Pharmacokinetic aspects of retinal drug delivery

Eva M. del Amo, Anna Kaisa Rimpelä, Emma Heikkinen, Otto K. Kari, Eva Ramsay, Tatu Lajunen, Mechthild Schmitt, Laura Pelkonen, Madhushree Bhattacharya, Dominique Richardson, Astrid Subrizi, Tiina Turunen, Mika Reinisalo, Jaakko Itkonen, Elisa Toropainen, Marco Casteleijn, Heidi Kidron, Maxim Antopolsky, Kati Sisko Vellonen, Marika RuponenArto Urtti (Corresponding Author)

Research output: Contribution to journalReview Articlepeer-review

441 Citations (Scopus)


Drug delivery to the posterior eye segment is an important challenge in ophthalmology, because many diseases affect the retina and choroid leading to impaired vision or blindness. Currently, intravitreal injections are the method of choice to administer drugs to the retina, but this approach is applicable only in selected cases (e.g. anti-VEGF antibodies and soluble receptors). There are two basic approaches that can be adopted to improve retinal drug delivery: prolonged and/or retina targeted delivery of intravitreal drugs and use of other routes of drug administration, such as periocular, suprachoroidal, sub-retinal, systemic, or topical. Properties of the administration route, drug and delivery system determine the efficacy and safety of these approaches. Pharmacokinetic and pharmacodynamic factors determine the required dosing rates and doses that are needed for drug action. In addition, tolerability factors limit the use of many materials in ocular drug delivery. This review article provides a critical discussion of retinal drug delivery, particularly from the pharmacokinetic point of view. This article does not include an extensive review of drug delivery technologies, because they have already been reviewed several times recently. Instead, we aim to provide a systematic and quantitative view on the pharmacokinetic factors in drug delivery to the posterior eye segment. This review is based on the literature and unpublished data from the authors' laboratory.
Original languageEnglish
Pages (from-to)134-185
Number of pages52
JournalProgress in Retinal and Eye Research
Publication statusPublished - Mar 2017
MoE publication typeA2 Review article in a scientific journal


  • Choroid
  • Clearance
  • Distribution
  • Intravitreal
  • Pharmacokinetic modeling
  • Retina
  • Sub-conjunctival
  • Suprachoroidal
  • Topical
  • Transport
  • Vitreous


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