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http://hdl.handle.net/1843/61199| Type: | Artigo de Periódico |
| Title: | A long-lasting oral preformulation of the angiotensin II AT1 receptor antagonist losartan |
| Authors: | Washington Xavier de Paula Ângelo Márcio Leite Denadai Aline Nardoni Gonçalves Braga Venkatram Prasad Shastri Sérgio Veloso Brant Pinheiro Frédéric Jean Georges Frézard Robson Augusto Souza dos Santos Rubén Dario Sinisterra Millán |
| Abstract: | 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 β-cyclodextrin (βCD). The results suggest that Los included in βCD 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/βCD 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. |
| Subject: | Agentes hipotensores Tecnologia de liberação controlada Farmacocinética Absorção (Fisiologia) Biodisponibilidade Ciclodextrinas |
| language: | eng |
| metadata.dc.publisher.country: | Brasil |
| Publisher: | Universidade Federal de Minas Gerais |
| Publisher Initials: | UFMG |
| metadata.dc.publisher.department: | ICB - DEPARTAMENTO DE FISIOLOGIA E BIOFÍSICA ICX - DEPARTAMENTO DE QUÍMICA MED - DEPARTAMENTO DE PEDIATRIA |
| Rights: | Acesso Restrito |
| metadata.dc.identifier.doi: | https://doi.org/10.1080/03639045.2018.1467923 |
| URI: | http://hdl.handle.net/1843/61199 |
| Issue Date: | 2018 |
| metadata.dc.url.externa: | https://www.tandfonline.com/doi/full/10.1080/03639045.2018.1467923 |
| metadata.dc.relation.ispartof: | Drug Development and Industrial Pharmacy |
| Appears in Collections: | Artigo de Periódico |
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