1. OCTN2- and ATB 0,+ -targeted nanoemulsions for improving ocular drug delivery.
- Author
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Tang B, Wang Q, Zhang G, Zhang A, Zhu L, Zhao R, Gu H, Meng J, Zhang J, and Fang G
- Subjects
- Animals, Humans, Rabbits, Solute Carrier Family 22 Member 5 metabolism, Biological Transport, Carnitine metabolism, Carnitine pharmacology, Drug Delivery Systems, Epithelial Cells metabolism
- Abstract
Traditional eye drops are administered via topical instillation. However, frequent dosing is needed due to their relatively rapid precorneal removal and low ocular bioavailability. To address these issues, stearoyl L-carnitine-modified nanoemulsions (SC-NEs) were fabricated. The physicochemical properties of SC-NEs in terms of size, morphology, zeta potential, encapsulation efficiency, and in vitro drug release behavior were characterized. The cellular uptake and mechanisms of SC-NEs were comprehensively studied in human corneal epithelial cells and the stearoyl L-carnitine ratio in SC-NEs was optimized. The optimized SC-NEs could target the novel organic cation/carnitine transporter 2 (OCTN2) and amino acid transporter B (0 +) (ATB
0,+ ) on the corneal epithelium, which led to superior corneal permeation, ocular surface retention ability, ocular bioavailability. Furthermore, SC-NEs showed excellent in vivo anti-inflammatory efficacy in a rabbit model of endotoxin-induced uveitis. The ocular safety test indicated that the SC-NEs were biocompatible. In general, the current study demonstrated that OCTN2 and ATB0,+ -targeted nanoemulsions were promising ophthalmologic drug delivery systems that can improve ocular drug bioavailability and boost the therapeutic effects of drugs for eye diseases., (© 2024. The Author(s).)- Published
- 2024
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