Non-ionic surfactants as novel intranasal absorption enhancers: in vitro and in vivo characterization

作者：Li, Ying; Li, Jinfeng; Zhang, Xin; Ding, Jiaojiao; Mao, Shirui^*

来源：Drug Delivery, 2016, 23(7): 2272-2279.

DOI：10.3109/10717544.2014.971196

• Absorption enhancer
• cremophor EL
• intranasal
• laurate sucrose ester
• poloxamer 188
• sumatriptan succinate

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.

• 出版日期2016-9
• 单位沈阳药科大学