Puglia Carmelo, Blasi Paolo, Ostacolo Carmine, Sommella Eduardo, Bucolo Claudio, Platania Chiara B M, Romano Giovanni L, Geraci Federica, Drago Filippo, Santonocito Debora, Albertini Barbara, Campiglia Pietro, Puglisi Giovanni, Pignatello Rosario
Department of Drug Sciences, University of Catania, Catania, Italy.
NANO-i - Research Centre on Ocular Nanotechnology, University of Catania, Catania, Italy.
Front Pharmacol. 2018 Mar 28;9:285. doi: 10.3389/fphar.2018.00285. eCollection 2018.
Nanostructured lipid carriers (NLCs) loaded with palmitoylethanolamide (PEA) were formulated with the aim to enhance ocular bioavailability of PEA, particularly to the back of the eye. Technological characterization (e.g., size, charge) of NLC loaded with PEA formulation (PEA-NLC) was performed, and NLC morphology was characterized by electron microscopy. Ocular pharmacokinetic study, after topical administration of the formulation, was carried out in rabbit eye. Ultra-high performance liquid chromatography tandem mass spectrometry analysis was carried out to detect PEA levels in ocular tissues. Finally, the ocular tolerability of PEA-NLC formulation was assessed in rabbit eye. The novel formulation significantly increased PEA levels in ocular tissues compared to PEA suspension. Vitreous and retinal levels of PEA were significantly higher in the group treated with PEA-NLC formulation versus PEA suspension (PEA-NLC C 5919 ± 541 pmol/g and 315 ± 70 pmol/g in vitreous and retina, respectively). The PEA-NLC formulation was characterized by high stability and robust ocular bioavailability. Therefore, this innovative formulation may be useful in clinical practice to manage retinal diseases.
负载棕榈酰乙醇胺（PEA）的纳米结构脂质载体（NLCs）被制备出来，目的是提高PEA的眼部生物利用度，尤其是提高其在眼后部的生物利用度。对负载PEA的制剂（PEA-NLC）进行了技术表征（如尺寸、电荷），并通过电子显微镜对NLC的形态进行了表征。在兔眼中进行了制剂局部给药后的眼部药代动力学研究。采用超高效液相色谱串联质谱分析法检测眼部组织中的PEA水平。最后，在兔眼中评估了PEA-NLC制剂的眼部耐受性。与PEA混悬液相比，该新型制剂显著提高了眼部组织中的PEA水平。与PEA混悬液相比，用PEA-NLC制剂治疗的组中PEA的玻璃体和视网膜水平显著更高（PEA-NLC组玻璃体和视网膜中的PEA水平分别为5919±541 pmol/g和315±70 pmol/g）。PEA-NLC制剂具有高稳定性和强大的眼部生物利用度。因此，这种创新制剂可能在临床实践中对治疗视网膜疾病有用。
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