W/O microemulsions for ocular delivery: Evaluation of ocular irritation and precorneal retention

Alany, RG, Rades, T, Nicoll, J, Tucker, IG and Davies, NM (2006) W/O microemulsions for ocular delivery: Evaluation of ocular irritation and precorneal retention. Journal of Controlled Release, 111 1-2: 145-152. doi:10.1016/j.jconrel.2005.11.020

Author Alany, RG
Rades, T
Nicoll, J
Tucker, IG
Davies, NM
Title W/O microemulsions for ocular delivery: Evaluation of ocular irritation and precorneal retention
Journal name Journal of Controlled Release   Check publisher's open access policy
ISSN 0168-3659
Publication date 2006-03-10
Sub-type Article (original research)
DOI 10.1016/j.jconrel.2005.11.020
Volume 111
Issue 1-2
Start page 145
End page 152
Total pages 8
Editor K. Park
Place of publication Dordrecht, The Netherland
Publisher Elsevier BV
Collection year 2006
Language eng
Subject C1
730111 Hearing, vision, speech and their disorders
320500 Pharmacology and Pharmaceutical Sciences
320501 Pharmaceutical Sciences and Pharmacy
250103 Colloid and Surface Chemistry
Abstract Water-in-oil microemulsions (w/o ME) capable of undergoing a phase-transition to lamellar liquid crystals (LC) or bicontinuous ME upon aqueous dilution were formulated using Crodarnol EO, Crill 1 and Crillet 4, an alkanol or alkanediol as cosurfactant and water. The hypothesis that phase-transition of ME to LC may be induced by tears and serve to prolong precomeal retention was tested. The ocular irritation potential of components and formulations was assessed using a modified hen's egg chorioallantoic membrane test (HET-CAM) and the preocular retention of selected formulations was investigated in rabbit eye using gamma scintigraphy. Results showed that Crill 1, Crillet 4 and Crodamol EO were non-irritant. However, all other cosurfactants investigated were irritant and their irritation was dependent on their carbon chain length. A w/o ME formulated without cosurfactant showed a protective effect when a strong irritant (0.1 M NaOH) was used as the aqueous phase. Precorneal clearance studies revealed that the retention of colloidal and coarse dispersed systems was significantly greater than an aqueous solution with no significant difference between ME systems (containing 5% and 10% water) as well as o/w emulsion containing 85% water. Conversely, a LC system formulated without cosurfactant displayed a significantly greater retention compared to other formulations. (c) 2005 Elsevier B.V. All rights reserved.
Keyword Chemistry, Multidisciplinary
Pharmacology & Pharmacy
Ophthalmic Delivery
Phase Transition
Preparing Nontoxic Microemulsions
Egg Chorioallantoic Membrane
Ophthalmic Drug-delivery
Rabbit Eye
Mucoadhesive Polymers
Q-Index Code C1

Document type: Journal Article
Sub-type: Article (original research)
Collections: Excellence in Research Australia (ERA) - Collection
2007 Higher Education Research Data Collection
School of Pharmacy Publications
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 54 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 69 times in Scopus Article | Citations
Google Scholar Search Google Scholar
Created: Wed, 15 Aug 2007, 06:59:03 EST