دورية أكاديمية
Corneal and conjunctival drug permeability:Systematic comparison and pharmacokinetic impact in the eye
| العنوان: | Corneal and conjunctival drug permeability:Systematic comparison and pharmacokinetic impact in the eye |
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| المؤلفون: | Ramsay, Eva, Del Amo, Eva M, Toropainen, Elisa, Tengvall-Unadike, Unni, Ranta, Veli-Pekka, Urtti, Arto, Ruponen, Marika |
| المصدر: | Ramsay , E , Del Amo , E M , Toropainen , E , Tengvall-Unadike , U , Ranta , V-P , Urtti , A & Ruponen , M 2018 , ' Corneal and conjunctival drug permeability : Systematic comparison and pharmacokinetic impact in the eye ' , European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences , vol. 119 , pp. 83-89 . https://doi.org/10.1016/j.ejps.2018.03.034Test |
| سنة النشر: | 2018 |
| المجموعة: | The University of Manchester: Research Explorer - Publications |
| مصطلحات موضوعية: | Animals, Aqueous Humor/metabolism, Biological Availability, Conjunctiva/blood supply, Cornea/metabolism, Permeability, Pharmaceutical Preparations/metabolism, Quantitative Structure-Activity Relationship, Regional Blood Flow, Swine |
| الوصف: | On the surface of the eye, both the cornea and conjunctiva are restricting ocular absorption of topically applied drugs, but barrier contributions of these two membranes have not been systemically compared. Herein, we studied permeability of 32 small molecular drug compounds across an isolated porcine cornea and built a quantitative structure-property relationship (QSPR) model for the permeability. Corneal drug permeability (data obtained for 25 drug molecules) showed a 52-fold range in permeability (0.09-4.70 × 10-6 cm/s) and the most important molecular descriptors in predicting the permeability were hydrogen bond donor, polar surface area and halogen ratio. Corneal permeability values were compared to their conjunctival drug permeability values. Ocular drug bioavailability and systemic absorption via conjunctiva were predicted for this drug set with pharmacokinetic calculations. Drug bioavailability in the aqueous humour was simulated to be <5% and trans-conjunctival systemic absorption was 34-79% of the dose. Loss of drug across the conjunctiva to the blood circulation restricts significantly ocular drug bioavailability and, therefore, ocular absorption does not increase proportionally with the increasing corneal drug permeability. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| DOI: | 10.1016/j.ejps.2018.03.034 |
| الإتاحة: | https://doi.org/10.1016/j.ejps.2018.03.034Test https://research.manchester.ac.uk/en/publications/54533db8-0b16-4a92-b6d2-142167291e0cTest |
| حقوق: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.5FE760FA |
| قاعدة البيانات: | BASE |
| DOI: | 10.1016/j.ejps.2018.03.034 |
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