Dj. Pillion et al., SYSTEMIC ABSORPTION OF INSULIN AND GLUCAGON APPLIED TOPICALLY TO THE EYES OF RATS AND A DIABETIC DOG, Journal of ocular pharmacology and therapeutics, 11(3), 1995, pp. 283-295
Nondiabetic rats were anesthetized with xylazine/ketamine to induce hy
perglycemia and systemic insulin absorption from eyedrops formulated w
ith dodecylmaltoside was quantitated by both a decrease in serum level
s of D-glucose and an increase in immunoreactive insulin levels. When
insulin eyedrop administration was delayed until 60 minutes after the
administration of eyedrops containing 0.25% dodecylmaltoside, the enha
nced systemic absorption of insulin was maintained, suggesting that do
decylmaltoside had an effect directly on the permeability of the nasal
sinus epithelium. When glucagon was formulated in eyedrops or nosedro
ps containing dodecylmaltoside, systemic absorption of glucagon could
be measured in the form of an increase in the serum D-glucose concentr
ation following nasal application, but not after ocular application. E
yedrops containing insulin plus 0.125% dodecylmaltoside were administe
red to a diabetic dog; a dose of 20 units of regular insulin caused a
modest decrease in serum D-glucose concentration and a concomitant inc
rease in serum immunoreactive insulin content. These results provide e
vidence that peptide drugs such as insulin can be formulated in eyedro
ps with low concentrations of dodecylmaltoside, a mild nonionic surfac
tant.