title: In vivo evaluation of the highly soluble oral β-cyclodextrin-Sertraline supramolecular complexes.
abstract: The aim of the present work was to evaluate the antidepressant like-effect and plasma concentration of Sertraline (SRT) using an inclusion complex (IC) with β-cyclodextrin (βCD) in mice. This supramolecular system was prepared using two different molar ratios at 1:1 and 1:2 SRT:βCD and both were characterized to assess the drug inclusion into the host cavity. Based on the X-ray powder diffraction, Fourier transform infrared spectroscopy and thermal analysis the interaction between host and guest molecules could be suggested. This result indicates that the freeze drying process was efficient to prepare the ICs, when these are compared with the physical mixtures. By comparing the solid state results of 1:1 and 1:2 ICs no significant chemical or structural changes were identified between these systems. However, in vivo experiments indicated that the host-guest ratio was able to modify the SRT activity. Mice treated with both ICs (20 mg kg(-1), p.o.) have shown lower immobility time in the tail suspension test in comparison with mice treated with free SRT (20 mg kg(-1), p.o.). Mice spontaneous locomotor activity was not affected by any treatment. Higher SRT plasma concentration was determined after 30 min of treatment with 1:1 IC in comparison with free SRT, demonstrating the IC greater drug transport efficacy.
authors: Laboratório de Encapsulamento Molecular e Biomateriais (LEMB) - Departamento de Química, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais (UFMG), Belo Horizonte, MG 31270-901, Brazil.
authors: Joel J
authors: JJ
authors: Passos
authors: Frederico B
authors: FB
authors: De Sousa
authors: Iram M
authors: IM
authors: Mundim
authors: Ricardo R
authors: RR
authors: Bonfim
authors: Robson
authors: R
authors: Melo
authors: Alice F
authors: AF
authors: Viana
authors: Eveline D
authors: ED
authors: Stolz
authors: Milene
authors: M
authors: Borsoi
authors: Stela M K
authors: SM
authors: Rates
authors: Rubén D
authors: RD
authors: Sinisterra
mesh_terms: D000818:Animals; D000928:Antidepressive Agents / Q000097:blood / Q000737:chemistry / Q000494:pharmacology*; D019417:Hindlimb Suspension; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D033362:Powder Diffraction; D020280:Sertraline / Q000097:blood / Q000737:chemistry / Q000494:pharmacology*; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction; D047392:beta-Cyclodextrins / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000928:Antidepressive Agents; D047392:beta-Cyclodextrins; C031215:betadex; D020280:Sertraline