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Supramolecular strategy for reducing the cardiotoxicity of bedaquiline without compromising its antimycobacterial efficacy
Kuok K.I.1; In Ng P.C.1; Ji X.1; Wang C.1; Yew W.W.2; Chan D.P.C.2; Zheng J.1; Lee S.M.Y.1; Wang R.1
2018-09-01
Source PublicationFood and Chemical Toxicology
ISSN18736351 02786915
Volume119Pages:425-429
Abstract

Bedaquiline (BDQ) is a newly approved anti-tuberculosis drug in treating multidrug-resistant tuberculosis. However, it has very poor aqueous solubility and several case reports have proposed that BDQ has potential risk of cardiotoxicity to patients. In this present study, we have explored into employing host-guest interactions between a synthetic receptor, cucurbit[7]uril (CB[7]), and BDQ aiming to improve the solubility and reduce the inherent cardiotoxicity of BDQ. HPLC-UV test on the solubility of BDQ in the absence and in the presence of increasing concentrations of CB[7] suggested a host-dependent guest-solubility enhancements. Cardiovascular studies using an in vivo zebrafish model demonstrated that the cardiotoxicity of BDQ was indeed alleviated upon its complexations by the synthetic receptor. Furthermore, our in vitro antibacterial studies suggested that CB[7] formulated BDQ preserved its antimycobacterial efficacy against Mycobacterium smegmatis. Therefore, CB[7] may become a suitable pharmaceutical excipient in formulating BDQ for improving its physiochemical properties (such as solubility), and for alleviating its side effects (such as cardiotoxicity), while the antimycobacterial efficacy of BDQ may be well maintained.

KeywordAntimycobacterial Bedaquiline Cardiotoxicity Cucurbit[7]Uril Supramolecular Formulation
DOI10.1016/j.fct.2017.12.022
URLView the original
Indexed BySCI
Language英语
WOS Research AreaFood Science & Technology ; Toxicology
WOS SubjectFood Science & Technology ; Toxicology
WOS IDWOS:000443664200051
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Citation statistics
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.Universidade de Macau
2.Chinese University of Hong Kong
Recommended Citation
GB/T 7714
Kuok K.I.,In Ng P.C.,Ji X.,et al. Supramolecular strategy for reducing the cardiotoxicity of bedaquiline without compromising its antimycobacterial efficacy[J]. Food and Chemical Toxicology,2018,119:425-429.
APA Kuok K.I..,In Ng P.C..,Ji X..,Wang C..,Yew W.W..,...&Wang R..(2018).Supramolecular strategy for reducing the cardiotoxicity of bedaquiline without compromising its antimycobacterial efficacy.Food and Chemical Toxicology,119,425-429.
MLA Kuok K.I.,et al."Supramolecular strategy for reducing the cardiotoxicity of bedaquiline without compromising its antimycobacterial efficacy".Food and Chemical Toxicology 119(2018):425-429.
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