Non-ionic thiolated cyclodextrins - the next generation

International Journal of Nanomedicine
Ali MoghadamAndreas Bernkop-Schnürch

Abstract

The current study was aimed at developing a novel mucoadhesive thiolated cyclodextrin (CD) without ionizable groups and an intact ring backbone for drug delivery. Thiolated beta CD (β-CD) was prepared through bromine substitution of its hydroxyl groups followed by replacement to thiol groups using thiourea. The thiolated β-CD was characterized in vitro via dissolution studies, cytotoxicity studies, mucoadhesion studies on freshly excised porcine intestinal mucosa, and inclusion complex formation with miconazole nitrate. Thiolated β-CDs namely β-CD-SH600 and β-CD-SH1200 displayed 558.66 ± 78 and 1,163.45 ± 96 µmol thiol groups per gram of polymer, respectively. Stability constant (Kc) of 190 M-1 confirmed the inclusion complex formation of miconazole nitrate with β-CD-SH. Inclusion complexes of β-CD-SH600 and β-CD-SH1200 resulted in 157- and 257-fold increased solubility of miconazole nitrate, respectively. In addition, more than 80% of thiol groups were stable even after 6 hours at pH 5. Both β-CD-SH compounds showed at least 1.3-fold improved solubility in water. In contrast to cationic thiolated CDs of the first generation, both thiomers showed no significant cytotoxicity. The mucoadhesive properties of the new thiolated CDs ...Continue Reading

Citations

Dec 29, 2020·Review Journal of Chemistry·D N MakhayevaV V Khutoryanskiy
Mar 7, 2021·International Journal of Pharmaceutics·Mulazim Hussain AsimAndreas Bernkop-Schnürch
Jul 24, 2018·Journal of Colloid and Interface Science·Mulazim Hussain AsimAndreas Bernkop-Schnürch
Jul 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Danielle M Beaupre, Richard G Weiss
Jan 28, 2020·ACS Applied Materials & Interfaces·Mulazim Hussain AsimAndreas Bernkop-Schnürch

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Methods Mentioned

BETA
solubility studies
nuclear magnetic resonance

Software Mentioned

GraphPad Prism
HyStar
GraphPad

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