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

2019; Elsevier BV; Volume: 53; Linguagem: Inglês

10.1016/j.jddst.2019.101153

2588-8943

Ana Cristina Sousa Gramoza Vilarinho Santana, Daniela Nadvorny, Taisa Daiany da Rocha Passos, Mônica Felts de La Roca Soares, José Lamartine Soares‐Sobrinho,

Polysaccharides Composition and Applications

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.