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

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

Authors

Barbara McKenzie

Graeme Kay

Kerr H. Matthews

Rachel Knott

Donald Cairns

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.

Journal Article Type Article
Publication Date Dec 30, 2016
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
Institution 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
DOI https://doi.org/10.1016/j.ijpharm.2016.10.044
Keywords Cystinosis; Ophthalmic delivery; Gel; Cysteamine; Preformulation

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