title: Zn-Al-NO(3)-layered double hydroxides with intercalated diclofenac for ocular delivery.
abstract: This study was aimed to evaluate the potential use of a drug delivery system, drug-layered double hydroxide (LDH) nanocomposites for ocular delivery. Diclofenac was successfully intercalated into Zn-Al-NO(3)-LDH by coprecipitation method. The nanocomposites were characterized by particle size, elemental chemical analysis, thermogravimetric analysis, etc. A tilt bilayer of diclofenac molecules formed in the interlayer with the gallery height of 1.868 nm. In vivo precorneal retention studies were conducted with diclofenac sodium (DS) saline, diclofenac-LDH nanocomposite dispersion, 2% polyvinylpyrrolidone (PVP) K30-diclofenac-LDH nanohybrid dispersion and 10% PVP K30-diclofenac-LDH nanohybrid dispersion, separately. Compared with DS saline, all the dispersions have extended the detectable time of DS from 3h to 6h; C(max) and AUC(0-t) of diclofenac-LDH nanocomposite dispersion showed 3.1-fold and 4.0-fold increase, respectively; C(max) and AUC(0-t) of 2% PVP K30-LDH nanohybrid dispersion were about 5.3-fold and 6.0-fold enhancement, respectively. Results of the Draize test showed that no eye irritation was demonstrated in rabbits after single and repeated administration. These results suggest that this novel ocular drug delivery system appears to offer promise as a means to improving the bioavailability of drugs after ophthalmic applications.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, No 24 Tongjia Xiang, Nanjing 210009, China.
authors.forename: Feng
authors.initials: F
authors.lastname: Cao
authors.forename: Yanjun
authors.initials: Y
authors.lastname: Wang
authors.forename: Qineng
authors.initials: Q
authors.lastname: Ping
authors.forename: Zhenggen
authors.initials: Z
authors.lastname: Liao
mesh_terms: D000287:Administration, Topical; D017607:Aluminum Compounds / Q000737:chemistry* / Q000633:toxicity; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D001682:Biological Availability; D011232:Chemical Precipitation; D002626:Chemistry, Pharmaceutical; D004008:Diclofenac / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000633:toxicity; D004337:Drug Carriers; D004339:Drug Compounding; D005123:Eye / Q000187:drug effects / Q000378:metabolism*; D005260:Female; D006863:Hydrogen-Ion Concentration; D006878:Hydroxides / Q000737:chemistry* / Q000633:toxicity; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D053761:Nanocomposites; D036103:Nanotechnology; D009883:Ophthalmic Solutions; D010316:Particle Size; D011205:Povidone / Q000737:chemistry; D011817:Rabbits; D012997:Solvents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods; D013818:Thermogravimetry; D017967:Zinc Compounds / Q000737:chemistry* / Q000633:toxicity
chemical_list: D017607:Aluminum Compounds; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D006878:Hydroxides; D009883:Ophthalmic Solutions; D012997:Solvents; D017967:Zinc Compounds; D004008:Diclofenac; D011205:Povidone