title: Corneal permeation properties of a charged lipid nanoparticle carrier containing dexamethasone.
abstract: Drug delivery carriers can maintain effective therapeutic concentrations in the eye. To this end, we developed lipid nanoparticles (L/NPs) in which the surface was modified with positively charged chitosan, which engaged in hydrogen bonding with the phospholipid membrane. We evaluated in vitro corneal permeability and release characteristics, ocular irritation, and drug dynamics of modified and unmodified L/NPs in aqueous humor. The size of L/NPs was uniform and showed a narrow distribution. Corneal permeation was altered by the presence of chitosan and was dependent on particle size; the apparent permeability coefficient of dexamethasone increased by 2.7 and 1.8 times for chitosan-modified and unmodified L/NPs, respectively. In conclusion, a chitosan-modified system could be a promising method for increasing the ocular bioavailability of unmodified L/NPs by enhancing their retention time and permeation into the cornea. These findings provide a theoretical basis for the development of effective drug delivery systems in the treatment of ocular disease.
authors.affiliation: Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.
authors.forename: Junfeng
authors.initials: J
authors.lastname: Ban
authors.affiliation: Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.
authors.forename: Xin
authors.initials: X
authors.lastname: Huang
authors.affiliation: Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.
authors.forename: Guanghan
authors.initials: G
authors.lastname: Deng
authors.affiliation: Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.
authors.forename: Dongzhi
authors.initials: D
authors.lastname: Hou
authors.affiliation: Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.
authors.forename: Yanzhong
authors.initials: Y
authors.lastname: Chen
authors.affiliation: Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, People's Republic of China.
authors.forename: Zhufen
authors.initials: Z
authors.lastname: Lu
mesh_terms: D000818:Animals; D001082:Aqueous Humor / Q000187:drug effects; D001682:Biological Availability; D048271:Chitosan / Q000494:pharmacology; D003315:Cornea / Q000187:drug effects*; D003907:Dexamethasone / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D065546:Drug Liberation; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D010539:Permeability / Q000187:drug effects; D011817:Rabbits; D055672:Static Electricity
chemical_list: D004337:Drug Carriers; D008055:Lipids; D003907:Dexamethasone; D048271:Chitosan
keywords: dexamethasone; eye drop administration; local bioavailability; ocular drug delivery system