Abstract
Phyllosilicates have interesting properties, such as high capacity of ion exchange, adsorption, physicochemical stability and low/null toxicity, and thus, they are a promising material in pharmaceutical studies. Olanzapine (OLZ), used in the treatment of schizophrenia, is a drug of high cost and low water solubility, which are an obstacle to its use. In this work, an oral delivery system was developed using phyllosilicate (PHY-NT) and OLZ together to increase its solubility. PHY-NT was synthesized by sol–gel method, and then, OLZ was adsorbed creating the system called PHY-NT:OLZ. Thermal analysis was performed to investigate possible interactions between olanzapine and phyllosilicate. a sharp endothermic peak at 468 K was observed, which corresponds to the melting process of OLZ. When OLZ was added to PHY-NT, this peak was absent, suggesting an efficient denaturation of its crystal lattice. FTIR spectroscopy and X-ray powder diffraction were performed as complementary techniques to adequately support thermal analysis results. The created system caused a considerable increase in OLZ dissolution efficiency, and more than 80 % of the drug was released from PHY-NT:OLZ after 20 min. Drug release was evaluated in vitro and showed a Fickian diffusion-based pattern. Thus, results suggest that PHY-NT can be used as an alternative to increase drug dissolution rate of OLZ, expanding applications of these materials.
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The authors thank Capes, Facepe and CNPq for financial support.
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Gonçalves, M.L.C.M., Lyra, M.A.M., Oliveira, F.J.V.E. et al. Use of phyllosilicate clay mineral to increase solubility olanzapine. J Therm Anal Calorim 127, 1743–1750 (2017). https://doi.org/10.1007/s10973-016-5719-9
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DOI: https://doi.org/10.1007/s10973-016-5719-9