title: Implementation of mixture design for formulation of albumin containing enteric-coated spray-dried microparticles.
abstract: BACKGROUND
  Oral delivery of proteins has been a challenging as well as rapidly developing field.
  
  
  OBJECTIVE
  To implement mixture design of experiment to develop enteric-coated microparticles containing bovine serum albumin.
  
  
  METHODS
  Microparticles were prepared using Buchi Spray Dryer 191. Simplex lattice mixture design computed using JMP software was implemented to compare the gastric protection rendered by Eudragit FS30D, Eudragit L100-55, and Eudragit S100 in microparticulate form. Further, an extreme vertices mixture design was used to incorporate hydroxypropyl methylcellulose (HPMC) Chitosan in the formulation to delay the release. Microparticle recovery yield and protein content in microparticles were evaluated.
  
  
  CONCLUSIONS
  The design was statistically significant with Eudragit S100 resulting in protein release of < 5% in acidic buffer. The selected optimal formulation had 70% of Eudragit S, 25% HPMC, and 5% Chitosan. The release profiles of protein from Eudragit S alone and along with HPMC were compared. About 25% decrease in the amount of protein release was observed 6 h post exposure of microparticle to buffer of pH 6.8. The microparticle recovery yield reduced from 77.99% to 71.56% which is due to addition of HPMC into the formulation matrix.
  
  
  CONCLUSIONS
  Although all three Eudragit polymers can be used for enteric coating, in the microparticulate form Eudragit S resulted in higher gastric protection. Also use of HPMC along with Eudragit S resulted in further sustained release.
authors.affiliation: Mercer University, Nanotechnology Laboratory, College of Pharmacy and Health Sciences, Atlanta, GA 30341, USA.
authors.forename: Prathap Nagaraja
authors.initials: PN
authors.lastname: Shastri
authors.forename: Ruhi V
authors.initials: RV
authors.lastname: Ubale
authors.forename: Martin J
authors.initials: MJ
authors.lastname: D'Souza
mesh_terms: D000180:Acrylic Resins / Q000008:administration & dosage / Q000737:chemistry*; D000418:Albumins / Q000008:administration & dosage*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D016503:Drug Delivery Systems; D006863:Hydrogen-Ion Concentration; D008863:Microspheres; D010316:Particle Size; D011109:Polymethacrylic Acids / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility
chemical_list: D000180:Acrylic Resins; D000418:Albumins; D004337:Drug Carriers; C446821:Eudragit L100-55; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer