Antidepressant/BCD complexes

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The paper Aree [1] starts with an interesting statistics on depression (for the references see the original paper):

Depression is a global mental illness as over 300 million people suffer from it and about 800,000 people die from suicide each year (WHO, 2017) – the situation before the coronavirus disease 2019 (COVID-19) pandemic. Recent data of the COVID-19 era frighten us: i) 1.5-year since the outbreak, the number of confirmed COVID-19 cases has gone beyond 170 million worldwide (Our World in Data, 2021); ii) about one-fourth of COVID-19 patients globally commonly experience depression (Rogers et al., 2021); and iii) one-half of the COVID-19 survivors suffer from depression (Perlis et al., 2021). An efficacious treatment for depression is achievable by using antidepressants. Selective serotonin reuptake inhibitors (SSRIs) are first-line, second-generation antidepressants including for example, sertraline (STL; Zoloft), fluoxetine (FXT; Prozac) and paroxetine (PXT; Paxil). SSRIs for the treatment of depression have been approved by the US Food and Drug Administration (FDA, 2014). Prozac is one of the most commonly prescribed and popular SSRIs in the US (Stokes and Holtz, 1997) as it is the only FDA-approved drug for adolescents (McClanahan, 2009). SSRIs have equivalent clinical efficacy in treating depression to tricyclic antidepressants (TCAs), firstgeneration drugs, and have fewer side effects due to their high selectivity in binding with serotonin transporters. Hence, SSRIs are safer in overdose than TCAs (Peretti et al. , 2000). SSRI drugs are rather less soluble in water and hence have limited oral bioavailability. To overcome the problem, the cyclodextrin encapsulation is a method of choice for enhancing aqueous solubility and reducing side effects of SSRIs (Passos et al., 2011, 2012; Buko et al., 2017; Abouhussein et al., 2019). Plus, light in the mist of COVID-19 crisis, SSRIs with antiinflammatory properties can be used in treating COVID-19-associated inflammatory lung disease, thus reducing severity of COVID-19 (Lenze et al., 2020; Hoertel et al., 2021; Meikle et al., 2021).

The BCD encapsulation of sertraline (STL) HCl and fluoxetine (FXT) HCl was studied by single-crystal X-ray diffraction and DFT complete-geometry optimization, in comparison to the reported complex of paroxetine (PXT) base.

[1] T. Aree, Advancing insights on β -cyclodextrin inclusion complexes with SSRIs through lens of X-ray diffraction and DFT calculation, International Journal of Pharmaceutics (2021), doi:

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