Sánchez-López Elena, Esteruelas Gerard, Ortiz Alba, Espina Marta, Prat Josefina, Muñoz Montserrat, Cano Amanda, Calpena Ana Cristina, Ettcheto Miren, Camins Antoni, Alsafi Zaid, Souto Eliana B, García Maria Luisa, Pujol Montserrat
Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, Spain.
Institute of Nanoscience and Nanotechnology (IN2UB), Universitat de Barcelona, 08028 Barcelona, Spain.
Nanomaterials (Basel). 2020 Apr 10;10(4):720. doi: 10.3390/nano10040720.
Ocular inflammation is one of the most prevalent diseases in ophthalmology, which can affect various parts of the eye or the surrounding tissues. Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, are commonly used to treat ocular inflammation in the form of eye-drops. However, their bioavailability in ocular tissues is very low (less than 5%). Therefore, drug delivery systems such as biodegradable polymeric PLGA nanoparticles constitute a suitable alternative to topical eye administration, as they can improve ocular bioavailability and simultaneously reduce drug induced side effects. Moreover, their prolonged drug release can enhance patient treatment adherence as they require fewer administrations. Therefore, several formulations of PLGA based nanoparticles encapsulating dexibuprofen (active enantiomer of Ibuprofen) were prepared using the solvent displacement method employing different surfactants. The formulations have been characterized and their interactions with a customized lipid corneal membrane model were studied. Ex vivo permeation through ocular tissues and in vivo anti-inflammatory efficacy have also been studied.
眼部炎症是眼科最常见的疾病之一，可影响眼睛的各个部位或周围组织。非甾体抗炎药（NSAIDs）如布洛芬，通常以滴眼液的形式用于治疗眼部炎症。然而，它们在眼组织中的生物利用度非常低（低于5%）。因此，诸如可生物降解的聚合物聚乳酸-羟基乙酸共聚物（PLGA）纳米颗粒之类的药物递送系统构成了局部眼部给药的合适替代方案，因为它们可以提高眼部生物利用度并同时减少药物引起的副作用。此外，它们延长的药物释放可以提高患者的治疗依从性，因为给药次数更少。因此，采用溶剂置换法，使用不同的表面活性剂制备了几种包裹右布洛芬（布洛芬的活性对映体）的PLGA基纳米颗粒制剂。对这些制剂进行了表征，并研究了它们与定制的脂质角膜膜模型的相互作用。还研究了通过眼组织的体外渗透和体内抗炎功效。
