Lectin-mediated attachment of liposomes to cornea: influence on transcorneal drug flux.
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.
D000818:Animals; D002217:Carbachol / Q000378:metabolism; D002250:Carbon Radioisotopes; D003315:Cornea / Q000187:drug effects* / Q000378:metabolism; D005732:Gangliosides / Q000494:pharmacology*; D066298:In Vitro Techniques; D037102:Lectins / Q000494:pharmacology*; D008081:Liposomes / Q000008:administration & dosage* / Q000378:metabolism; D037121:Plant Lectins; D011817:Rabbits; D013666:Tears / Q000378:metabolism; D014908:Triticum
D002250:Carbon Radioisotopes; D005732:Gangliosides; D037102:Lectins; D008081:Liposomes; D037121:Plant Lectins; D002217:Carbachol