Influence of cyclodextrin on posaconazole stability, release and activity: Improve the utility of the drug

Cyclodextrins (CDs) are cyclic oligosaccharides capable to improve chemical and physical stability of drugs through formation of drug/CD complexes. In this work, were related the formation of complex inclusion from β-CD and antifungal drug posaconazole (POS) by kneading represented by singular features observed from material amorphization, disorganized surface morphological, elevation of thermal decomposition in relation to β-CD. The inclusion complex formation increased the stability of POS in oxidative stress condition promoting increase of half-life time (29.20–46.61 h) and shelf-time (3.22–5.17 h). This fact occurred due to protection of attack sites of hydrogen peroxide in the presence of β-CD, evidenced by computational simulation. In addition, the β-CD:POS complex provided enhanced solubility (about 5 times) and dissolution rate for drug. These features facility the availability of drug over time to promoting of in vitro antifungal activity. These results indicate that inclusion complex has promisor characteristics to future medicine once increase the stability, increment dissolution rate maintaining the antifungal efficacy of posaconazole. [Display omitted] •Formation of inclusion complex from β-cyclodextrin and posaconazole by co-grinding.•β-cyclodextrin increased of half-life time and shelf-time of posaconazole.•Drug protection against oxidative attack as visualized by computational simulation.•Simultaneous analysis of dissolution and in vitro antifungal activity.•Increment solubility enhancing in vitro activity.