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Published on: April 4, 2022
Inclusion complex of methyl-β-cyclodextrin and olanzapine as potential drug delivery system for schizophrenia
Márcia Rocha de Freitas1, Larissa Araújo Rolim2, Monica Felts de La Roca Soares1
1Core of Medicines and Corelated Quality Control - NCQMC, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n. 50740-521 Recife, PE, Brazil.
Abstract:
Olanzapine (OLP), the most important atypical antipsychotic drug of the new generation, a high cost drug, has low aqueous solubility, affecting its dissolution and absorption. Its complexation with modified cyclodextrins (CDs) is designed to achieve novel vectorization systems with higher solubility, consequently higher bioavailability. From the CD selection, among β-CD, methyl-β-CD (MβCD) and hydroxypropyl-β-CD, it was obtained a phase solubility diagram suggesting a 1:1 (mol:mol) OLP-CD stoichiometry and complexation constants of 966.9, 149.4 and 91.1 L/mol, respectively. The MβCD was selected for the inclusion complexes (IC) attainment, a physical mixture (PM) and a rotatory evaporator product (ROE). The analysis showed differences in the structure, morphology and performance of OLP, MβCD, PM and ROE, revealing the occurrence of interactions between drug and CD. The ROE presented the higher dissolution efficiency and stability. The results suggest that the IC was formation, being a technological resource efficient and profitable for drug delivery.
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