TAT-surface modified acyclovir-loaded albumin nanoparticles as a novel ocular drug delivery system

Abstract

The aim of this study was to develop acyclovir (ACV)-loaded bovine serum albumin (BSA) nanoparticles (NPs) which were surface modified with transactivating transduction (TAT) peptide to improve the transcorneal drug delivery in treating viral related keratitis. The TAT-surface modifications were carried out by both conjugation (TAT-con) and coating (TAT-coat) techniques. Characterization of physicochemical properties and assessment of in vitro transcorneal permeation across human corneal epithelial (HCE-T) cell multilayers of prepared TAT-surface modified ACV-BSA NPs were subsequently investigated. The prepared TAT-surface modified ACV-BSA NPs appeared to be spherical in shape and uniform in size of about 200 nm with surface charges ranging between −20 and −30 mV. Increasing TAT amount in TAT-coat ACV-BSA NPs resulted in an increased size of NPs as expected, but it was not the case for TAT-con ACV-BSA NPs. The prepared TAT-coat ACV-BSA NPs were shown to have less cytotoxic effects on HCE-T cells used in permeation studies than those of TAT-con ACV-BSA NPs and ACV solution. The in vitro transcorneal permeation results indicated that TAT-coat ACV-BSA NPs could bring about the highest ACV permeability as compared to ACV-BSA NPs and ACV solution. Such TAT-surface modified ACV-BSA NPs could be developed as novel ocular drug delivery systems.