title: Liposomes as a potential ocular delivery system of distamycin A.
abstract: Liposomes containing Distamycin A (DA) may be clinically useful in the treatment of ocular HSV infections, especially in acyclovir-resistant HSV keratitis. This study evaluated the in vitro and in vivo performance of a topical controlled release liposomal formulation containing DA (DA-Lipo) aimed at reducing the toxicity of the encapsulated active agent and improving drug uptake by ocular tissues. The bioavailability of DA in the tear fluid and the DA uptake into the cornea were increased after instillation of DA-Lipo in rabbits, reaching the DA corneal concentration corresponding to IC50 values against HSV without any sign of transcorneal permeation of drug. DA-Lipo was definitely less cytotoxic then plain DA in rabbit corneal epithelial cells. These results provide new insights into the correlation between the in vitro data and the drug kinetics following ocular applications of liposomal vesicles.
authors.affiliation: Department of Pharmacy, University of Pisa, Pisa, Italy. Electronic address: patrizia.chetoni@farm.unipi.it.
authors.forename: Patrizia
authors.initials: P
authors.lastname: Chetoni
authors.affiliation: Department of Pharmacy, University of Pisa, Pisa, Italy.
authors.forename: Daniela
authors.initials: D
authors.lastname: Monti
authors.affiliation: Department of Pharmacy, University of Pisa, Pisa, Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Tampucci
authors.affiliation: Department of Translational Medicine NTMS, University of Pisa, Pisa, Italy.
authors.forename: Barbara
authors.initials: B
authors.lastname: Matteoli
authors.affiliation: Department of Translational Medicine NTMS, University of Pisa, Pisa, Italy.
authors.forename: Luca
authors.initials: L
authors.lastname: Ceccherini-Nelli
authors.affiliation: Department of Pharmacy, University of Pisa, Pisa, Italy.
authors.forename: Alessando
authors.initials: A
authors.lastname: Subissi
authors.affiliation: Department of Pharmacy, University of Pisa, Pisa, Italy.
authors.forename: Susi
authors.initials: S
authors.lastname: Burgalassi
mesh_terms: D060433:Administration, Ophthalmic; D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001082:Aqueous Humor / Q000378:metabolism; D001682:Biological Availability; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D003315:Cornea / Q000378:metabolism; D004214:Distamycins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D018259:Herpesvirus 1, Human / Q000187:drug effects; D018258:Herpesvirus 2, Human / Q000187:drug effects; D008081:Liposomes; D008297:Male; D011817:Rabbits; D013666:Tears / Q000378:metabolism; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D004214:Distamycins; D008081:Liposomes; C030000:stallimycin
keywords: Antiviral; Cytotoxicity; Distamycin A; Liposome; Pharmacokinetic; Rabbit