Preformulation of cysteamine gels for treatment of the ophthalmic complications in cystinosis.

McKenzie, Barbara; Kay, Graeme; Matthews, Kerr H.; Knott, Rachel; Cairns, Donald

Abstract

Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all organs. It is treated by regular administration of the aminothiol, cysteamine. Corneal crystal deposition is one of the most troublesome complications affecting patients and requires the hourly administration of cysteamine eye drops. In an attempt to reduce this frequency and improve the treatment, the preformulation and evaluation of cysteamine containing gels is reported. Suitability for ophthalmic delivery was determined by analysis of rheology, bioadhesion, dissolution and stability. The results demonstrated that three polymers were suitable for ophthalmic delivery of cysteamine; namely sodium hyaluronate, hydroxyethyl cellulose and carbomer 934. Sodium hyaluronate displayed optimum performance in the preformulation tests, being pseudoplastic (reduction in apparent viscosity under increasing shear rate), bioadhesive, releasing cysteamine over 40 minutes and displaying stability over time. In conclusion these results offer the possibility to formulate cysteamine in an ocular applicable gel formulation.

Citation

MCKENZIE, B., KAY, G., MATTHEWS, K.H., KNOTT, R. and CAIRNS, D. 2016. Preformulation of cysteamine gels for treatment of the ophthalmic complications in cystinosis. International journal of pharmaceutics [online], 515(1-2), pages 575-582. Available from: https://doi.org/10.1016/j.ijpharm.2016.10.044

• Journal Article Type: Article
• Acceptance Date: Oct 19, 2016
• Online Publication Date: Oct 19, 2016
• Publication Date: Dec 30, 2016
• Deposit Date: Oct 31, 2016
• Publicly Available Date: Oct 20, 2017
• Journal: International journal of pharmaceutics
• Print ISSN: 0378-5173
• Electronic ISSN: 1873-3476
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 515
• Issue: 1-2
• Pages: 575-582
• DOI: https://doi.org/10.1016/j.ijpharm.2016.10.044
• Keywords: Cystinosis; Ophthalmic delivery; Gel; Cysteamine; Preformulation
• Public URL: http://hdl.handle.net/10059/1912
• Contract Date: Oct 31, 2016