Design and evaluation of brimonidin-loaded nanostructure for enhanced ocular drug delivery in glaucoma treatment to maintain performance in a week and evaluation in goat’s eye
Leila Rezaei1 *, Shahla Mirzaeei2 , Fariba sheikhi shushtari3 , Shakib Naghshbandi3 , Ahmad Jahanbakhshi4
- Associate professor of ophthalmology ,Kermanshah university of medical science
- Pharmaceutical Sciences Research Center, Health Institute, Nano Drug Delivery Research Center, Health Technology Institute, Kermanshah University of Medical Sciences, Kermanshah, Iran
- Kermanshah university of medical science
- Kermanshah Army Hospital No.520
Abstract: Brimonidine tartrate (BRI) is a potent anti-glaucoma agent prescribed three times a day to control the IOP. Repetitive administration makes eye drop formulation of BRI less desired by patients and the fast elimination from the eye limited its intraocular bioavailability. This study aimed to design and develop sustained-release inserts of BRI to achieve an improved drug delivery.
Methods: Nanostructure ocular insert of BRI was fabricated of a drug-loaded polymeric solution. The developed inserts were subjected to stability, strength, and flexibility testing to ensure the integrity and non-irritancy during the administration. The morphology and mean diameter were observed using scanning electron microscopy and the drug-polymer interaction was assessed by Fourier transform infrared spectroscopy. The in vitro release of BRI from the insert was evaluated and its efficacy in reducing the IOP was investigated in the goat eye as an animal model. A single-dose administration of optimized nanofibrous insert as intervention was compared to the untreated eye as the control. Changes in IOP were reported.
Results: The fabricated inserts showed suitable physicochemical properties and morphology with a mean fiber diameter of <200 nm. A prolonged in vitro release during 4 days were observed for insert formulation. The insert formulation indicated efficacy in lowering the IOP for 8-days interval with a maximum 4-unit reduction in the IOP during the first 2 days.
Conclusion: Despite the commercial BRI eye drop, ocular insert had the advantage of a sustained release profile which could reduce the required frequency of administration. Accordingly, fabricated ocular inserts could be considered suitable for improving BRI ocular delivery and patient acceptance in treatment of glaucoma.
