Cyclodextrins and topical drug delivery to the anterior and posterior segments of the eye

Loftsson, Þorsteinn; Stefánsson, Einar

doi:10.1016/j.ijpharm.2017.04.010

Cited by 105 publications

(71 citation statements)

References 125 publications

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“…Recently, dexamethasone was formulated in cyclodextrin containing eye drop solutions and compared with dexamethasone suspensions [126]. The hydroxypropyl cyclodextrin formulation showed increased dexamethasone solubility by orders of magnitude and resulted in substantial increases in ocular drug absorption, even in the posterior eye segment.…”

Section: Inclusion Complexes (Clathrates)mentioning

confidence: 99%

Polysaccharides in Ocular Drug Delivery

et al. 2019

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Polysaccharides, such as cellulose, hyaluronic acid, alginic acid, and chitosan, as well as polysaccharide derivatives, have been successfully used to augment drug delivery in the treatment of ocular pathologies. The properties of polysaccharides can be extensively modified to optimize ocular drug formulations and to obtain biocompatible and biodegradable drugs with improved bioavailability and tailored pharmacological effects. This review discusses the available polysaccharide choices for overcoming the difficulties associated with ocular drug delivery, and it explores the reasons for the dependence between the physicochemical properties of polysaccharide-based drug carriers and their efficiency in different formulations and applications. Polysaccharides will continue to be of great interest to researchers endeavoring to develop ophthalmic drugs with improved effectiveness and safety.

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Section: Inclusion Complexes (Clathrates)mentioning

confidence: 99%

Polysaccharides in Ocular Drug Delivery

et al. 2019

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“…Different types of oligomeric CD molecules are currently being used to produce cyclodextrin-based eye drops. These molecules are the β-CD [7], the γ-CD [8], its CD derivatives (hydroxypropyl-beta-cyclodextrin (HP-β-CD)), and the randomly methylated beta-cyclodextrin (RM-β-CD) [118]. Econazole nitrate (EC) and CD/ HP-β-CD were complexed to form different EC-CD inclusion complexes through coprecipitation in order to improve ocular bioavailability [119].…”

Section: Cyclodextrin Nanoparticlesmentioning

confidence: 99%

Breaking down the Barrier: Topical Liposomes as Nanocarriers for Drug Delivery into the Posterior Segment of the Eyeball

Santos¹,

Altamirano-Vallejo²,

Navarro-Partida³

et al. 2020

Role of Novel Drug Delivery Vehicles in Nanobiomedicine

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Topical instillation is the most widely preferred noninvasive route of drug administration to treat diseases affecting the anterior segment of the eye. Nonetheless, the ocular bioavailability for deeper ocular tissues is very low. Different routes of administration, such as intravitreal injections, periocular injections, and systemic administration, have been used to deliver drugs into the posterior segment ocular tissues. However, the presence of blood-retinal barriers (BRBs) makes systemic administration an impractical approach, whereas the drug delivery with the periocular administration route is compromised by ocular static and dynamic barriers. On the other hand, intravitreal injection, the most common and widely recommended route for drug administration to treat posterior ocular diseases, is related to several side effects such as endophthalmitis, hemorrhage, retinal detachment, and poor patient tolerance. Diverse strategies to overcome ocular barriers have been explored for topical drop formulations in order to deliver drugs into the posterior segment ocular tissues. In this chapter, we will review the promising topical nanocarriers for drug delivery into the posterior segment of the eye, emphasizing the use of liposomes for topical ophthalmic formulations targeting the vitreous cavity and the retina.

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“…Additionally, conventional eye drops are not able to maintain therapeutic concentrations in the ocular tissues due to short contact time and fast elimination [31][32][33]. To overcome these problems, cyclodextrin (CD) nanoparticles have been proposed as one of the best options for topical eye drop instillation of both small-molecule drugs and biomolecules to the eye [34]. An aqueous-based eye drop formulation of 0.2% (w/v) cyclosporine A with 12.5% (w/v) alpha-cyclodextrin (α-CD), various amounts of gamma-cyclodextrin (γ-CD), and 1.4% (w/v) hydrolyzed poly(vinyl alcohol) (PVA) was shown to be well tolerated in rabbits [35,36].…”

Section: Introductionmentioning

confidence: 99%

In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation

et al. 2020

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The aim of this study was to design and evaluate novel cyclodextrin (CD)-based aggregate formulations to efficiently deliver nepafenac topically to the eye structure, to treat inflammation and increase nepafenac levels in the posterior segment, thus attenuating the response of inflammatory mediators. The physicochemical properties of nine aggregate formulations containing nepafenac/γ-CD/hydroxypropyl-β (HPβ)-CD complexes as well as their rheological properties, mucoadhesion, ocular irritancy, corneal and scleral permeability, and anti-inflammatory activity were investigated in detail. The results were compared with a commercially available nepafenac suspension, Nevanac® 3 mg/mL. All formulations showed microparticles, neutral pH, and negative zeta potential (–6 to –27 mV). They were non-irritating and nontoxic and showed high permeation through bovine sclera. Formulations containing carboxymethyl cellulose (CMC) showed greater anti-inflammatory activity, even higher than the commercial formulation, Nevanac® 0.3%. The optimized formulations represent an opportunity for topical instillation of drugs to the posterior segment of the eye.

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Cyclodextrins and topical drug delivery to the anterior and posterior segments of the eye

Cited by 105 publications

References 125 publications

Polysaccharides in Ocular Drug Delivery

Polysaccharides in Ocular Drug Delivery

Breaking down the Barrier: Topical Liposomes as Nanocarriers for Drug Delivery into the Posterior Segment of the Eyeball

In Vitro and Ex Vivo Evaluation of Nepafenac-Based Cyclodextrin Microparticles for Treatment of Eye Inflammation

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