Formulation of an ophthalmic lipid emulsion containing an anti-inflammatory steroidal drug, difluprednate

Abstract:Transport of drugs applied by traditional dosage forms is restricted to the eye, and therapeutic drug concentrations in the target tissues are not maintained for a long duration since the eyes are protected by a unique anatomy and physiology. For the treatment of the anterior segment of the eye, various droppable products to prolong the retention time on the ocular surface have been introduced in the market. On the other hand, direct intravitreal implants, using biodegradable or non-biodegradable polymer technology, have been widely investigated for the treatment of chronic vitreoretinal diseases. There is urgent need to develop ocular drug delivery systems which provide controlled release for the treatment of chronic diseases, and increase patient's and doctor's convenience to reduce the dosing frequency and invasive treatment. In this article, progress of ocular drug delivery systems under clinical trials and in late experimental stage is reviewed.

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“…Difluprednate emulsion clears these problems, and can more easily penetrate into intraocular tissues compared with its suspension [153].…”

Section: Eye-dropsmentioning

confidence: 99%

Recent Advances in Ocular Drug Delivery Systems

2011

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“…6 Its anti-inflammatory activity is further augmented by replacing the 17-hydroxyl group with butyrate, while its lipophilicity -and hence corneal penetration -is enhanced by substituting the 21-hydroxyl group with acetate. 7 Given the paucity of strong ophthalmic steroids available, difluprednate was formulated as a topical ophthalmic preparation.…”

Section: Review Of Pharmacology Formulation Pharmacokinetics and Imentioning

confidence: 99%

“…Yet another obstacle is that particle variance precludes ophthalmic suspensions from undergoing a filtration technique of sterilization. 7 One elegant solution to these problems is to create an oil-in-water lipid emulsion. This allows drugs that are poorly water soluble to dissolve in the oil phase (which does not have uniformity problems), undergo sterile filtration, and provide better ocular bioavailability.…”

Section: Review Of Pharmacology Formulation Pharmacokinetics and Imentioning

confidence: 99%

“…This allows drugs that are poorly water soluble to dissolve in the oil phase (which does not have uniformity problems), undergo sterile filtration, and provide better ocular bioavailability. 7 As mentioned above, lipid emulsions also require the addition of surfactants, and both high concentrations of these agents and the use of ionic varieties can lead to ocular toxicity.…”

Section: Review Of Pharmacology Formulation Pharmacokinetics and Imentioning

confidence: 99%

“…15,16 The difluprednate emulsion formulation began by suspending DFBA in a variety of oils (castor, cottonseed, medium-chain fatty acid triglyceride, oleic, olive, peanut, and soybean). 7 As castor oil showed the highest solubility, it was selected as the lipid phase. Next, various concentrations of polysorbate 80, a nonionic emulsifying surfactant with a good safety profile for ophthalmic use, were added to determine the optimal proportion of drug, oil, and surfactant to avoid blurred vision and ocular surface toxicity.…”

Section: Review Of Pharmacology Formulation Pharmacokinetics and Imentioning

confidence: 99%

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The role of difluprednate ophthalmic emulsion in clinical practice

Jamal¹,

Callanan²

2009

OPTH

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Abstract:The mainstay in the treatment of ocular inflammation, either post-surgical or endogenous, is the use of steroids. While these agents effectively address inflammation, they are not without their risks, including ocular hypertension and acceleration of cataract formation. The most notorious culprits are the strong steroids, such as prednisolone acetate and betamethasone. This review aims to cover the biochemistry and drug development of difluprednate, a novel synthetic strong steroid emulsion. In vivo pharmacokinetics as well as ocular distribution and metabolism are discussed, followed by a comprehensive summary of phase I, II, and III clinical trials evaluating safety and efficacy in patients suffering from postoperative inflammation or anterior uveitis. The objective is to provide an increased familiarity with this newly approved medication as a welcome addition to the ophthalmologist's armamentarium.

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Selective permeation of cross‐linked polyelectrolyte and polyelectrolyte‐filled nonwoven membranes

Jung

Pourdeyhimi

Zhang

2011

J of Applied Polymer Sci

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Selective permeation, driven by ionic attraction, is one of the most important properties of polyelectrolyte membranes. In this study, selective permeation behaviors of different polyelectrolytes, poly(2-acrylamido-2-methyl-1-propanesulfonic acid) (PAMPS), poly(styrene sulfonic acid) (PSS), and poly(methacrylic acid) (PMA), were studied via solution-diffusion mechanism. Among these three polyelectrolytes, PSS membranes showed the highest permeabilities for both water and dimethyl methylphophonate vapors due to their high diffusion coefficients caused by the high flexibility of PSS chains. It was also found that the cross-linking of polymer chains increased membrane permeabilities by weakening the physical network formed by ionic attraction. However, the type and cross-linking of polyelectrolytes did not have significant effect on the membrane selectivities. Nonwoven fabric was employed to control the selective permeation of polyelectrolyte membranes. It was found that filling the nonwoven fabric with polyelectrolytes led to composite membranes with reduced permeabilities and increased selectivities.

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Formulation of an ophthalmic lipid emulsion containing an anti-inflammatory steroidal drug, difluprednate

Cited by 87 publications

References 16 publications

Recent Advances in Ocular Drug Delivery Systems

Recent Advances in Ocular Drug Delivery Systems

The role of difluprednate ophthalmic emulsion in clinical practice

Selective permeation of cross‐linked polyelectrolyte and polyelectrolyte‐filled nonwoven membranes

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