title: Preparation and in vitro/pharmacokinetic/pharmacodynamic evaluation of a slow-release nano-liposomal form of prednisolone.
abstract: A nano-liposomal carrier was prepared for the anti-inflammatory drug prednisolone acetate (PA). The drug showed remarkable loading in the nano-carriers. The drug-loaded nano-liposmes with average sizes of about 186 nm and zeta potentials of -20 mV were obtained. Our drug release studies showed an apparently zero-order trend with only 18% of the drug released in the first 120 h. Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) analyses showed no chemical interaction between the drug and carrier. Transmission electron microscopy (TEM) imaging showed near-spherical drug-containing nano-carriers. The intramuscular (IM) trial of the nanoformulation compared with the free drug showed both pharmacokinetic (lower Cmax, higher area under the curve (AUC)) and pharmacodynamic (higher and longer lasting anti-inflammatory effect, both macroscopically and biochemically) superiority for the nano-liposomal drug above the free prednisolone in rats.
authors.affiliation: a Department of Veterinary Basic Science , Tehran Science and Research Branch, Islamic Azad University , Tehran , Iran and.
authors.forename: Seyed Hojjat
authors.initials: SH
authors.lastname: Hosseini
authors.affiliation: b Zanjan Pharmaceutical Nanotechnology Research Center (ZPNRC), Zanjan University of Medical Sciences , Zanjan , Iran.
authors.forename: Aziz
authors.initials: A
authors.lastname: Maleki
authors.affiliation: a Department of Veterinary Basic Science , Tehran Science and Research Branch, Islamic Azad University , Tehran , Iran and.
authors.forename: Hamid Reza
authors.initials: HR
authors.lastname: Eshraghi
authors.affiliation: b Zanjan Pharmaceutical Nanotechnology Research Center (ZPNRC), Zanjan University of Medical Sciences , Zanjan , Iran.
authors.forename: Mehrdad
authors.initials: M
authors.lastname: Hamidi
mesh_terms: D000818:Animals; D019540:Area Under Curve; D002152:Calorimetry, Differential Scanning / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry; D065546:Drug Liberation; D008081:Liposomes / Q000737:chemistry*; D008297:Male; D046529:Microscopy, Electron, Transmission / Q000379:methods; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011239:Prednisolone / Q000031:analogs & derivatives / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008081:Liposomes; C009935:prednisolone acetate; D011239:Prednisolone
keywords: Nano-liposomes; pharmacodynamic evaluation; pharmacokinetic evaluation; prednisolone; slow-release