[Functional and pathological study of intranasal absorption of insulin aided by azone].
OBJECTIVE
To distinguish the different permeation function between sodium glycocholic acid (SGC) and Azone, and study the pathological changes induced by Azone on nasal mucosa.


METHODS
Insulin was given intravenouslly at the dose of 4.0 U. The blood samples were determined by radioimmunity method. SGC or Azone was administered respectively via nasal route with Insulin 270 U/ml. Insulin nasal drops 10 microL were given to each of rabbits via nasal route. The Azone 50 microL was administered via nasal route, t.i.d., lasted for 1 week and 3 months.


RESULTS
The level of blood Insulin was as follows: (3,954.47 +/- 644.47) mU/L, AUC = (1,264.87 +/- 148.00) mU.L-1.min-1 x 10(-3) in i.v. group; (740.44 +/- 94.16) mU/L, AUC = (298.02 +/- 63) mU.L-1.min-1 x 10(-3) in SGC group; (908.18 +/- 201.19) mU/L, AUC = (596.92 +/- 84.00) mU.L-1.min-1 x 10(-3) in Azone group. The bioavailability was 23.56% and 47.19% respectively. The pathological changes included cilia detachment from epithelium, glandular hypertrophy and connective tissue proliferation.


CONCLUSIONS
It was found that Azone was an excellent permeation enhance which promoted more Insulin to be absorbed into blood stream through nasal mucosa. However, Azone also damaged the nasal mucosa in the view of pathology.
Hou
Tiening
T
Department of Otorhinolaryngology Head and Neck Surgery, Affiliated SIR RUN RUN SHAW Hospital, Zhejiang University, Hangzhou 310016, China. Houtiening@mail.hz.zj.cn
Xin
Weihong
W
Dong
Zhen
Z
D000042:Absorption; D000281:Administration, Intranasal; D000818:Animals; D001381:Azepines / Q000494:pharmacology*; D005260:Female; D007328:Insulin / Q000493:pharmacokinetics*; D008297:Male; D009297:Nasal Mucosa / Q000378:metabolism / Q000473:pathology; D011817:Rabbits
D001381:Azepines; D007328:Insulin