title: Inclusion of water insoluble drugs in amorphous silica nanoparticles.
abstract: Amorphous silica nanoparticles (a-SiNPs) with high surface area and small pore size have been synthesized using a zwitterionic surfactant in acid media. The produced nanoparticles displayed large specific surface area (-850 m2/g) with an average particles size of 45 nm. The loading efficiency was assessed by incorporating three model water insoluble active substances Carbamazepine (CBZ), Ibuprofen (IBU) and Cyclosporin (CyA) via passive loading and it was found to varying from 15-40%. The loaded silica nanoparticles were analyzed using X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) to investigate the state of the adsorbed active agents. CyA was found to be in amorphous state, IBU was partially crystalline while CBZ was transformed into form I. The dissolution profiles showed rapid release for CBZ while IBU and CyA demonstrated prolonged release for 24 hr. The viability of Caco-2 cells was not affected in the presence of a-SiNPs showing negligible cytotoxicity (85%) at high concentrations up to 15 mg/ml.
authors.affiliation: Medway School of Science, Department of Pharmaceutical Sciences, University of Greenwich, Chatham Maritime ME4 4TB, Kent, United Kingdom.
authors.forename: A
authors.initials: A
authors.lastname: Patil
authors.forename: A A
authors.initials: AA
authors.lastname: Lafarga
authors.forename: M
authors.initials: M
authors.lastname: Chebrot
authors.forename: D A
authors.initials: DA
authors.lastname: Lamprou
authors.forename: A
authors.initials: A
authors.lastname: Urquhart
authors.forename: D
authors.initials: D
authors.lastname: Douroumis
mesh_terms: D000327:Adsorption; D018938:Caco-2 Cells; D002152:Calorimetry, Differential Scanning; D002220:Carbamazepine / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D016572:Cyclosporine / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D004339:Drug Compounding; D006801:Humans; D007052:Ibuprofen / Q000737:chemistry / Q000494:pharmacology; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry*; D011208:Powders / Q000737:chemistry; D012822:Silicon Dioxide / Q000008:administration & dosage* / Q000737:chemistry*; D012995:Solubility; D013499:Surface Properties; D014867:Water / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D004364:Pharmaceutical Preparations; D011208:Powders; D014867:Water; D002220:Carbamazepine; D012822:Silicon Dioxide; D016572:Cyclosporine; D007052:Ibuprofen