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Topical ocular delivery of NSAIDs
Munish Ahuja1, Avinash S Dhake, Surendra K Sharma
1Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science & Technology, Hisar, 125 001, Haryana, India.
The AAPS Journal
|April 26, 2008
Summary
Nonsteroidal anti-inflammatory drugs (NSAIDs) are used for eye inflammation. Formulating non-irritating ophthalmic NSAID solutions involves careful selection of salts, solubilizers, and pH to improve ocular penetration and efficacy.
Area of Science:
- Ophthalmology
- Pharmacology
- Drug Delivery
Background:
- Prostaglandins, derived from arachidonic acid metabolism by cyclooxygenase (COX), are key mediators of ocular inflammation.
- Nonsteroidal anti-inflammatory drugs (NSAIDs), acting as COX inhibitors, are employed to manage inflammatory eye conditions.
- Topical ophthalmic NSAIDs include various chemical derivatives, presenting formulation challenges due to poor water solubility and acidic nature.
Purpose of the Study:
- To review formulation strategies for nonsteroidal anti-inflammatory drugs (NSAIDs) in ophthalmic preparations.
- To address challenges in achieving adequate ocular penetration, stability, and minimizing irritation with ophthalmic NSAIDs.
- To explore advanced delivery systems and specific drug choices for enhanced efficacy in ocular inflammation treatment.
Main Methods:
- Analysis of NSAID physicochemical properties (pKa, solubility) relevant to ophthalmic formulations.
- Evaluation of solubilization techniques: salt formation, complexation with cyclodextrins, and use of solubilizers.
- Review of excipient compatibility (e.g., benzalkonium chloride, polysorbate 80, tromethamine) and potential ocular irritants (e.g., lysine salts).
Main Results:
- Aqueous ophthalmic NSAID solutions can be formulated using water-soluble salts, cyclodextrins, or tromethamine in mildly acidified water.
- Strategies exist to overcome NSAID incompatibility with preservatives like benzalkonium chloride.
- Alternative delivery systems like oil drops and ointments offer options for insoluble drugs or sustained release, while suspensions and inserts may cause irritation.
Conclusions:
- Non-irritating ophthalmic NSAID solutions can be achieved through careful formulation, considering pH, excipients, and drug solubility.
- Prodrugs have shown limited success due to incomplete hydrolysis; advanced formulations like nanoparticles and specific agents (e.g., bromfenac) show promise.
- Optimizing NSAID delivery systems is crucial for effective management of ocular inflammatory disorders.
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