CriticalSorb™: A novel efficient nasal delivery system for human growth hormone based on Solutol HS15

The absorption enhancing efficiency of CriticalSorb (TM) for human growth hormone ( MW 22 kDa) was investigated in the conscious rat model. The principle absorption enhancing component of CriticalSorb (TM), Solutol (R) HS15, comprises polyglycol mono- and di-esters of 12-hydroxystearic acid combined with free polyethylene glycol. When administering hGH nasally in rats with increasing concentrations of Solutol (R) HS15, it was found that for a 10% w/v solution formulation a bioavailability of 49% was obtained in the first 2 h after administration. Furthermore it was shown that the most effective ratio of Solutol (R) HS15 to hGH was 4: 1 on a mg to mg basis. Histopathology studies in rats after 5 days repeated nasal administration showed that Solutol (R) HS15 had no toxic effect on the nasal mucosa. These results have been confirmed in a 6 month repeat nasal toxicity study in rats. It can be concluded that the principle absorption enhancing component of CriticalSorb (TM) Solutol (R) HS15 - is a potent and non- toxic nasal absorption enhancer that warrants further development. (C) 2012 Elsevier B. V. All rights reserved.