Rapid-onset sildenafil nasal spray carried by microemulsion systems: In vitro evaluation and in vivo pharmacokinetic studies in rabbits

Hsien-Tsung Lu, Ray Neng Chen, Ming Thau Sheu, Chung Chiao Chang, Po Yu Chou, Hsiu O. Ho

研究成果: 雜誌貢獻文章同行評審

15 引文 斯高帕斯(Scopus)

摘要

An oleic acid-based microemulsion system with a member of the Tween series or Cremophor EL as the surfactant and a short-chain alcohol as the cosolvent was developed for rapid-onset intranasal delivery of sildenafil. The phase behaviour and solubilization capacity of the microemulsion system were characterized, and nasal absorption of sildenafil from the microemulsion formulations was investigated in rabbits. Sildenafil displayed a high solubility of 124 mg/mL in the microemulsion consisting of 40% oleic acid, 10% H2O, and 50% Tween 80:ethanol (EA) (at a 1:4 weight ratio). Nasal absorption of sildenafil from this microemulsion was found to be fairly rapid. With a 10-mg dose, the onset of action was arrived instantly following intranasal administration and the duration was over 3 h using an in vivo rabbit studies. In addition, nasal ciliotoxicity studies were carried out using in vivo rat nasal mucosa model and showed no ciliotoxicity. Therefore, the prepared systems are no serious nasal ciliotoxicity for intranasal administration. The microemulsion system composed of oleic acid, Tween 80, EA, and water may be a practical approach for the rapid-onset delivery of sildenafil for the treatment of erectile dysfunction.
原文英語
頁(從 - 到)567-577
頁數11
期刊Xenobiotica
41
發行號7
DOIs
出版狀態已發佈 - 七月 2011

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology
  • Biochemistry
  • Health, Toxicology and Mutagenesis

指紋 深入研究「Rapid-onset sildenafil nasal spray carried by microemulsion systems: In vitro evaluation and in vivo pharmacokinetic studies in rabbits」主題。共同形成了獨特的指紋。

引用此