title: A potential carrier based on liquid crystal nanoparticles for ophthalmic delivery of pilocarpine nitrate.
abstract: Poor corneal penetration and short preocular retention of a clinical hydrophilic drug, pilocarpine nitrate (PN), for the treatment of open-angle glaucoma and acute angle-closure glaucoma, limit its ocular application. The purpose of this study was to investigate the potential of liquid crystal nanoparticles (LCNPs) for ocular delivery of PN. LCNPs were developed by a top-down method using glyceryl monoolein (GMO) and water in the presence of stabilizer Poloxamer 407. They were characterized by transmission electron microscopy (TEM) and small angle X-ray diffraction (SAXS). The size of LCNP is 202.28±19.32 nm and the encapsulation efficiency reached 61.03%. The in vitro release profiles indicated that PN could keep sustained release from PN-loaded LCNPs for 8h. An ex vivo corneal permeation study revealed that the apparent permeability coefficient of PN-loaded LCNPs was 2.05-fold higher than that of commercial eye drops. In addition, the topical administration test showed that PN-loaded LCNPs had a prolonged effect on decreasing intraocular pressure (IOP) of rabbits compared with commercial drug and physiological saline. In conclusion, LCNPs had been demonstrated to be potential for controlled-release ocular drug delivery.
authors.affiliation: School of Pharmacy, Nanjing Medical University, Lane 818, East Tianyuan Road, Nanjing, Jiangsu 211166, PR China.
authors.forename: Jing
authors.initials: J
authors.lastname: Li
authors.forename: Lin
authors.initials: L
authors.lastname: Wu
authors.forename: Weijun
authors.initials: W
authors.lastname: Wu
authors.forename: Baoyan
authors.initials: B
authors.lastname: Wang
authors.forename: Zhongyuan
authors.initials: Z
authors.lastname: Wang
authors.forename: Hongliang
authors.initials: H
authors.lastname: Xin
authors.forename: Qunwei
authors.initials: Q
authors.lastname: Xu
mesh_terms: D060433:Administration, Ophthalmic; D000818:Animals; D003315:Cornea / Q000033:anatomy & histology / Q000187:drug effects / Q000378:metabolism; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D005989:Glycerides / Q000737:chemistry; D066298:In Vitro Techniques; D007429:Intraocular Pressure / Q000187:drug effects; D050866:Liquid Crystals / Q000737:chemistry*; D008916:Miotics / Q000008:administration & dosage / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D009883:Ophthalmic Solutions; D010539:Permeability; D010862:Pilocarpine / Q000008:administration & dosage / Q000737:chemistry*; D020442:Poloxamer / Q000737:chemistry; D011817:Rabbits
chemical_list: D004337:Drug Carriers; D005989:Glycerides; D008916:Miotics; D009883:Ophthalmic Solutions; D010862:Pilocarpine; D020442:Poloxamer; C005953:monoolein
keywords: Corneal permeability; Glycerol monooleate; Liquid crystal nanoparticle; Pilocarpine nitrate; Reverse hexagonal phase