Use of phyllosilicate clay mineral to increase solubility olanzapine

• Published in: Journal of thermal analysis and calorimetry Vol. 127; no. 2; pp. 1743 - 1750
• Main Authors: Gonçalves, M. L. C. M., Lyra, M. A. M., Oliveira, F. J. V. E., Rolim, L. A., Nadvorny, D., Vilarinho, A. C. S. G., Nunes, L. C. C., Soares, M. F. L. R., Silva-Filho, E. C., Soares-Sobrinho, J. L.
• Format: Journal Article
• Language: English
• Published: Dordrecht Springer Netherlands 01-02-2017; Springer; Springer Nature B.V
• Subjects: Adsorption; Analytical Chemistry; Calorimetry; Chemistry; Chemistry and Materials Science; Clay minerals; Crystal lattices; Delivery systems; Denaturation; Diffraction patterns; Diffusion rate; Dissolution; Drug delivery systems; Drugs; Endothermic reactions; Inorganic Chemistry; Ion exchange; Measurement Science and Instrumentation; Obstacles; Olanzapine; Physical Chemistry; Polymer Sciences; Protein denaturation; Schizophrenia; Sol-gel processes; Solubility; Thermal analysis; X ray powder diffraction; Drug delivery; Olanzapine; Phyllosilicate; New excipient; Increased solubility
• ISSN: 1388-6150; 1588-2926; 1572-8943
• DOI: 10.1007/s10973-016-5719-9

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.