Effects of absorption enhancers on human nasal tissue ciliary movement in vitro.
Sodium taurodihydrofusidate (STDHF) is one of the most promising absorption enhancers for nasal delivery of peptide drugs. Drugs and additives in nasal formulations should not interfere with the self-cleaning capacity of the nose by the ciliary epithelium. Measured in vitro on human adenoid tissue with a photoelectric method, STDHF was found to induce ciliostasis at concentrations of 0.3% (w/v) and higher. STDHF (0.3%) is less ciliostatic than laureth-9 (0.3%) or deoxycholate (0.3%). Glyco- and taurocholate (0.3%) show only very mild effects on nasal ciliary movement. Human insulin (1%) has no ciliostatic potency in vitro, whereas a combination of human insulin (1%) and STDHF (1%) is ciliostatic but not as potent as STDHF (1%) alone.
Hermens
W A
WA
Department Clinical Pharmacy and Toxicology, Maasland Hospital, Sittard, The Netherlands.
Hooymans
P M
PM
Verhoef
J C
JC
Merkus
F W
FW
D000042:Absorption; D000234:Adenoids / Q000166:cytology / Q000187:drug effects; D000277:Adjuvants, Pharmaceutic / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005672:Fusidic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007328:Insulin / Q000494:pharmacology; D008823:Micelles; D009079:Mucociliary Clearance / Q000187:drug effects*; D009297:Nasal Mucosa / Q000166:cytology / Q000187:drug effects*
D000277:Adjuvants, Pharmaceutic; D007328:Insulin; D008823:Micelles; D005672:Fusidic Acid; C053824:tauro-24,25-dihydrofusidate