Drug Delivery to the Posterior Segment of the Eye: Biopharmaceutic and Pharmacokinetic Considerations

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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.

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Ocular drug delivery.

Ripal Gaudana, Hari Krishna Ananthula, Ashwin Parenky … (2010)

Ocular drug delivery has been a major challenge to pharmacologists and drug delivery scientists due to its unique anatomy and physiology. Static barriers (different layers of cornea, sclera, and retina including blood aqueous and blood-retinal barriers), dynamic barriers (choroidal and conjunctival blood flow, lymphatic clearance, and tear dilution), and efflux pumps in conjunction pose a significant challenge for delivery of a drug alone or in a dosage form, especially to the posterior segment. Identification of influx transporters on various ocular tissues and designing a transporter-targeted delivery of a parent drug has gathered momentum in recent years. Parallelly, colloidal dosage forms such as nanoparticles, nanomicelles, liposomes, and microemulsions have been widely explored to overcome various static and dynamic barriers. Novel drug delivery strategies such as bioadhesive gels and fibrin sealant-based approaches were developed to sustain drug levels at the target site. Designing noninvasive sustained drug delivery systems and exploring the feasibility of topical application to deliver drugs to the posterior segment may drastically improve drug delivery in the years to come. Current developments in the field of ophthalmic drug delivery promise a significant improvement in overcoming the challenges posed by various anterior and posterior segment diseases.

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Adverse events and complications associated with intravitreal injection of anti-VEGF agents: a review of literature.

K Ghasemi Falavarjani, Anna Nguyen (2013)

Intravitreal injection of anti-vascular endothelial growth factor (VEGF) agents is increasingly used for the treatment of a wide variety of retinal diseases, including age-related macular degeneration, diabetic retinopathy and retinal vascular occlusions, and retinopathy of prematurity. Despite encouraging results in halting the disease and improving the vision, intravitreal injection of anti-VEGF agents may be associated with systemic adverse events and devastating ocular complications. In this review, we provide an overview of safety data for intravitreal injection of common anti-VEGF agents.

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Challenges and obstacles of ocular pharmacokinetics and drug delivery.

Arto Urtti (2006)

Modern biological research has produced increasing number of promising therapeutic possibilities for medical treatment. These include for example growth factors, monoclonal antibodies, gene knockdown methods, gene therapy, surgical transplantations and tissue engineering. Ocular application of these possibilities involves drug delivery in many forms. Ocular drug delivery is hampered by the barriers protecting the eye. This review presents an overview of the essential factors in ocular pharmacokinetics and selected pharmacological future challenges in ophthalmology.

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Journal

Journal ID (nlm-ta): Pharmaceutics

Journal ID (iso-abbrev): Pharmaceutics

Journal ID (publisher-id): pharmaceutics

Title: Pharmaceutics

Publisher: MDPI

ISSN (Electronic): 1999-4923

Publication date (Electronic): 16 March 2020

Publication date Collection: March 2020

Volume: 12

Issue: 3

Electronic Location Identifier: 269

Affiliations

[1 ]Department of Pharmacology, Pharmacy and Pharmaceutical Technology, University of Santiago de Compostela (USC), Campus vida, 15782 Santiago de Compostela, Spain; rubenvf1@ 123456gmail.com (R.V.-F.); victoriadiaztome@ 123456gmail.com (V.D.-T.); andrealuaces21@ 123456gmail.com (A.L.-R.); andrea.conde.penedo@ 123456rai.usc.es (A.C.-P.); xurxo.garcia.otero@ 123456gmail.com (X.G.-O.); asteriam.luzardo@ 123456usc.es (A.L.-Á.)

[2 ]Clinical Neurosciences Group, University Clinical Hospital, Health Research Institute of Santiago de Compostela (IDIS), Travesía da Choupana s/n, 15706 Santiago de Compostela, Spain

[3 ]Clinical Pharmacology Group, University Clinical Hospital, Health Research Institute of Santiago de Compostela (IDIS), Travesía da Choupana s/n, 15706 Santiago de Compostela, Spain

[4 ]Paraquasil Group, Health Research Institute of Santiago de Compostela (IDIS), Travesía da Choupana s/n, 15706 Santiago de Compostela, Spain

[5 ]Molecular Imaging Group. University Clinical Hospital, Health Research Institute of Santiago de Compostela (IDIS), Travesía da Choupana s/n, 15706 Santiago de Compostela, Spain

Author notes

[* ]Correspondence: anxordes@ 123456gmail.com (A.F.-F.); francisco.otero@ 123456usc.es (F.J.O.-E.)

[†]

These authors contributed equally to this work.

Author information

Xurxo García-Otero https://orcid.org/0000-0002-8351-3180

Asteria Luzardo-Álvarez https://orcid.org/0000-0002-8842-0960

Anxo Fernández-Ferreiro https://orcid.org/0000-0002-7348-7337

Francisco J. Otero-Espinar https://orcid.org/0000-0001-9030-2253

Article

Publisher ID: pharmaceutics-12-00269

DOI: 10.3390/pharmaceutics12030269

PMC ID: 7151081

PubMed ID: 32188045

SO-VID: 2f963ce6-9cb9-464c-a8d1-d2efc525bae7

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Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

Drug Delivery to the Posterior Segment of the Eye: Biopharmaceutic and Pharmacokinetic Considerations

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Abstract

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RNA drug delivery

Most cited references 211

Ocular drug delivery.

Adverse events and complications associated with intravitreal injection of anti-VEGF agents: a review of literature.

Challenges and obstacles of ocular pharmacokinetics and drug delivery.

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