title: Synthesis and evaluation of mesoporous carbon/lipid bilayer nanocomposites for improved oral delivery of the poorly water-soluble drug, nimodipine.
abstract: OBJECTIVE
  A novel mesoporous carbon/lipid bilayer nanocomposite (MCLN) with a core-shell structure was synthesized and characterized as an oral drug delivery system for poorly water-soluble drugs. The objective of this study was to investigate the potential of MCLN-based formulation to modulate the in vitro release and in vivo absorption of a model drug, nimodipine (NIM).
  
  
  METHODS
  NIM-loaded MCLN was prepared by a procedure involving a combination of thin-film hydration and lyophilization. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), specific surface area analysis, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were employed to characterize the NIM-loaded MCLN formulation. The effect of MCLN on cell viability was assessed using the MTT assay. In addition, the oral bioavailability of NIM-loaded MCLN in beagle dogs was compared with that of the immediate-release formulation, Nimotop®.
  
  
  RESULTS
  Our results demonstrate that the NIM-loaded MCLN formulation exhibited a typical sustained release pattern. The NIM-loaded MCLN formulation achieved a greater degree of absorption and longer lasting plasma drug levels compared with the commercial formulation. The relative bioavailability of NIM for NIM-loaded MCLN was 214%. MCLN exhibited negligible toxicity.
  
  
  CONCLUSIONS
  The data reported herein suggest that the MCLN matrix is a promising carrier for controlling the drug release rate and improving the oral absorption of poorly water-soluble drugs.
authors.affiliation: Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical College, P.O. Box 62, No. 209, Tongshan Road, Xuzhou, 221004, China, yanzhuozhang@126.com.
authors.forename: Yanzhuo
authors.initials: Y
authors.lastname: Zhang
authors.forename: Qinfu
authors.initials: Q
authors.lastname: Zhao
authors.forename: Wufu
authors.initials: W
authors.lastname: Zhu
authors.forename: Lihua
authors.initials: L
authors.lastname: Zhang
authors.forename: Jin
authors.initials: J
authors.lastname: Han
authors.forename: Qisi
authors.initials: Q
authors.lastname: Lin
authors.forename: Fengwei
authors.initials: F
authors.lastname: Ai
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D018938:Caco-2 Cells; D002152:Calorimetry, Differential Scanning; D002244:Carbon / Q000737:chemistry*; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry; D065546:Drug Liberation; D005612:Freeze Drying; D019073:HT29 Cells; D006801:Humans; D008051:Lipid Bilayers / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D046529:Microscopy, Electron, Transmission; D008954:Models, Biological; D053761:Nanocomposites / Q000737:chemistry*; D009553:Nimodipine / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D016062:Porosity; D012995:Solubility; D013499:Surface Properties; D014867:Water / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D008051:Lipid Bilayers; D014867:Water; D009553:Nimodipine; D002244:Carbon