Ocular delivery systems for poorly soluble drugs: An in-vivo evaluation

Luschmann, Christoph; Herrmann, W. M.; Strauß, Olaf; Luschmann, Karl; Goepferich, Achim

doi:10.1016/j.ijpharm.2013.07.002

Cited by 36 publications

(23 citation statements)

References 18 publications

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“…Unfortunately, these solutions are poorly tolerated and have a low bioavailability because CsA is nonpolar and has a greater attraction to the lipophilic vehicle rather than to the tissue [72]. Development of different delivery mechanisms, such as aqueous preparations, have been explored to provide an increase in corneal drug tissue levels, bioavailability and tolerability.…”

Section: Translational Prospectsmentioning

confidence: 99%

“…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%

“…In a study measuring both tolerability and tissue uptake in rabbit corneas, Luschmann et al evaluated an in situ nanosuspension [0.4% CsA] and a micellar solution [0.05% CsA] as delivery systems for CsA [72]. Both solutions were tolerated well, evoking minimal to no irritation.…”

Section: Translational Prospectsmentioning

confidence: 99%

“…Both solutions were tolerated well, evoking minimal to no irritation. The nano-suspension and micellar solution also delivered high levels of CsA, exceeding drug tissue levels reported for Restasis as well as cationic emulsions [72]. In another study therapeutically active CsA levels were achieved in tissues of both the anterior and posterior segments using a water-soluble CsA prodrug formulated within an aqueous solution.…”

Section: Translational Prospectsmentioning

confidence: 99%

See 3 more Smart Citations

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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Section: Translational Prospectsmentioning

confidence: 99%

Section: Translational Prospectsmentioning

confidence: 99%

Section: Translational Prospectsmentioning

confidence: 99%

Section: Translational Prospectsmentioning

confidence: 99%

See 2 more Smart Citations

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

Ames

2015

Clinical Investigation

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“…The first and only US FDA approved and commercially available formulation Restasis ® is a 0.05% CsA oil-in-water emulsion that does not deliver CsA to the corneal tissue [126]. Alternative formulations are the polymeric MPEG-hexPLA/CsA micelles [118,119,122], the cationic oil-in-water nanoemulsions leading to approximately 350 ng CsA /g cornea, 3 h after a single instillation [127,128,129] and the nonionic micelles of Solutol HS15 (poly oxyethylene esters of 12-hydroxystearic acid) with low toxicity in vivo [130]. Polymeric micelles [106,122] and cationic emulsions significantly increase CsA tissue levels after single and multiple dosing in vivo [127,128,129].…”

Section: Novel Formulations For Peptides and The Cyclosporin Casementioning

confidence: 99%

Novel Formulations for Antimicrobial Peptides

Carmona-Ribeiro

Carrasco

2014

IJMS

119

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Peptides in general hold much promise as a major ingredient in novel supramolecular assemblies. They may become essential in vaccine design, antimicrobial chemotherapy, cancer immunotherapy, food preservation, organs transplants, design of novel materials for dentistry, formulations against diabetes and other important strategical applications. This review discusses how novel formulations may improve the therapeutic index of antimicrobial peptides by protecting their activity and improving their bioavailability. The diversity of novel formulations using lipids, liposomes, nanoparticles, polymers, micelles, etc., within the limits of nanotechnology may also provide novel applications going beyond antimicrobial chemotherapy.

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Nanomicelle‐Assisted Targeted Ocular Delivery with Enhanced Antiinflammatory Efficacy In Vivo

Weng

Che

et al. 2017

Advanced Science

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Ocular inflammations are common diseases that may lead to serious vision‐threatening obstacles. Eye drops for antiinflammation therapy need to be administered multiple times daily at a high dosage due to the rapid precorneal removal and low bioavailability of drugs. To overcome these problems, a cRGD‐functionalized DSPE‐PEG2000 nanomicelle (DSPE‐PEG2000‐cRGD) encapsulated with flurbiprofen is proposed. The tailored nanomicelles trigger specific binding to integrin receptors on the ocular surface, which leads to rapid and robust mucoadhesion, superior ocular surface retention, and transcorneal penetration behaviors of nanomicelles. Due to the enhanced drug delivery on ocular surface and in aqueous humor, the functionalized nanoformulation significantly improves ocular antiinflammation efficacy at a low dosage by blocking the synthesis of inflammatory mediators and cytokines. The present study demonstrates a promising strategy that uses a functional peptide combined with nanomicelles for targeted delivery to the eye in ophthalmologic applications.

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Ocular delivery systems for poorly soluble drugs: An in-vivo evaluation

Cited by 36 publications

References 18 publications

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

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

Novel Formulations for Antimicrobial Peptides

Nanomicelle‐Assisted Targeted Ocular Delivery with Enhanced Antiinflammatory Efficacy In Vivo

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