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A long-lasting oral preformulation of the angiotensin II AT1 receptor antagonist losartan.
De Paula, Washington X; Denadai, Ângelo M L; Braga, Aline N G; Shastri, V Prasad; Pinheiro, Sérgio V B; Frezard, Frederic; Santos, Robson A S; Sinisterra, Ruben D.
Afiliación
  • De Paula WX; a Laboratório de Encapsulamento Molecular e Biomateriais (LEMB), Chemistry Department, Universidade Federal de Minas Gerais (UFMG) , Belo Horizonte , MG , Brazil.
  • Denadai ÂML; b Laboratório de Nanotecnologia dos Fluidos Complexos, Pharmacy Department, Universidade Federal de Juiz de Fora (UFJF) , Valadares , MG , Brazil.
  • Braga ANG; c Biophysics and Physiology Department , Universidade Federal de Minas Gerais (UFMG) , Belo Horizonte , MG , Brazil.
  • Shastri VP; d Department of Chemistry , Pharmacy, and Earth Sciences, Institute for Macromolecular Chemistry and BIOSS Centre for Biological Signalling Studies, University of Freiburg , Freiburg , Germany.
  • Pinheiro SVB; c Biophysics and Physiology Department , Universidade Federal de Minas Gerais (UFMG) , Belo Horizonte , MG , Brazil.
  • Frezard F; c Biophysics and Physiology Department , Universidade Federal de Minas Gerais (UFMG) , Belo Horizonte , MG , Brazil.
  • Santos RAS; c Biophysics and Physiology Department , Universidade Federal de Minas Gerais (UFMG) , Belo Horizonte , MG , Brazil.
  • Sinisterra RD; a Laboratório de Encapsulamento Molecular e Biomateriais (LEMB), Chemistry Department, Universidade Federal de Minas Gerais (UFMG) , Belo Horizonte , MG , Brazil.
Drug Dev Ind Pharm ; 44(9): 1498-1505, 2018 Sep.
Article en En | MEDLINE | ID: mdl-29683352
Losartan (Los), a non-peptidic orally active agent, reduces arterial pressure through specific and selective blockade of angiotensin II receptor AT1. However, this widely used AT1 antagonist presents low bioavailability and needs once or twice a day dosage. In order to improve its bioavailability, we used the host: guest strategy based on ß-cyclodextrin (ßCD). The results suggest that Los included in ßCD showed a typical pulsatile release pattern after oral administration to rats, with increasing the levels of plasma of Los. In addition, the inclusion compound presented oral efficacy for 72 h, in contrast to Los alone, which shows antagonist effect for only 6 h. In transgenic (mREN2)L27 rats, the Los/ßCD complex reduced blood pressure for about 6 d, whereas Los alone reduced blood pressure for only 2 d. More importantly, using this host: guest strategy, sustained release of Los for over a week via the oral route can be achieved without the need for encapsulation in a polymeric carrier. The proposed preformulation increased the efficacy reducing the dose or spacing between each dose intake.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptor de Angiotensina Tipo 1 / Bloqueadores del Receptor Tipo 1 de Angiotensina II Límite: Animals Idioma: En Revista: Drug Dev Ind Pharm Año: 2018 Tipo del documento: Article País de afiliación: Brasil Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptor de Angiotensina Tipo 1 / Bloqueadores del Receptor Tipo 1 de Angiotensina II Límite: Animals Idioma: En Revista: Drug Dev Ind Pharm Año: 2018 Tipo del documento: Article País de afiliación: Brasil Pais de publicación: Reino Unido