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

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

doi:10.1016/j.ijpharm.2016.10.044

Authors

Barbara McKenzie

Dr Graeme Kay g.kay@rgu.ac.uk
Academic Strategic Lead

Dr Kerr Matthews k.h.matthews@rgu.ac.uk
Lecturer

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.

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