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Glucagon administration to the rat via eye drops
D J Pillion1, D L McCracken, M Yang
1Department of Pharmacology, University of Alabama, Birmingham.
Summary
Glucagon eye drops with saponin significantly increased blood sugar in rats. Other emulsants were ineffective, highlighting the critical role of the emulsant in systemic glucagon absorption via the eye.
Area of Science:
- Ophthalmology
- Endocrinology
- Pharmacology
Background:
- Systemic absorption of medications via ocular delivery is an area of interest.
- Glucagon is a hormone that elevates blood glucose levels.
- The efficacy of ocular drug delivery depends on formulation, including the use of emulsants.
Purpose of the Study:
- To investigate the systemic absorption of glucagon delivered via eye drops in rats.
- To determine the effect of different emulsants on glucagon absorption and its hyperglycemic action.
Main Methods:
- Anesthetized rats received glucagon (0.03 mg) in eye drops with either buffered saline, saponin, Brij78, or BL-9.
- Blood D-glucose concentrations and immunoreactive glucagon levels were measured over time.
- Different concentrations of emulsants were tested.
Main Results:
- Glucagon in buffered saline did not cause hyperglycemia.
- Eye drops containing 0.25% saponin induced a rapid, dose-dependent increase in blood D-glucose.
- Maximal absorption occurred at 20 minutes, returning to baseline by 60 minutes.
- Immunoreactive glucagon levels increased 2.4-fold with saponin.
- Brij78 and BL-9 as emulsants were ineffective for glucagon absorption.
Conclusions:
- Systemic absorption of glucagon from eye drops is feasible in rats.
- Saponin acts as an effective emulsant for enhancing ocular glucagon absorption.
- The choice of emulsant is critical for successful systemic delivery of glucagon via eye drops.