College of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, People's Republic of China.
J Pharm Sci. 2012 Oct;101(10):3833-44. doi: 10.1002/jps.23251. Epub 2012 Jul 5.
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.
本研究旨在开发一种新型的纳米结构脂质载体（NLC）系统，以提高芒果苷（MGN）的眼部生物利用度，用于白内障的潜在治疗。通过粒径、多分散指数、Zeta 电位、包封效率、载药量、形态特性和晶体状态对载药 NLC（MGN-NLC）制剂的理化性质进行了表征。通过 NLC 系统的药物释放、物理稳定性和通过离体兔角膜的角膜渗透来研究体外特性。此外，通过改良的 Draize 试验和组织学显微镜评估体内眼耐受性。通过裂隙灯观察评估预眼滞留能力。通过微透析技术进行房水药代动力学研究。透射电子显微镜显示出球形和均匀的形态。差示扫描量热法和 X 射线衍射法显示出不完美的晶体晶格。优化的 MGN-NLC 制剂表现出持续的药物释放，具有 3 个月的稳定性和体外角膜渗透增加 4.31 倍。此外，体内研究表明，眼部组织具有高耐受性，并且在角膜表面具有延长的药物滞留能力。最后，药代动力学研究表明，与 MGN 溶液（MGN-SOL）相比，眼部生物利用度提高了 5.69 倍。因此，NLC 系统是一种有前途的 MGN 眼部递药方法。
