Cyclodextrins in eye drop formulations: enhanced topical delivery of corticosteroids to the eye.

T. Loftsson, E. Stefánsson
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引用次数: 153

Abstract

Cyclodextrins are cylindrical oligosaccharides with a lipophilic central cavity and hydrophilic outer surface. They can form water-soluble complexes with lipophilic drugs, which 'hide' in the cavity. Cyclodextrins can be used to form aqueous eye drop solutions with lipophilic drugs, such as steroids and some carbonic anhydrase inhibitors. The cyclodextrins increase the water solubility of the drug, enhance drug absorption into the eye, improve aqueous stability and reduce local irritation. Cyclodextrins are useful excipients in eye drop formulations of various drugs, including steroids of any kind, carbonic anhydrase inhibitors, pilocarpine, cyclosporins, etc. Their use in ophthalmology has already begun and is likely to expand the selection of drugs available as eye drops. In this paper we review the properties of cyclodextrins and their application in eye drop formulations, of which their use in the formulation of dexamethasone eye drops is an example. Cyclodextrins have been used to formulate eye drops containing corticosteroids, such as dexamethasone, with levels of concentration and ocular absorption which, according to human and animal studies, are many times those seen with presently available formulations. Cyclodextrin-based dexamethasone eye drops are well tolerated in the eye and seem to provide a higher degree of bioavailability and clinical efficiency than the steroid eye drop formulations presently available. Such formulations offer the possibility of once per day application of corticosteroid eye drops after eye surgery, and more intensive topical steroid treatment in severe inflammation. While cyclodextrins have been known for more than a century, their use in ophthalmology is just starting. Cyclodextrins are useful excipients in eye drop formulations for a variety of lipophilic drugs. They will facilitate eye drop formulations for drugs that otherwise might not be available for topical use, while improving absorption and stability and decreasing local irritation.
滴眼液配方中的环糊精:增强皮质类固醇对眼睛的局部递送。
环糊精是一种圆柱形低聚糖,具有亲脂的中心腔和亲水的外表面。它们可以与亲脂性药物形成水溶性复合物,“隐藏”在腔内。环糊精可与亲脂性药物(如类固醇和一些碳酸酐酶抑制剂)形成滴眼液水溶液。环糊精增加药物的水溶性,促进药物进入眼睛的吸收,提高水稳定性,减少局部刺激。环糊精是各种药物滴眼液配方中有用的辅料,包括任何种类的类固醇、碳酸酐酶抑制剂、匹罗卡品、环孢素等。它们在眼科中的应用已经开始,并可能扩大眼药水的选择范围。本文综述了环糊精的性质及其在滴眼液中的应用,并以环糊精在地塞米松滴眼液中的应用为例。环糊精已被用于配制含有皮质类固醇(如地塞米松)的滴眼液,根据人类和动物研究,其浓度和眼吸收水平是目前可用配方的许多倍。基于环糊精的地塞米松滴眼液在眼内耐受性良好,似乎比目前可用的类固醇滴眼液提供更高程度的生物利用度和临床效率。这种配方提供了在眼部手术后每天一次使用皮质类固醇滴眼液的可能性,以及在严重炎症时更密集的局部类固醇治疗。虽然环糊精已经被发现了一个多世纪,但它们在眼科中的应用才刚刚开始。环糊精是各种亲脂药物滴眼液配方中有用的赋形剂。它们将促进药物的滴眼液配方,否则这些药物可能无法用于局部使用,同时改善吸收和稳定性,减少局部刺激。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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