Pharmacokinetic Simulations of Intravitreal Biologicals: Aspects of Drug Delivery to the Posterior and Anterior Segments
Biologicals are important ocular drugs that are be delivered using monthly and bimonthly intravitreal injections to treat retinal diseases, such as age-related macular degeneration. Long acting delivery systems are needed for prolongation of their dosing interval. Intravitreal biologicals are elimin...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2018-12-01
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| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1999-4923/11/1/9 |
| _version_ | 1811262790557499392 |
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| author | Anna-Kaisa Rimpelä Iiro Kiiski Feng Deng Heidi Kidron Arto Urtti |
| author_facet | Anna-Kaisa Rimpelä Iiro Kiiski Feng Deng Heidi Kidron Arto Urtti |
| author_sort | Anna-Kaisa Rimpelä |
| collection | DOAJ |
| description | Biologicals are important ocular drugs that are be delivered using monthly and bimonthly intravitreal injections to treat retinal diseases, such as age-related macular degeneration. Long acting delivery systems are needed for prolongation of their dosing interval. Intravitreal biologicals are eliminated from the eye via the aqueous humor outflow. Thus, the anterior and posterior segments are exposed to the drug. We utilized a kinetic simulation model to estimate protein drug concentrations in the vitreous and aqueous humor after bolus injection and controlled release administration to the vitreous. The simulations predicted accurately the experimental levels of 5 biologicals in the vitreous and aqueous humor. The good match between the simulations and experimental data demonstrated almost complete anterior segment bioavailability, and major dose sparing with ocular controlled release systems. Overall, the model is a useful tool in the design of intraocular delivery of biologicals. |
| first_indexed | 2024-04-12T19:33:00Z |
| format | Article |
| id | doaj.art-4f074820a58f4213bac5319345e7ee7c |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-12T19:33:00Z |
| publishDate | 2018-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-4f074820a58f4213bac5319345e7ee7c2022-12-22T03:19:17ZengMDPI AGPharmaceutics1999-49232018-12-01111910.3390/pharmaceutics11010009pharmaceutics11010009Pharmacokinetic Simulations of Intravitreal Biologicals: Aspects of Drug Delivery to the Posterior and Anterior SegmentsAnna-Kaisa Rimpelä0Iiro Kiiski1Feng Deng2Heidi Kidron3Arto Urtti4Drug Research Program, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, 00790 Helsinki, FinlandDrug Research Program, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, 00790 Helsinki, FinlandDrug Research Program, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, 00790 Helsinki, FinlandDrug Research Program, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, 00790 Helsinki, FinlandDrug Research Program, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, 00790 Helsinki, FinlandBiologicals are important ocular drugs that are be delivered using monthly and bimonthly intravitreal injections to treat retinal diseases, such as age-related macular degeneration. Long acting delivery systems are needed for prolongation of their dosing interval. Intravitreal biologicals are eliminated from the eye via the aqueous humor outflow. Thus, the anterior and posterior segments are exposed to the drug. We utilized a kinetic simulation model to estimate protein drug concentrations in the vitreous and aqueous humor after bolus injection and controlled release administration to the vitreous. The simulations predicted accurately the experimental levels of 5 biologicals in the vitreous and aqueous humor. The good match between the simulations and experimental data demonstrated almost complete anterior segment bioavailability, and major dose sparing with ocular controlled release systems. Overall, the model is a useful tool in the design of intraocular delivery of biologicals.http://www.mdpi.com/1999-4923/11/1/9intravitreal injectionocular drug deliverybevacizumabranibizumabafliberceptcontrolled release |
| spellingShingle | Anna-Kaisa Rimpelä Iiro Kiiski Feng Deng Heidi Kidron Arto Urtti Pharmacokinetic Simulations of Intravitreal Biologicals: Aspects of Drug Delivery to the Posterior and Anterior Segments Pharmaceutics intravitreal injection ocular drug delivery bevacizumab ranibizumab aflibercept controlled release |
| title | Pharmacokinetic Simulations of Intravitreal Biologicals: Aspects of Drug Delivery to the Posterior and Anterior Segments |
| title_full | Pharmacokinetic Simulations of Intravitreal Biologicals: Aspects of Drug Delivery to the Posterior and Anterior Segments |
| title_fullStr | Pharmacokinetic Simulations of Intravitreal Biologicals: Aspects of Drug Delivery to the Posterior and Anterior Segments |
| title_full_unstemmed | Pharmacokinetic Simulations of Intravitreal Biologicals: Aspects of Drug Delivery to the Posterior and Anterior Segments |
| title_short | Pharmacokinetic Simulations of Intravitreal Biologicals: Aspects of Drug Delivery to the Posterior and Anterior Segments |
| title_sort | pharmacokinetic simulations of intravitreal biologicals aspects of drug delivery to the posterior and anterior segments |
| topic | intravitreal injection ocular drug delivery bevacizumab ranibizumab aflibercept controlled release |
| url | http://www.mdpi.com/1999-4923/11/1/9 |
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