Multifunctional Nanocomposites Based on Liposomes and Layered Double Hydroxides Conjugated with Glycylsarcosine for Efficient Topical Drug Delivery to the Posterior Segment of the Eye

• DOI: 10.1021/acs.molpharmaceut.8b01136
• Publication Date: 2019-06-03T20:30:33Z
• Authors: Yan Gu; Chen Xu; Yanyan Wang; Xiangying Zhou; Lei Fang; Feng Cao
• Keywords: Nanocarriers

To achieve efficient drug delivery to the posterior segment of eye via topical instillation, novel multifunctional nanocomposites were prepared by hybridizing dexamethasone disodium phosphate (DEXP)-loaded liposome (LP) glycylsarcosine (GS)-anchored layered double hydroxides (named DEXP-HSPC@LDH-GS) and then fully characterized. The exhibited sustained-release performance as well prolonged precorneal retention ability. MTT assays showed that not cytotoxic both human corneal epithelial cells (HCEpiC) conjunctival (HConEpiC) at an LDH concentration 100 μg/mL. DEXP-HSPC@LDH-GS superior in vitro permeability on HConEpiC-cell-based model. In case HConEpiC cells, clathrin-mediated endocytosis active transport peptide transporter-1 (PepT-1) involved internalization nanocomposites. Fluorescent images frozen sections ocular tissues suggested possible route for doxorubicin hydrochloride (DOX)-labeled from surface back was a non-corneal pathway. Furthermore, rabbit eyes, hybrid displayed markedly higher choroid-retina tissue than other single nanocarriers, such LPs LDH. Besides, results irritancy test nanocomposite drops can be classified nonirritant, which are suitable used drops. word, based could promising vehicles noninvasive eye.