Faculty of Pharmacy, Federal University of Minas Gerais, Belo Horizonte, 31270-901, Minas Gerais, Brazil.
Pharmaceutical Research and Development, Ezequiel Dias Foundation, Belo Horizonte, 30510-010, Minas Gerais, Brazil.
AAPS PharmSciTech. 2021 Jan 6;22(1):35. doi: 10.1208/s12249-020-01898-4.
Non-infectious uveitis, an ocular inflammatory condition that affects the iris, ciliary body, choroid, and adjacent tissues (retina, optic nerve, and vitreous), is an important cause of blindness worldwide. Sirolimus (SRL), a potent immunomodulatory drug, has shown promising results in the treatment of inflammatory ocular diseases. Despite this therapeutic potential, its clinical use is a major challenge due to low bioavailability and poor solubility. Poly(lactic-co-glycolic acid) (PLGA) is a biodegradable polymer commonly used for ophthalmic drug delivery due to its suitable characteristics such as biocompatibility, good mechanical properties, and improvement of the pharmacokinetic profile of the drug. In the present study, we investigated the effects of SRL-PLGA implant on experimental autoimmune uveitis in rabbits. Clinical and histopathological examinations were performed, followed by assessment of protein levels and determination of myeloperoxidase (MPO) and N-acetylglucosaminidase (NAG) activity in the aqueous humor/vitreous. As a result, treated eyes had decreased average inflammatory scores, protein significant decreases in treated eyes, assessed after 35 days. Histopathological examination showed less severe intraocular inflammation and decreased tissue damage in treated eyes. According to these results, the SRL-PLGA implant evaluated in this study was apparently safe, reducing inflammation in treated eyes, with an extended effect possibly associated with prolonged release of SRL in the posterior segment of the eye. Therefore, intravitreal SRL-PLGA implant could be a promising alternative for treatment of non-infectious uveitis.
非感染性葡萄膜炎是一种影响虹膜、睫状体、脉络膜和邻近组织(视网膜、视神经和玻璃体)的眼部炎症性疾病,是全球范围内导致失明的重要原因。西罗莫司(SRL)是一种有效的免疫调节剂药物,在治疗炎症性眼病方面显示出良好的疗效。尽管具有这种治疗潜力,但由于其生物利用度低和溶解度差,其临床应用仍然是一个重大挑战。聚(乳酸-共-乙醇酸)(PLGA)是一种可生物降解的聚合物,由于其具有生物相容性、良好的机械性能和改善药物药代动力学特征等特点,常用于眼科药物递送。在本研究中,我们研究了 SRL-PLGA 植入物对兔实验性自身免疫性葡萄膜炎的影响。进行了临床和组织病理学检查,随后评估了房水/玻璃体液中的蛋白水平以及髓过氧化物酶(MPO)和 N-乙酰氨基葡萄糖苷酶(NAG)的活性。结果显示,治疗组的平均炎症评分降低,治疗组的蛋白水平显著降低,在 35 天后评估。组织病理学检查显示治疗组眼内炎症程度较轻,组织损伤程度降低。根据这些结果,本研究中评估的 SRL-PLGA 植入物显然是安全的,可减轻治疗组眼内炎症,其延长的作用可能与 SRL 在眼后段的延长释放有关。因此,玻璃体内注射 SRL-PLGA 植入物可能是治疗非感染性葡萄膜炎的一种有前途的选择。