Nanostructured lipid carriers as novel ophthalmic delivery system for mangiferin: Improving in vivo ocular bioavailability

The aim of this study was to develop a novel nanostructured lipid carriers (NLCs) system to improve ocular bioavailability of mangiferin (MGN) for the potential treatment of cataract. The physicochemical properties of MGN‐loaded NLC (MGN‐NLC) formulation were characterized by particle size, polydispersity index, zeta potential, entrapment efficiency, drug loading, morphological property, and crystalline state. in vitro characteristics were investigated by drug release from NLC system, physical stability, and corneal permeation through excised rabbit cornea. Moreover, in vivo ocular tolerability was assessed by a modified Draize test and histological microscopy. Preocular retention capability was evaluated by slit‐lamp observation. Pharmacokinetic study in the aqueous humor was performed by microdialysis technique. Transmission electron microscopy depicted spherical and uniform morphology. Differential scanning calorimetry and X‐ray diffractometry displayed imperfect crystalline lattice. The optimized MGN‐NLC formulation exhibited a sustained drug release with 3 months stability and 4.31‐fold increase of in vitro corneal permeation. Furthermore, in vivo studies exhibited a high tolerance in the ocular tissues and prolonged drug retention capacity on the corneal surface. Finally, pharmacokinetic study suggested a 5.69‐fold increase of ocular bioavailability compared with MGN solution (MGN‐SOL). Therefore, NLC system is a promising approach for ocular delivery of MGN. © 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:3833-3844, 2012