carried out. NMR and FTIR confirmed the interaction of BQF and Captisol^®.

DSC, NMR, and polarized microscopy results concluded the amorphous nature of BQF within the IC. The BQF-Captisol^® IC was biocompatible with Caco-2 cells, and its uptake study showed a 7-fold improvement over BQF alone. The pharmacokinetic results confirmed a surge in C_max and in the relative bioavailability of BQF with BQF-Captisol^® IC. Thereby, the present work demonstrated the safety and efficacy of BQF-Captisol^® IC for the treatment of TB.

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Pardhi, V.P., Tarannum, S., Dey, M. et al. Development and evaluation of Captisol^®-based inclusion complex of bedaquiline fumarate for enhanced pharmaceutical performance: a proof-of-concept study. Polym. Bull. 83, 471 (2026). https://doi.org/10.1007/s00289-026-06514-2

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