title: Nanosponge-based pediatric-controlled release dry suspension of Gabapentin for reconstitution.
abstract: BACKGROUND
  Gabapentin was selected to formulate oral controlled release dry suspension because of short biological half life of 5-7 h and low bioavailability (60%). Gabapentin is a bitter drug so an attempt was made to mask its taste.
  
  
  OBJECTIVE
  To formulate and evaluate controlled release dry suspension for reconstitution to increase the bioavailability and to control bitter taste of drug.
  
  
  METHODS
  Cyclodextrin based nanosponges were synthesized by previously reported melt method. The nanosponge-drug complexes were characterized by FTIR, DSC and PXRD as well as evaluated for taste and saturation solubility. The complexes were coated on Espheres by a suspension layering technique followed by coating with ethyl cellulose and Eudragit RS-100. A dry powder suspension for reconstitution of the microspheres was formulated and evaluated for taste, redispersibility, in vitro dissolution, sedimentation volume, leaching and pharmacokinetics.
  
  
  CONCLUSIONS
  The complexes showed partial entrapment of drug nanocavities. Significant decrease in solubility (25%) was observed in the complexes than pure drug in different media. The microspheres of nanosponge complexes showed desired controlled release profile for 12 h. Insignificant drug leaching was observed in reconstituted suspension during storage for 7 days at 45 °C/75% RH. Nanosponges effectively masked the taste of Gabapentin and the coating polymers provided controlled release of the drug and enhanced taste masking. The results of in vivo studies showed increase in bioavailability of controlled release suspension by 24.09% as compared to pure drug.
  
  
  CONCLUSIONS
  The dry powder suspension loaded with microspheres of nanosponges complexes can be proposed as a suitable controlled release drug delivery for Gabapentin.
authors.affiliation: a Department of Pharmaceutics , AISSMS College of Pharmacy , Pune , India.
authors.forename: Monica R P
authors.initials: MR
authors.lastname: Rao
authors.affiliation: a Department of Pharmaceutics , AISSMS College of Pharmacy , Pune , India.
authors.forename: Rohini C
authors.initials: RC
authors.lastname: Bhingole
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000588:Amines / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D002626:Chemistry, Pharmaceutical; D003509:Cyclohexanecarboxylic Acids / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D000077206:Gabapentin; D006801:Humans; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D013535:Suspensions; D013649:Taste / Q000187:drug effects / Q000502:physiology; D014961:X-Ray Diffraction; D055815:Young Adult; D005680:gamma-Aminobutyric Acid / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D000588:Amines; D003509:Cyclohexanecarboxylic Acids; D003692:Delayed-Action Preparations; D013535:Suspensions; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin
keywords: Ethyl cellulose; Eudragit RS-100; Gabapentin; nanosponges; pan coating; taste masking