title: Preparation and optimization of tablets containing a self-nano-emulsifying drug delivery system loaded with rosuvastatin.
abstract: BACKGROUND
  Rosuvastatin (ROS) calcium is the latest synthetic drug in the statin group that has an anti-hyperlipidemic activity. It is available as tablets, and its poor aqueous solubility, slow dissolution rate and low-absorption extent result in less than 20% bioavailability and about 80% being excreted unchanged in the feces without absorption.
  
  
  OBJECTIVE
  To utilize nanotechnology to reformulate ROS as a self-nano-emulsifying drug delivery system (SNEDDS), and utilizing design optimization to fabricate the SNEDDS as a tablet.
  
  
  METHODS
  The solubility of ROS in different oils, surfactants and co-surfactants was tested. Pseudo-ternary phase diagrams were developed and various SNEDDS formulations were prepared and evaluated regarding globule size, self-emulsification, viscosity and transmittance. The optimized system was examined using transmission electron microscopy. The self-nano-emulsifying tablets were prepared using two types of nano-silica and different percentages of Avicel as a binder and Ac-Di-Sol as a disintegrant. The prepared tablets were evaluated for their physicochemical properties. Bioavailability in human volunteers was assessed.
  
  
  RESULTS
  A SNEDDS system was successfully developed with a droplet size range of 15 nm and a composition of 10% Labrafac, 80% Cremophore RH40 and 10% Propylene glycol. The optimized tablet formula contained: hydrophilic nano-silica, 3% Ac-Di-Sol and 30% Avicel. The pharmacokinetic study revealed that the bioavailability was enhanced by more than 2.4-fold compared with the commercially available tablet.
  
  
  CONCLUSIONS
  Tablets containing SNEDDS loaded with ROS represent a promising novel formula that has higher gastrointestinal absorption and enhanced systemic bioavailability.
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy, Beni-Suef University , Beni Suef , Egypt and.
authors.forename: Heba F
authors.initials: HF
authors.lastname: Salem
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy, Beni-Suef University , Beni Suef , Egypt and.
authors.forename: Rasha M
authors.initials: RM
authors.lastname: Kharshoum
authors.affiliation: b Department of Pharmaceutics , Faculty of Pharmacy, Nahda University , Beni Suef , Egypt.
authors.forename: Abdel Khalek A
authors.initials: AKA
authors.lastname: Halawa
authors.affiliation: b Department of Pharmaceutics , Faculty of Pharmacy, Nahda University , Beni Suef , Egypt.
authors.forename: Demiana M
authors.initials: DM
authors.lastname: Naguib
mesh_terms: D000328:Adult; D001682:Biological Availability; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D065546:Drug Liberation; D004655:Emulsions; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D000960:Hypolipidemic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use; D007700:Kinetics; D008081:Liposomes / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D000068718:Rosuvastatin Calcium / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use; D012822:Silicon Dioxide / Q000737:chemistry; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry; D013607:Tablets; D014783:Viscosity; D014867:Water / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D004655:Emulsions; D000960:Hypolipidemic Agents; D008081:Liposomes; D009821:Oils; D013501:Surface-Active Agents; D013607:Tablets; D014867:Water; D012822:Silicon Dioxide; D000068718:Rosuvastatin Calcium
keywords: Nano-silica; pharmacokinetics; pseudo ternary diagram; rosuvastatin calcium; self-nano-emulsifying system