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Brinzolamide Dimethyl Sulfoxide In Situ Gelling Ophthalmic Solution: Formulation Optimisation and In Vitro and In
Hemant Bhalerao1, K B Koteshwara2, Sajeev Chandran3
1Advanced Drug Delivery Systems R&D, Pharma Research, Lupin Limited, Lupin Research Park, 46/47A, Nande Village, Mulshi Taluka, Pune, 412115, India.
AAPS Pharmscitech
|January 18, 2020
Summary
A new in situ gelling eye drop formulation for brinzolamide (BRZ) offers sustained release for glaucoma treatment. This single daily dose matches the efficacy of multiple doses of commercial products, improving patient compliance.
Area of Science:
- Ophthalmology
- Pharmaceutics
- Materials Science
Background:
- Glaucoma treatment often requires frequent eye drop administration.
- Brinzolamide is a key medication for managing intraocular pressure (IOP).
- Improving drug delivery systems can enhance therapeutic outcomes and patient adherence.
Purpose of the Study:
- To develop a cost-effective, stable, sustained-release ophthalmic solution of brinzolamide (BRZ).
- To utilize an in situ gelling system for prolonged ocular residence time.
- To evaluate the efficacy and safety of the novel formulation compared to a commercial product.
Main Methods:
- Formulation of brinzolamide using dimethyl sulfoxide, polyoxyl 35 castor oil, polysorbate 80, and gellan gum as an in situ gelling agent.
- Optimization of formulation variables including drug concentration, solubilizer type/concentration, and gelling agent concentration.
- In vitro assessment of drug solubility, gelling properties, drug release kinetics, and gel stability.
- In vivo evaluation in New Zealand white rabbits for ocular toxicity and IOP reduction.
Main Results:
- The in situ gelling formulation demonstrated sustained drug release and prolonged ocular residence time (16-24 hours).
- Formulations were well-tolerated in rabbit models, showing no ocular toxicity.
- Significant reduction in intraocular pressure (IOP) was observed, from 25-28 mmHg to 12-14 mmHg.
- Mean residence time (MRT) of the test formulation (7.4-17.7 h) was significantly longer than Azopt® (4.9 h).
Conclusions:
- The developed in situ gelling formulation provides a viable and effective strategy for ocular brinzolamide delivery.
- Once-daily dosing achieved therapeutic endpoints comparable to multiple daily doses of commercial brinzolamide suspension.
- This approach offers potential for improved patient compliance and therapeutic management of glaucoma.
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