Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt.
Departments of Pharmaceutical Sciences, Ophthalmology, and Bioengineering, University of Colorado Anschutz Medical Campus, Aurora, CO, 80045, USA.
Drug Deliv Transl Res. 2021 Jun;11(3):866-893. doi: 10.1007/s13346-020-00843-z.
Corticosteroids remain the mainstay of the treatment for various ocular conditions affecting the ocular surface, anterior and posterior segments of the eye due to their anti-inflammatory, anti-oedematous, and anti-neovascularization properties. Prednisolone, prednisolone acetate, dexamethasone, triamcinolone acetonide, fluocinolone acetonide, and loteprednol etabonate are amongst the most widely used ophthalmic corticosteroids. Corticosteroids differ in their activity and potency in the eye due to their inherent pharmacological and pharmaceutical differences. Different routes and regimens are available for ocular administration of corticosteroids. Conventional topical application to the eye is the route of choice when targeting diseases affecting the ocular surface and anterior segment, while periocular, intravitreal, and suprachoroidal injections can be potentially effective for posterior segment diseases. Corticosteroid-induced intraocular pressure elevation and cataract formation remain the most significant local risks following topical as well as systemic corticosteroid administration. Invasive drug administration via intracameral, subconjunctival, and intravitreal injection can enhance ocular bioavailability and minimize dose and dosing frequency of administration, yet may exacerbate ocular side effects of corticosteroids. This review provides a critical appraisal of the ophthalmic uses of corticosteroid, routes of administration, drug delivery fundamentals and novel ocular implantable steroid delivery systems, factors influencing side effects, and future perspectives for ocular corticosteroid therapy.
皮质类固醇仍然是治疗各种影响眼表、眼前段和眼后段的眼部疾病的主要药物，因为它们具有抗炎、抗水肿和抗新生血管形成的特性。泼尼松龙、醋酸泼尼松龙、地塞米松、曲安奈德、氟轻松醋酸酯和依托泊苷依托泊苷是最广泛使用的眼科皮质类固醇之一。由于其固有的药理学和药物学差异，皮质类固醇在眼部的活性和效力存在差异。皮质类固醇有多种眼部给药途径和方案。当针对影响眼表和前段的疾病时，常规局部应用于眼部是首选途径，而眼周、玻璃体内和脉络膜下注射对于后段疾病可能是有效的。皮质类固醇引起的眼压升高和白内障形成仍然是局部应用以及全身应用皮质类固醇后最显著的局部风险。通过前房内、结膜下和玻璃体内注射等有创药物给药可以提高眼内生物利用度，减少药物剂量和给药频率，但可能会加重皮质类固醇的眼部副作用。本文对皮质类固醇的眼部应用、给药途径、药物输送基础以及新型眼内可植入类固醇输送系统、影响副作用的因素以及眼部皮质类固醇治疗的未来展望进行了批判性评估。
