Low molecular weight chitosan-coated liposomes for ocular drug delivery: in vitro and in vivo studies

In this study, low molecular weight chitosan coated liposomes (LCHL) were designed and prepared for ocular drug delivery, the coating mechanism was studied, and in vitro and in vivo characterization was conducted. The effects of molecular weight and concentration of low molecular weight chitosan on the liposomal coating were studied. The numeric relations between coating variables and coating efficiency were established using a mathematical model. Morphology of LCHL was examined by transmission electron microscopy (TEM). Cytotoxicity and cell internalization of FITC-BSA labeled LCHL in a rabbit conjunctival epithelium (RCE) cell line were studied. Cyclosporin A (CsA) was encapsulated as a model drug, and in vitro drug release and in vivo drug absorption were investigated. LCHL demonstrated low toxicity to RCE cells. In vitro drug release measurement showed that LCHL had a delayed release profile compared with non-coated liposomes. In vivo study in rabbits showed that the concentrations of CsA in cornea, conjunctiva, and sclera were remarkably increased by LCHL. In conclusion, LCHL might be a potential ocular drug carrier with characteristics such as prolonged drug retention, enhanced drug permeation, and biocompatibility.