Abstract
Glibenclamide (GL)-loaded microcapsules (MC) and transdermal patches (TDP) were formulated and
in vitro
and
in vivo
parameters compared to find out the best route of drug administration. The formulation TDP1 having a drug–polymer ratio 1:1 showed comparatively higher GL release and better permeation across mice skin (
p
< 0.05). From the comparative study, it was concluded that the transdermal system of GL produced better improvement compared to oral microcapsule administration (
p
< 0.05). The transdermal system exhibited comparatively slow and continuous supply of GL at a desired rate to systemic circulation avoiding metabolism, which improved day-to-day glycemic control in diabetic subjects. Transdermal system of GL exhibited better control of hyperglycemia and prolonged plasma half-life by transdermal systems (9.6 ± 1.2 h) in comparison with oral microcapsule (5.84 ± 2.1 h), indicating that the drug, when administered by transdermal systems, will remain in the body for a longer period. From the glucose tolerance test, transdermal route effectively maintained the normoglycemic levels in contrast to the oral group (MC1), which produced remarkable hypoglycemia ranging from −12.6 ± 2.1% to −18 ± 2.3%. The significantly high (
p
< 0.05) area under the curve values observed with transdermal system (1,346.2 ± 92.3 ng ml
−1
h
−1
) also indicate increased bioavailability of the drug from these systems compared to the oral route (829.8 ± 76.4 ng ml
−1
h
−1
).