IOVS Proceedings of the National Academy of Sciences
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Investigative Ophthalmology & Visual Science, Vol 23, 530-533, Copyright © 1982 by Association for Research in Vision and Ophthalmology

ARTICLES AND REPORTS

Lectin-mediated attachment of liposomes to cornea: influence on transcorneal drug flux

HE Schaeffer, JM Breitfeller and DL Krohn

A method to enhance retention of drug-bearing liposomes at the corneal surface under conditions of tear flow was investigated. Mixed brain gangliosides were incorporated into the membranes of phosphatidyl choline liposomes to provide receptor sites for wheat germ agglutinin, a plant lectin that binds strongly to both human and rabbit corneal epithelium. Ganglioside-containing liposomes showed a 2.5-fold increase in their binding to rabbit cornea in vitro when corneas were pretreated with wheat germ agglutinin (500 micrograms/ml), suggesting that the lectin mediates specific binding of these liposomes to the corneal surface. In addition, under conditions of continuous tear flow (1 ml/hr), ganglioside-containing liposomes with entrapped carbachol significantly enhanced carbachol flux across isolated rabbit corneas pretreated with wheat germ agglutinin 90 min after drug delivery. The data support the potential use of liposomes as a vehicle for topical drug flux enhancement.




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Copyright © 1982 by the Association for Research in Vision and Ophthalmology