Abstract

The treatment of the posterior-segment ocular diseases, such as age-related eye diseases (AMD) or diabetic retinopathy (DR), present a challenge for ophthalmologists due to the complex anatomy and physiology of the eye. This specialized organ is composed of various static and dynamic barriers that restrict drug delivery into the target site of action. Despite numerous efforts, effective intraocular drug delivery remains unresolved and, therefore, it is highly desirable to improve the current treatments of diseases affecting the posterior cavity. This review article gives an overview of pharmacokinetic and biopharmaceutics aspects for the most commonly-used ocular administration routes (intravitreal, topical, systemic, and periocular), including information of the absorption, distribution, and elimination, as well as the benefits and limitations of each one. This article also encompasses different conventional and novel drug delivery systems designed and developed to improve drug pharmacokinetics intended for the posterior ocular segment treatment.

Highlights

  • The posterior segment of the eye comprises the back two-thirds of the eye, including the vitreous humor, the retina, the choroid and the optic nerve

  • The aim of this review is to show an overview of the main aspects involved in ocular drug pharmacokinetics intended to treat Posterior Segment Eye Diseases (PSEDs)

  • In terms of drug delivery, it must be taken into consideration that choroid shows two different behaviors: (1) It acts as a static barrier due to suprachoroid structure and (2) it provides a dynamic barrier as a consequence of a high choriocapillaris-layer blood flow

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Summary

Introduction

The posterior segment of the eye comprises the back two-thirds of the eye, including the vitreous humor, the retina, the choroid and the optic nerve. Physiological barriers and drug transport pathways are described and because of the low effectiveness and bioavailability of the administered drug It should the be advantages and drawbacks different administration routes are to the eye invasive, are discussed. Intravitreal injection istheir the mainstream route administration to treat diseases acceptability by increasing quality of life, butofalso, a notable reduction in the affecting economicthe costs posterior segment of the eye. The aim of this review is to show an overview of the main aspects involved in ocular drug pharmacokinetics intended to treat PSEDs. A discussion of the different factors that are involved in the ocular drug delivery is first made, encompassing the different routes towards the posterior segment of the eye. Physiological barriers and drug transport pathways are described and the advantages and drawbacks of different administration routes to the eye are discussed

Intravitreal Administration
Sclera
Advantages and Limitations
Pharmacokinetics
Anterior Route
Drug Delivery Systems
Topical Administration
Ocular Barriers for the Entry of Drugs
Corneal and Anterior Compartment Barriers
Conjunctiva
Blood–Aqueous
Systemic Administration
Systemic Drugs for Posterior Segment Eye Diseases
Periocular Administration
Subconjunctival Route
SubTenon’s Route
Retrobulbar Route
Peribulbar Route
Posterior Juxtascleral Route
Suprachoroidal Route
Subretinal Route
Conclusions
Findings
81. Genentech
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