title: A Multi-layered Particulate System for Desvenlafaxine Succinate Oral Customized Release.
abstract: BACKGROUND
  With its reported side effects Desvenlafaxine succinate (DSV) is a good candidate to prepare prolonged release system. Such prolonged release could decrease the rapid DSV absorption after oral administration and reduce its exaggerated side effects.
  
  
  METHODS
  A prolonged release Desvenlafaxine succinate (DSV) multilayered system was prepared by ionotropic gelation using sodium alginate (SA) and calcium chloride as a cross-linker. DSV was incorporated simultaneously during the gelation stage and the formed beads were evaluated for shape and particle size. Thirteen formulation variables including pH, DSV: polymer ratio, cross-linker concentration and curing time were optimized for optimal drug entrapment. The optimized formula was evaluated ex vivo using the everted sac technique to predict DSV absorption through intestinal mucosal cells, follow the permeation and calculate its apparent permeability coefficient.
  
  
  RESULTS
  The optimum formulation variables were: pH (8-9), DSV: SA ratio (2:1), cross-linker concentration (5%w/v) and 30 min curing time. Multilayered beads coating using chitosan and SA was compared with uncoated beads or the innovator for DSV release. Coating of the beads greatly retarded DSV release with a release profile similar to that of the innovator. An optimized formula (T13) coated with 0.04% w/v of each of chitosan and SA was selected. The developed system gave rise to a prolonged release pattern with high similarity factor with the innovator.
  
  
  CONCLUSIONS
  The results of the current work can be applied to prepare controlled release systems of similar drugs that have intense side effects associated with their initial burst after oral administration.
authors.affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Egypt.
authors.forename: Nazik
authors.initials: N
authors.lastname: Elgindy
authors.affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Egypt.
authors.forename: Ayman
authors.initials: A
authors.lastname: Elnoby
authors.affiliation: Faculty of Pharmacy, Alexandria University, Egypt Pharmacology and Toxicology, Alexandria, Egypt.
authors.forename: Hanan M
authors.initials: HM
authors.lastname: El-Gowelli
authors.affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Egypt.
authors.forename: Wael
authors.initials: W
authors.lastname: Samy
mesh_terms: D000284:Administration, Oral; D000464:Alginates; D002626:Chemistry, Pharmaceutical; D048271:Chitosan; D000069468:Desvenlafaxine Succinate / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D005079:Excipients; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D010316:Particle Size
chemical_list: D000464:Alginates; D004337:Drug Carriers; D005079:Excipients; D006603:Hexuronic Acids; D020723:Glucuronic Acid; D048271:Chitosan; D000069468:Desvenlafaxine Succinate
keywords: Desvenlafaxine succinate; everted sac; ionotropic gelation; permeability coefficient