Liposomal amphotericin B eye drops to treat fungal keratitis: Physico-chemical and formulation stability
- 作者：K. Mor ; A.C. Bartoletti ; A. Bochot ; G. Barratt ; M.L. Br ; ely ; F. Chast
- 关键词：Liposomes ; Amphotericin B ; Fungal infections ; Eye drops
- 刊名：International Journal of Pharmaceutics
- 出版年：2007
- 期刊代码：24_03785173
- 类别：pha
- 出版时间：1 November 2007
- 卷：344
- 期：1-2
- 页码：150-153
- 文件大小：186 K
摘要
Local fungal infections with Candida, Fusarium, Curvularia and Aspergillus can lead to serious ulceration of the cornea and must be treated rapidly. The current treatment consists of 0.15%(w/v) amphotericin B eye drops prepared from Fungizone®, containing deoxycholate, irritant for the cornea, which reduces patient compliance. Eye drops based on liposomal amphotericin B (AmBisome®) would be a convenient alternative; however, according to the manufacturer's instructions, AmBisome® can only be kept refrigerated for 1 week after reconstitution. A longer shelf-life at ambient temperature would be preferable for a preparation made in a hospital pharmacy and delivered to patients. Thus, the possibility of storing an ophthalmic preparation of 0.5%(w/v) liposomal amphotericin B after reconstitution was investigated. After 6 months at room temperature or at +2–8 °C, the hydrodynamic diameter measured by quasi-elastic light scattering remained constant at 108 ± 30 nm with a polydispersity index lower than 0.15. Amphotericin B content, checked by a validated HPLC method, was maintained between 94 and 107%. Amphotericin B and soy phosphatidylcholine proportions remained constant, indicating that the liposomes remained intact and retained the drug. These results show the feasibility of an ophthalmic preparation based on liposomal amphotericin B developed in hospital pharmacies.