title: Non-ionic surfactants as novel intranasal absorption enhancers: in vitro and in vivo characterization.
abstract: OBJECTIVE
  To explore the potential of non-ionic surfactants as novel intranasal absorption enhancers.
  
  
  METHODS
  Taking sumatriptan succinate (SMS) as a model drug, influence of different non-ionic surfactants, including laurate sucrose ester (SE), cremophor EL and poloxamer 188, on the intranasal absorption of SMS was investigated using an in situ nasal perfusion technique in rats. Ciliotoxicity of the non-ionic surfactants was evaluated using an in situ toad palate model. In vivo behavior of the selected formulations was studied in rats.
  
  
  RESULTS
  All the non-ionic surfactants investigated increased the intranasal absorption of SMS remarkably but with varied extent and trend. Moreover, it was revealed that at the same concentration, laurate SE had better permeation-enhancing effect than that of cremophor EL and poloxamer 188. The ciliotoxicity results showed that all the non-ionic surfactants were regarded as safe at selected concentrations. Based on the in situ absorption data and ciliotoxicity results, the following three samples, 0.5% laurate SE, 0.1% cremophor EL and 0.5% poloxamer 188 were selected for in vivo absorption studies in rats. Among them, 0.5% laurate SE group presented the highest enhancing effect, followed by 0.1% cremophor EL and 0.5% poloxamer 188 group, with absolute bioavailability 29.99%, 22.64% and 20.90%, respectively.
  
  
  CONCLUSIONS
  Laurate SE is a promising intranasal absorption enhancer.
authors.affiliation: a School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , People's Republic of China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Li
authors.affiliation: a School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , People's Republic of China.
authors.forename: Jinfeng
authors.initials: J
authors.lastname: Li
authors.affiliation: a School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , People's Republic of China.
authors.forename: Xin
authors.initials: X
authors.lastname: Zhang
authors.affiliation: a School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , People's Republic of China.
authors.forename: Jiaojiao
authors.initials: J
authors.lastname: Ding
authors.affiliation: a School of Pharmacy , Shenyang Pharmaceutical University , Shenyang , People's Republic of China.
authors.forename: Shirui
authors.initials: S
authors.lastname: Mao
mesh_terms: D000281:Administration, Intranasal / Q000379:methods; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005990:Glycerol / Q000031:analogs & derivatives / Q000737:chemistry; D007848:Laurates / Q000737:chemistry; D008297:Male; D065588:Nasal Absorption / Q000187:drug effects*; D009297:Nasal Mucosa / Q000378:metabolism; D020442:Poloxamer / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D018170:Sumatriptan / Q000737:chemistry* / Q000378:metabolism; D013501:Surface-Active Agents / Q000737:chemistry*
chemical_list: D007848:Laurates; D013501:Surface-Active Agents; D020442:Poloxamer; C000515:cremophor EL; D018170:Sumatriptan; D005990:Glycerol
keywords: Absorption enhancer; cremophor EL; intranasal; laurate sucrose ester; poloxamer 188; sumatriptan succinate