title: Inclusion complex of methyl-β-cyclodextrin and olanzapine as potential drug delivery system for schizophrenia.
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.
authors.affiliation: Core 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.
authors.forename: Márcia Rocha
authors.initials: MR
authors.lastname: de Freitas
authors.affiliation: Laboratory of Medicines Technology - LTM, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n. 50740-521 Recife, PE, Brazil.
authors.forename: Larissa Araújo
authors.initials: LA
authors.lastname: Rolim
authors.affiliation: Core 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.
authors.forename: Monica Felts de La Roca
authors.initials: MF
authors.lastname: Soares
authors.affiliation: Laboratory of Medicines Technology - LTM, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n. 50740-521 Recife, PE, Brazil.
authors.forename: Pedro José
authors.initials: PJ
authors.lastname: Rolim-Neto
authors.affiliation: Core 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.
authors.forename: Miracy Muniz
authors.initials: MM
authors.lastname: de Albuquerque
authors.affiliation: Core 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.
authors.forename: José Lamartine
authors.initials: JL
authors.lastname: Soares-Sobrinho
mesh_terms: D014150:Antipsychotic Agents / Q000737:chemistry*; D001569:Benzodiazepines / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D000077152:Olanzapine; D012559:Schizophrenia / Q000188:drug therapy*; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D014150:Antipsychotic Agents; D004337:Drug Carriers; D047392:beta-Cyclodextrins; C108732:methyl-beta-cyclodextrin; D001569:Benzodiazepines; D000077152:Olanzapine