Ocular Drug Distribution After Topical Administration: Population Pharmacokinetic Model in Rabbits

Djebli, Nassim; Khier, Sonia; Griguer, Florence; Coutant, Anne-Laure; Tavernier, Alexandra; Fabre, Gérard; Leriche, Caroline; Fabre, David

doi:10.1007/s13318-016-0319-4

Cited by 37 publications

(26 citation statements)

References 16 publications

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“…Due to this fact, first-pass metabolism is minimized compared to peroral administration. This depends, of course, on the drugs used but becomes especially relevant when using drugs with low absorption rates as it can then result in systemic adverse effects 15,16. In addition, the volume of commercial drop dispensers often exceeds the capacity of drug absorption of the conjunctival sac, so that some of the liquid can drain out of the eye and onto the eyelids and cheeks 17.…”

Section: Introductionmentioning

confidence: 99%

Systemic side effects of eye drops: a pharmacokinetic perspective

Farkouh¹,

Frigo²,

Czejka

2016

OPTH

184

131

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When administering eye drops, even when completely correctly applied, several routes of absorption are possible and excess amounts can sometimes cause an unwanted systemic bioavailability of the drops when not completely absorbed into the eye. Furthermore, the concentration of active ingredients in such medicinal preparations is usually very high, so that despite the correct application of the recommended dose, considerable amounts may be absorbed in an unwanted manner through various routes. Children are subject to a much higher risk of systemic side effects because ocular dosing is not weight adjusted and physiological development (eg, liver status) differs from that of adults. There is a lack of information about pediatric dosing in the current literature. This review summarizes the most important clinically relevant systemic side effects that may occur during ophthalmic eye treatments. In this review, we discuss general pharmacokinetic considerations as well as the advantages, disadvantages, and consequences of administering drugs from some important drug groups to the eye.

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Section: Introductionmentioning

confidence: 99%

Systemic side effects of eye drops: a pharmacokinetic perspective

Farkouh¹,

Frigo²,

Czejka

2016

OPTH

184

131

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“…80 to 90%) is drained into the naso-lacrimal duct. Naso-lacrimal drainage helps maintaining the volume of pre-corneal fluid about 7 to 10 μl at any time (19). A natural protective physiological mechanism causes loss of any excess fluid present; it's drained out through the naso-lacrimal duct.…”

Section: Barriers Of Ocular Drug Deliverymentioning

confidence: 99%

“…However, for drugs administered through ocular route with a local therapeutic effect, cannot be sampled. A very few exceptions are made such as monitoring of drug levels in biopsies or aqueous humor collected from patients subjected to ophthalmic surgical procedures (19). Therefore, animal models are used to study the drugs distribution in ocular tissues.…”

Section: Ocular Pharmacokineticsmentioning

confidence: 99%

A comprehensive insight on ocular pharmacokinetics

Agrahari

Mandal

Agrahari

et al. 2016

Drug Deliv. and Transl. Res.

339

249

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Eye is a distinctive organ with protective anatomy and physiology. Several pharmacokinetics compartment model of ocular drug delivery has been developed for describing the absorption, distribution and elimination of ocular drugs in the eye. Determining pharmacokinetics parameters in ocular tissues is a major challenge because of the complex anatomy and dynamic physiological barrier of the eye. In this review, pharmacokinetics of these compartments exploring different drugs, delivery systems and routes of administration are discussed including factors affecting intraocular bioavailability. Factors such as pre-corneal fluid drainage, drug binding to tear proteins, systemic drug absorption, corneal factors, melanin binding, drug metabolism renders ocular delivery challenging and elaborated in this manuscript. Several compartment models are discussed those are developed in ocular drug delivery to study the pharmacokinetics parameters. There are several transporters present in both anterior and posterior segments of the eye which play a significant role in ocular pharmacokinetics and summarized briefly. Moreover, several ocular pharmacokinetics animal models and relevant studies are reviewed and discussed in addition to the pharmacokinetics of various ocular formulations.

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“…After instillation, a big portion of an instilled volume (approximately from 80 to 90%) is drained into the nasolacrimal duct. Nasolacrimal drainage helps maintain the volume of precorneal fluid at about 7-10 μl at all times [46]. A natural protective physiological mechanism causes the loss of any excess fluid present: it is drained out through the nasolacrimal duct.…”

Section: Dynamic Barriersmentioning

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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Ocular Drug Distribution After Topical Administration: Population Pharmacokinetic Model in Rabbits

Cited by 37 publications

References 16 publications

Systemic side effects of eye drops: a pharmacokinetic perspective

Systemic side effects of eye drops: a pharmacokinetic perspective

A comprehensive insight on ocular pharmacokinetics

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

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