Ocular Surface Distribution and Pharmacokinetics of a Novel Ophthalmic 1% Azithromycin Formulation

Akpek, Esen K.; Vittitow, Jason L; Verhoeven, Rozemarijn S; Brubaker, K.; Amar, Thierry; Powell, Kendall D.; Boyer, José L.; Crean, Christopher S.

doi:10.1089/jop.2009.0026

Cited by 69 publications

(56 citation statements)

References 17 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…To the best of our knowledge, there is no published study assessing the efficacy of Azyter ® in blepharitis. Although most of the studies that evaluate azithromycin in blepharitis used AzaSite ® (Inspire Pharmaceuticals, Inc, Durham, NC, USA), our results are comparable (8,1921) . AzaSite ® is …”

supporting

confidence: 51%

Azithromycin 1.5% ophthalmic solution: efficacy and treatment modalities in chronic blepharitis

Fadlallah¹,

Rami²,

Fahd³

et al. 2012

Arq. Bras. Oftalmol.

View full text Add to dashboard Cite

Purpose: To assess the efficacy of topical 1.5% azithromycin in the treatment of mo derate to severe chronic blepharitis and to compare the efficacy of two different treatment modalities. Methods: A randomized clinical trial included 67 patients with chronic anterior and/or posterior blepharitis, followedup for 3 months. Signs and symptoms were graded according to severity. Patients were randomized into two groups: 33 patients in group I and 34 patients in group II. Group I patients were treated with topical 1.5% azithromycin twice a day for three days, and Group II patients were treated with topical 1.5% azithromycin twice a day for three days then at bedtime for the rest of the month. All patients were instructed to apply warm compresses and an eyefriendly soap twice daily. Results: Patients in both groups tolerated the treatment with minimal irritation. A signi ficant improvement in signs and symptoms was noted at the one week fol lowup visit. Group II showed a more pronounced and longerlasting improvement that persisted after three months of followup. Conclusion: Topical 1.5% azithromycin ophthalmic solution is an effective treat ment option for chronic blepharitis. In moderate to severe blepharitis, a one month treatment is safe and shows better improvement than the threeday protocol with no significant relapse until three months of followup.

show abstract

supporting

confidence: 51%

Azithromycin 1.5% ophthalmic solution: efficacy and treatment modalities in chronic blepharitis

Fadlallah¹,

Rami²,

Fahd³

et al. 2012

Arq. Bras. Oftalmol.

View full text Add to dashboard Cite

show abstract

“…14) Following the U.S. Food and Drug Administration (FDA)-approved regimen of 1 drop twice daily for 2 d followed by 1 drop daily for 5 d, topical azithromycin reached a maximum concentration of 180 µg/g of tissue in the rabbit eyelid. 15) However, our LC-MS-based bioanalysis revealed that azithromycin concentration in the meibomian glands was sub-inhibitory at 0.8 µg/g tissue after a single instillation. This is probably because our protocol enabled precise meibomian gland collection without surface contamination, resulting in much lower concentrations.…”

Section: Discussionmentioning

confidence: 79%

Limited Azithromycin Localization to Rabbit Meibomian Glands Revealed by LC-MS-Based Bioanalysis and DESI Imaging

Asano

Wiseman

Tsuji

et al. 2017

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

Meibomian gland dysfunction (MGD) is the leading cause of dry eye, and although it affects approximately 4% of the population, treatment options remain limited. Topical azithromycin is one of the most promising pharmacological agents because of its multiple mechanisms of action and long sustainability. Azithromycin is frequently used as an off-label medication in the U.S. However, although azithromycin is presumed to act directly on meibomian gland cells, the mechanisms of action that contribute to its clinical efficacy remain unclear because no studies using a pharmacokinetic approach have been performed. Therefore, we aimed to clarify whether topical azithromycin reaches the meibomian glands sufficiently to generate a biological effect. We measured azithromycin concentrations in rabbit meibomian glands collected using a recently developed method. Moreover, we also visualized the azithromycin micro-distribution using desorption electrospray ionization (DESI) imaging. Azithromycin concentration in the meibomian glands reached only 0.8 µg/g tissue following a single application of a 1% azithromycin ophthalmic solution and was 1000-fold lower than the concentration in conjunctival epithelium. Similarly, no signal was observed in the meibomian glands on DESI images. Our results clearly demonstrated that topical azithromycin had limited access to the meibomian glands and was predominantly distributed in ocular surface tissues such as the palpebral conjunctiva and lid margins. These findings provide new insight into the clinical responses to topical azithromycin therapy and will aid in the further development of effective drugs with more suitable pharmacokinetic properties.Key words meibomian gland; azithromycin; distribution; MS imaging; eye drop Meibomian glands are sebaceous glands embedded within specific types of dense connective tissue in the eyelid. They are primarily responsible for producing meibomian oil (meibum), which plays a physiologically important role in promoting tear film stability and preventing aqueous tear evaporation on the ocular surface.1) Meibomian gland blockages are clinically defined as meibomian gland dysfunction (MGD), which is the leading cause of dry eye disease. However, there is no pharmacologically approved drug useful in treating MGD. Azithromycin ophthalmic solution (AzaSite ® ; InSite Vision, a SUN PHARMA company, Alameda, CA, U.S.A.) is one of the most promising candidates for MGD treatment. 2)Although it has been approved only for the treatment of bacterial conjunctivitis, off-label application of topical azithromycin is the most commonly used pharmaceutical treatment in the U.S. for the management of MGD.3) In addition to its broad anti-bacterial spectrum, azithromycin inhibits pro-inflammatory cytokines and restores lipid properties. Indeed, several clinical studies have demonstrated that topical azithromycin ophthalmic solution significantly relieved the clinical signs and symptoms of MGD.4-6) Although significant progress has been made in human clinical studies to better u...

show abstract

“…Various treatment options for MGD including the LipiFlow instrument, intense pulsed light, eyelid-warming devices, intraductal probing, as well as topical or oral application of drugs have been developed [11][12][13][14][15][16][17][18][19]. Our present results regarding additional instruction by nurses for improving the outcome of treatment with the Azuki-no-chikara eyelid-warming device may also be applicable to other treatment approaches.…”

Section: Resultsmentioning

confidence: 97%

Additional Instruction by a Nurse Enhanced the Effect of Eyelid Warming on Subjective Symptoms in Patients with Meibomian Gland Dysfunction

T¹,

Ideta²,

Mera³

et al. 2018

J Healthc Commun

View full text Add to dashboard Cite

show abstract

Ocular Surface Distribution and Pharmacokinetics of a Novel Ophthalmic 1% Azithromycin Formulation

Cited by 69 publications

References 17 publications

Azithromycin 1.5% ophthalmic solution: efficacy and treatment modalities in chronic blepharitis

Azithromycin 1.5% ophthalmic solution: efficacy and treatment modalities in chronic blepharitis

Limited Azithromycin Localization to Rabbit Meibomian Glands Revealed by LC-MS-Based Bioanalysis and DESI Imaging

Additional Instruction by a Nurse Enhanced the Effect of Eyelid Warming on Subjective Symptoms in Patients with Meibomian Gland Dysfunction

Contact Info

Product

Resources

About