Ocular Distribution of Difluprednate Ophthalmic Emulsion 0.05% in Rabbits

Tajika, Tetsuya; Isowaki, Akiharu; Sakaki, Hideyuki

doi:10.1089/jop.2010.0093

Cited by 47 publications

(33 citation statements)

References 16 publications

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“…The half-life (T 1/2 ) reported in the aqueous humor, conjunctiva, and cornea [13] was similar to the present results.…”

Section: Discussionsupporting

confidence: 91%

“…T max in both studies was similar in aqueous humor, in spite of having used different methods of quantification [13, 16]. In the present data, T max was similar in aqueous humor according to mentioned below.…”

Section: Discussionsupporting

confidence: 73%

“…However, several factors are involved in ophthalmic drug efficacy, diffusion and distribution to targeted ocular tissues are of the most important [11, 12]. Due to its chemical structure, difluprednate ophthalmic emulsion has a high lipophilicity, which facilitates passage through the membranes, allowing a significant distribution to the anterior and posterior segments, unlike early generations of corticosteroids [13], and clinical efficacy in medical settings [14, 15]. …”

Section: Discussionmentioning

confidence: 99%

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Bioavailability of generic 0.05% difluprednate emulsion in the aqueous humor, cornea, and conjunctiva of New Zealand rabbits after a single dose compared with commercial difluprednate

Mercado-Sesma

Contreras-Rubio

Baiza-Durán

et al. 2017

J Ophthal Inflamm Infect

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BackgroundTo determine the concentration after a single dose of generic 0.05% difluprednate and commercial difluprednate in the aqueous humor, cornea, and conjunctiva of New Zealand rabbits, a preclinical study in 72 male New Zealand white rabbits was performed. A single dose (50 μL) of two 0.05% difluprednate ophthalmic formulations was instilled in both eyes. Conjunctiva, cornea, and aqueous humor samples were collected at nine time points over 8 h (four animals per time point). The active metabolite of difluprednate, 17-difluoroprednisolone-butyrate (DFB), concentrations was quantified using HPLC.ResultsMeasurable levels of DFB were quantified in all three ocular tissues. After a single instillation, the highest concentration of difluprednate was found between 30 and 60 min in the conjunctiva, cornea, and aqueous humor, respectively. There was no significant difference between both formulations in any tissue at any time point. After 3 h, no metabolites of either emulsion were found in any tissue.ConclusionsDifluprednate penetrates into different ocular tissues. Generic difluprednate has a similar pharmacokinetic profile compared with commercial difluprednate.

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“…The half-life (T 1/2 ) reported in the aqueous humor, conjunctiva, and cornea [13] was similar to the present results.…”

Section: Discussionsupporting

confidence: 91%

Section: Discussionsupporting

confidence: 73%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Bioavailability of generic 0.05% difluprednate emulsion in the aqueous humor, cornea, and conjunctiva of New Zealand rabbits after a single dose compared with commercial difluprednate

Mercado-Sesma

Contreras-Rubio

Baiza-Durán

et al. 2017

J Ophthal Inflamm Infect

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“…In a recent study, Tajika et al [28] demonstrated improved anti-inflammatory activity of prednisolone derivative, 0.05% [ 3 H] difluprednate, with emulsion as vehicle. Results confirmed that in the rabbit eye, emulsion could deliver drug to the anterior ocular tissues with small amount of drug reaching posterior tissues following single and multiple topical drop instillation.…”

