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Cited by 225Advanced Drug Delivery SystemsDrug Solubulity and Delivery SystemsInflammatory mediators and NSAID effects

Topical ocular delivery of NSAIDs

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Ahuja, Munish, Dhake, Avinash S., Sharma, Surendra K., Majumdar, Dipak K.·2008·The AAPS Journal
DOI 10.1208/s12248-008-9024-9PMC PMC2751374
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Abstract

In ocular tissue, arachidonic acid is metabolized by cyclooxygenase to prostaglandins which are the most important lipid derived mediators of inflammation. Presently nonsteroidal anti-inflammatory drugs (NSAIDs) which are cyclooxygenase (COX) inhibitors are being used for the treatment of inflammatory disorders. NSAIDs used in ophthalmology, topically, are salicylic-, indole acetic-, aryl acetic-, aryl propionic- and enolic acid derivatives. NSAIDs are weak acids with pKa mostly between 3.5 and 4.5, and are poorly soluble in water. Aqueous ophthalmic solutions of NSAIDs have been made using sodium, potassium, tromethamine and lysine salts or complexing with cyclodextrins/solubilizer. Ocular penetration of NSAID demands an acidic ophthalmic solution where cyclodextrin could prevent precipitation of drug and minimize its ocular irritation potential. The incompatibility of NSAID with benzalkonium chloride is avoided by using polysorbate 80, cyclodextrins or tromethamine. Lysine salts and alpha-tocopheryl polyethylene glycol succinate disrupt corneal integrity, and their use requires caution. Thus a nonirritating ophthalmic solution of NSAID could be formulated by dissolving an appropriate water-soluble salt, in the presence of cyclodextrin or tromethamine (if needed) in mildly acidified purified water (if stability permits) with or without benzalkonium chloride and polyvinyl alcohol. Amide prodrugs met with mixed success due to incomplete intraocular hydrolysis. Suspension and ocular inserts appear irritating to the inflamed eye. Oil drop may be a suitable option for insoluble drugs and ointment may be used for sustained effect. Recent studies showed that the use of colloidal nanoparticle formulations and the potent COX 2 inhibitor bromfenac may enhance NSAID efficacy in eye preparations.

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  • Hydrophobic NSAIDs such as indomethacin, ibuprofen, and diclofenac fail to achieve sufficient therapeutic effects in patients despite in-vitro pharmacological effectiveness, due to low solubility and inadequate retention at the ocular lesion.

    “Although in-vitro studies have demonstrated their pharmacological effectiveness, clinical trials suggest that they fail to achieve sufficient therapeutic effects in patients [4].”

    From From design to Deployment: The innovative role of nanomicelles in targeted ophthalmic therapeutics (2025) · cites this paper as [4]

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Authors
Ahuja, M., Dhake, A. S., Sharma, S. K., & Majumdar, D. K.
Affiliations
  • Guru Jambheshwar University of Science and Technology (IN)
  • University of Delhi (IN)
Corresponding author
Majumdar, Dipak K.
ORCID
Venue
The AAPS Journal
Publisher
Springer Science and Business Media LLC
Published
2008-04-25
Volume
10
Issue
2
Pages
229-41
ISSN
1550-7416 (ISSN-L)
DOI
10.1208/s12248-008-9024-9
PMC
PMC2751374
OpenAlex
W2015117635
Cited by
225
References
100
Citations by year
2026: 4 · 2025: 11 · 2024: 13 · 2023: 11 · 2022: 13 · 2021: 13 · 2020: 19 · 2019: 26 · 2018: 16 · 2017: 10 · 2016: 14 · 2015: 21 · 2014: 12 · 2013: 13 · 2012: 10
FWCI
0.50
Type
journal article
Language
en
Open access
Licence
Locations
  • The AAPS Journal (publishedVersion, cc-by-nc)
  • PubMed Central (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Health Sciences › Medicine › Pharmacology › Inflammatory mediators and NSAID effects
Keywords
topical ocular drug delivery, nonsteroidal anti-inflammatory drugs, cyclooxygenase inhibitors, arachidonic acid metabolism, prostaglandins, ocular inflammation, ophthalmic preparations, cyclodextrins, tromethamine, drug solubilization, benzalkonium chloride, Tween 80, colloidal nanoparticles, bromfenac, ocular penetration, eye irritation
MeSH terms
Administration, Topical, Animals, Anti-Inflammatory Agents, Non-Steroidal, Cyclodextrins, Drug Carriers, Eye, Eye Diseases, Humans, Ophthalmic Solutions, Molecular Structure, Nanoparticles

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