Cyclosporin nanosphere formulation for ophthalmic administration

Khan, Wahid; Aldouby, Yanir; Avramoff, Avi; Domb, Abraham J.

doi:10.1016/j.ijpharm.2012.08.016

Cited by 27 publications

(17 citation statements)

References 7 publications

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“…44 Very interestingly, the proposed liposomal formulation showed significantly lower eye irritation compared with that of Restasis ® . A similar result was also supported by Khan et al 43 where a CsA nanosphere formulation had a significantly lower irritation effect than Restasis ® . The current study showed that there was no sign of changes in the conjunctiva, cornea, Peak drug concentration (μg CsA/mg tear).…”

Section: Ocular Irritation Testssupporting

confidence: 79%

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Supercritical fluid-mediated liposomes containing cyclosporin A for the treatment of dry eye syndrome in a rabbit model: comparative study with the conventional cyclosporin A emulsion

Karn¹,

Kim²,

Kang³

et al. 2014

IJN

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Background The objective of this study was to compare the efficacy of cyclosporin (CsA)-encapsulated liposomes with the commercially available CsA emulsion (Restasis ® ) for the treatment of dry eye syndrome in rabbits. Methods Liposomes containing CsA were prepared by the supercritical fluid (SCF) method consisted of phosphatidylcholine from soybean (SCF-S100) and egg lecithins (SCF-EPCS). An in vitro permeation study was carried out using artificial cellulose membrane in Franz diffusion cells. Dry eye syndrome was induced in male albino rabbits and further subdivided into untreated, Restasis ® -treated, EPCS, and S100-treated groups. Tear formation in the dry-eye-induced rabbits was evaluated using the Schirmer tear test. All formulations were also evaluated by ocular irritation tests using the Draize eye and winking methods with the determination of CsA concentration in rabbit tears. Results After the treatment, the Schirmer tear test value significantly improved in EPCS-treated ( P =0.005) and S100-treated ( P =0.018) groups compared to the Restasis ® -treated group. The AUC 0–24 h for rabbit’s tear film after the administration of SCF-S100 was 32.75±9.21 μg·h/mg which was significantly higher than that of 24.59±8.69 μg·h/mg reported with Restasis ® . Liposomal CsA formulations used in this study showed lower irritation in rabbit eyes compared with Restasis ® . Conclusion These results demonstrate that the novel SCF-mediated liposomal CsA promises a significant improvement in overcoming the challenges associated with the treatment of dry eyes.

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Section: Ocular Irritation Testssupporting

confidence: 79%

“…Ocular irritation of Restasis ® has already been reported by many groups. 11,43 Restasis ® is an oil-in-water emulsion which contains castor oil that causes irritation to the eyes.…”

Section: Ocular Irritation Testsmentioning

confidence: 99%

Supercritical fluid-mediated liposomes containing cyclosporin A for the treatment of dry eye syndrome in a rabbit model: comparative study with the conventional cyclosporin A emulsion

Karn¹,

Kim²,

Kang³

et al. 2014

IJN

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“…Development of different delivery mechanisms, such as aqueous preparations, have been explored to provide an increase in corneal drug tissue levels, bioavailability and tolerability. Indeed several studies exist in the literature comparing aqueous vehicles to the gold standard oil-based emulsion, Restasis [72–74]. …”

Section: Translational Prospectsmentioning

confidence: 99%

“…Using Schirmer testing and osmolarity measurements, they demonstrated no altering effects on ocular surface properties [75]. Another study by Khan et al using nanoparticle suspensions reported that CsA aqueous-based solutions may even be less irritating to the eye than lipophilic emulsions [74]. They found their aqueous suspension caused less local irritation with nearly the same penetrability of CsA compared directly to Restasis [74].…”

Section: Translational Prospectsmentioning

confidence: 99%

“…Another study by Khan et al using nanoparticle suspensions reported that CsA aqueous-based solutions may even be less irritating to the eye than lipophilic emulsions [74]. They found their aqueous suspension caused less local irritation with nearly the same penetrability of CsA compared directly to Restasis [74]. Their success was believed to be attributed to the use of triglycerides in the nanosuspension to replace the high concentrations of surfactants, a known eye irritant present in Restasis.…”

Section: Translational Prospectsmentioning

confidence: 99%

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Cyclosporine ophthalmic emulsions for the treatment of dry eye: a review of the clinical evidence

Ames

2015

Clinical Investigation

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Dry eye has gained recognition as a public health problem given its high prevalence, morbidity and cost implications. Although dry eye is common and affects patients’ quality of life, only one medication, cyclosporine 0.05% emulsion, has been approved by the US FDA for its treatment. In this review, we summarize the basic science and clinical data regarding the use of cyclosporine in the treatment of dry eye. Randomized controlled trials showed that cyclosporine emulsion outperformed vehicles in the majority of trials, consistently decreasing corneal staining and increasing Schirmer scores. Symptom improvement was more variable, however, with ocular dryness shown to be the most consistently improved symptom over vehicle.

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Nanomedicine for the Brain and the Eye: Disease Management in Poorly Accessible Compartments of the Body

Cattaneo

Gornati

Bernardini

et al. 2014

Handbook of Nanotoxicology, Nanomedicine and Stem Cell Use in Toxicology

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Cyclosporin nanosphere formulation for ophthalmic administration

Cited by 27 publications

References 7 publications

Supercritical fluid-mediated liposomes containing cyclosporin A for the treatment of dry eye syndrome in a rabbit model: comparative study with the conventional cyclosporin A emulsion

Supercritical fluid-mediated liposomes containing cyclosporin A for the treatment of dry eye syndrome in a rabbit model: comparative study with the conventional cyclosporin A emulsion

Cyclosporine ophthalmic emulsions for the treatment of dry eye: a review of the clinical evidence

Nanomedicine for the Brain and the Eye: Disease Management in Poorly Accessible Compartments of the Body

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