Section: Conventional Ocular Drug Delivery Systemsmentioning

confidence: 99%

Ocular drug delivery systems: An overview

Patel

Cholkar

Agrahari

et al. 2013

WJP

700

552

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The major challenge faced by today’s pharmacologist and formulation scientist is ocular drug delivery. Topical eye drop is the most convenient and patient compliant route of drug administration, especially for the treatment of anterior segment diseases. Delivery of drugs to the targeted ocular tissues is restricted by various precorneal, dynamic and static ocular barriers. Also, therapeutic drug levels are not maintained for longer duration in target tissues. In the past two decades, ocular drug delivery research acceleratedly advanced towards developing a novel, safe and patient compliant formulation and drug delivery devices/techniques, which may surpass these barriers and maintain drug levels in tissues. Anterior segment drug delivery advances are witnessed by modulation of conventional topical solutions with permeation and viscosity enhancers. Also, it includes development of conventional topical formulations such as suspensions, emulsions and ointments. Various nanoformulations have also been introduced for anterior segment ocular drug delivery. On the other hand, for posterior ocular delivery, research has been immensely focused towards development of drug releasing devices and nanoformulations for treating chronic vitreoretinal diseases. These novel devices and/or formulations may help to surpass ocular barriers and associated side effects with conventional topical drops. Also, these novel devices and/or formulations are easy to formulate, no/negligibly irritating, possess high precorneal residence time, sustain the drug release, and enhance ocular bioavailability of therapeutics. An update of current research advancement in ocular drug delivery necessitates and helps drug delivery scientists to modulate their think process and develop novel and safe drug delivery strategies. Current review intends to summarize the existing conventional formulations for ocular delivery and their advancements followed by current nanotechnology based formulation developments. Also, recent developments with other ocular drug delivery strategies employing in situ gels, implants, contact lens and microneedles have been discussed.

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“…COX-2 is the primary mediator of ocular inflammation [6] and, therefore, is an ideal target of inhibition by ophthalmic medication. Bromfenac is the strongest ophthalmic nonsteroidal anti-inflammatory drug (NSAID) in terms of COX-2 inhibition [7,8,9]. …”

Section: Introductionmentioning

confidence: 99%

Bromfenac Sodium 0.1%, Fluorometholone 0.1% and Dexamethasone 0.1% for Control of Ocular Inflammation and Prevention of Cystoid Macular Edema after Phacoemulsification

Wang

Yao²,

Xu³

et al. 2013

Ophthalmologica

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Purpose: To compare bromfenac sodium 0.1%, fluorometholone 0.1% and dexamethasone 0.1% for the control of postoperative inflammation and prevention of cystoid macular edema (CME) after phacoemulsification. Methods: Patients were randomized to receive bromfenac sodium 0.1% for 1 month (OBS1) or 2 months (OBS2), or fluorometholone 0.1% for 1 month (OFM) or dexamethasone 0.1% for 1 month (ODM). Best-corrected visual acuity, intraocular pressure, endothelial cell density, photon count value and retinal foveal thickness were measured. Results: Mean photon count values were lower in the OBS1 and OBS2 groups compared with the ODM group during the first week. Bromfenac sodium cleared the ocular inflammation more rapidly than fluorometholone and dexamethasone. The foveal thickness was thinner in the second month and the incidence of CME was lower in the OBS1 and OBS2 groups compared with the OFM and ODM groups. Conclusion: Bromfenac sodium was more effective and safer than fluorometholone and dexamethasone as an anti-inflammatory, decreasing macular thickness and preventing CME in age-related cataract patients after cataract surgery.

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Ocular Distribution of Difluprednate Ophthalmic Emulsion 0.05% in Rabbits

Cited by 47 publications

References 16 publications

Bioavailability of generic 0.05% difluprednate emulsion in the aqueous humor, cornea, and conjunctiva of New Zealand rabbits after a single dose compared with commercial difluprednate

Bioavailability of generic 0.05% difluprednate emulsion in the aqueous humor, cornea, and conjunctiva of New Zealand rabbits after a single dose compared with commercial difluprednate

Ocular drug delivery systems: An overview

Bromfenac Sodium 0.1%, Fluorometholone 0.1% and Dexamethasone 0.1% for Control of Ocular Inflammation and Prevention of Cystoid Macular Edema after Phacoemulsification

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