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

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)567-577
Number of pages11
JournalXenobiotica
Volume41
Issue number7
DOIs
Publication statusPublished - Jul 2011

Fingerprint

Nasal Sprays
Pharmacokinetics
Microemulsions
Polysorbates
Rabbits
Oleic Acid
Intranasal Administration
Nose
Ethanol
Nasal Mucosa
Erectile Dysfunction
Surface-Active Agents
Solubility
Phase behavior
Alcohols
Sildenafil Citrate
In Vitro Techniques
Rats
Weights and Measures
Water

Keywords

  • intranasal absorption
  • Microemulsion
  • oleic acid
  • sildenafil
  • Tween

ASJC Scopus subject areas

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

Cite this

Rapid-onset sildenafil nasal spray carried by microemulsion systems : In vitro evaluation and in vivo pharmacokinetic studies in rabbits. / Lu, Hsien-Tsung; Chen, Ray Neng; Sheu, Ming Thau; Chang, Chung Chiao; Chou, Po Yu; Ho, Hsiu O.

In: Xenobiotica, Vol. 41, No. 7, 07.2011, p. 567-577.

Research output: Contribution to journalArticle

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