Effect of Citric Acid and Tromethamine on the Stability of Eyedrops Containing Lifitegrast

Lifitegrast is an effective treatment for dry eye disease, reducing inflammation and improving the ocular surface condition. Owing to its high sensitivity to oxidation and hydrolysis, formulation studies are required to maintain the physicochemical stability of lifitegrast. This study aimed to overc...

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Bibliographic Details
Published in:Pharmaceuticals (Basel, Switzerland) Switzerland), 2024-10, Vol.17 (11), p.1415
Main Authors: Jeong, Ji-Su, Ha, Eun-Sol, Park, Heejun, Lee, Seon-Kwang, Kang, Hui-Taek, Kim, Min-Soo
Format: Article
Language:English
Subjects:
Acids
Antioxidants
Care and treatment
Citric acid
Complications and side effects
Design of experiments
Diagnosis
Dosage and administration
Drug therapy
dry eye disease
Dry eye syndromes
Eye diseases
eyedrop formulation
FDA approval
Inflammation
lifitegrast
Oxidation
Oxidative stress
physicochemical stability
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Summary:Lifitegrast is an effective treatment for dry eye disease, reducing inflammation and improving the ocular surface condition. Owing to its high sensitivity to oxidation and hydrolysis, formulation studies are required to maintain the physicochemical stability of lifitegrast. This study aimed to overcome the instability of lifitegrast by developing a more stable eyedrop formulation by using citric acid and tromethamine to prevent the degradation of lifitegrast. Based on the Design of Experiment (DoE) approach, formulations were prepared at various concentrations of two stabilizers, citric acid and tromethamine. The stabilizers were carefully controlled to reduce the generation of degradation products. The eyedrops were stored under accelerated test conditions, and parameters such as appearance, pH, drug content, and impurities were evaluated. The results showed that all critical quality attributes (CQAs) including appearance, pH, drug content, and impurities were maintained at stable levels under accelerated conditions, meeting established criteria. In addition, it was suggested that citric acid provided protection against oxidative stress, while tromethamine prevented hydrolysis caused by pH fluctuations. Consequently, it was concluded that the developed lifitegrast-containing eyedrop formulation exhibited improved physicochemical stability, validated through statistical analyses. These findings contribute to the development of stable eyedrops and provide a foundation for commercial production and clinical applications.
ISSN:1424-8247
1424-8247
DOI:10.3390/ph17111415