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Cytoprotection of pancreatic ß-cells and hypoglycemic effect of 2-hydroxypropyl-ß-cyclodextrin: sertraline complex in alloxan-induced diabetic rats.
Buko, Vyacheslav; Zavodnik, Ilya; Lukivskaya, Oxana; Naruta, Elena; Palecz, Bartlomiej; Belica-Pacha, Silwia; Belonovskaya, Elena; Kranc, Robert; Abakumov, Vladimir.
Afiliação
  • Buko V; Division of Biochemical Pharmacology, Institute of Biochemistry of Biologically Active Compounds, National Academy of Sciences, BLK-50, 230030 Grodno, Belarus; Department of Biotechnology, School of Medical Sciences, Krakowska 9, 15-875 Bialystok, Poland. Electronic address: buko@bioch.basnet.by.
  • Zavodnik I; Division of Biochemical Pharmacology, Institute of Biochemistry of Biologically Active Compounds, National Academy of Sciences, BLK-50, 230030 Grodno, Belarus; Department of Biochemistry, Yanka Kupala Grodno State University, BLK-50, 230030 Grodno, Belarus.
  • Lukivskaya O; Division of Biochemical Pharmacology, Institute of Biochemistry of Biologically Active Compounds, National Academy of Sciences, BLK-50, 230030 Grodno, Belarus.
  • Naruta E; Division of Biochemical Pharmacology, Institute of Biochemistry of Biologically Active Compounds, National Academy of Sciences, BLK-50, 230030 Grodno, Belarus.
  • Palecz B; Department of Physical Chemistry, Faculty of Chemistry, University of Lodz, Pomorska 165, 90-236 Lodz, Poland.
  • Belica-Pacha S; Department of Physical Chemistry, Faculty of Chemistry, University of Lodz, Pomorska 165, 90-236 Lodz, Poland.
  • Belonovskaya E; Division of Biochemical Pharmacology, Institute of Biochemistry of Biologically Active Compounds, National Academy of Sciences, BLK-50, 230030 Grodno, Belarus.
  • Kranc R; Department of Biotechnology, School of Medical Sciences, Krakowska 9, 15-875 Bialystok, Poland.
  • Abakumov V; Department of Pathological Anatomy, Grodno State Medical University, Gorkogo str., 80, 20009 Grodno, Belarus.
Chem Biol Interact ; 244: 105-12, 2016 Jan 25.
Article em En | MEDLINE | ID: mdl-26593071
Sertraline, a selective inhibitor of serotonin reuptake, is widely used as antidepressant in diabetic patients for improvement of depression and glycemic control. Sertraline is poorly soluble in water, which limits its oral applicability. In this work we tried to improve the pharmaceutical properties of sertraline by complexation with 2-hydroxypropyl-ß-cyclodextrin (HPßCD) and evaluated the efficacy of the HPßCD:sertraline complex in prevention of alloxan-induced lesions in rats. The solubility of sertraline increased in the presence of HPßCD and the association constant for sertraline and HPßCD was equal to 4000 ± 1000 M(-1). Two-week treatment of diabetic animals with the HPßCD:sertraline complex improved pancreatic islet morphology and ß-cell survival, which, in turn, reduced the severity of diabetes, as evidenced by lowering of blood glucose and glycated hemoglobin contents as well as normalization of serum insulin level and insulin sensitivity (HOMA-IR). The effect of the HPßCD:sertraline complex was strongly expressed in comparison with the antidiabetic effect of both the monopreparations, HPßCD and sertraline. It is suggested that the cyclodextrin derivative increased the pharmacological effect of sertraline, probably due to enhanced drug bioavailability.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sertralina / Beta-Ciclodextrinas / Diabetes Mellitus Experimental / Células Secretoras de Insulina / Hipoglicemiantes Limite: Animals Idioma: En Ano de publicação: 2016 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sertralina / Beta-Ciclodextrinas / Diabetes Mellitus Experimental / Células Secretoras de Insulina / Hipoglicemiantes Limite: Animals Idioma: En Ano de publicação: 2016 Tipo de documento: Article