title: Optimization of self-microemulsifying drug delivery system for telmisartan using Box-Behnken design and desirability function.
abstract: OBJECTIVE
  To develop and optimize the novel self-microemulsifying drug delivery system (SMEDDS) formulation for enhanced water solubility and bioavailability of telmisartan (TMS) using the Box-Behnken design (BBD) and desirability function.
  
  
  METHODS
  TMS-SMEDDS formulation consisted of the mixture of oil (Peceol), surfactant (Labrasol), co-surfactant (Transcutol), TMS and triethanolamine. A three-level BBD was applied to explore the main effect, interaction effect and quadratic effect of three independent variables, including the amount of Peceol (X1 ), Labrasol (X2 ) and Transcutol (X3 ). Determined conditions were 20 < X1  < 40, 50 < X2  < 80 and 5 < X3  < 30. The response variables were droplet size (Y1 ), polydispersity index (Y2 ) and dissolution percentage of TMS after 15 min (Y3 ).
  
  
  RESULTS
  The optimized conditions were 28.93, 80 and 28.08 (mg) for X1 , X2 and X3 , respectively, and the response variables were predicted to be 159.8 nm, 0.241 and 85.8% for Y1 , Y2 and Y3 , respectively. The actual values from the optimized formulation showed good agreement with predicted values. The optimized TMS-SMEDDS formulation showed faster drug dissolution rate and higher bioavailability than TMS powder.
  
  
  CONCLUSIONS
  Our results suggest that response surface methodology using BBD and desirability function is a promising approach to understand the effect of SMEDDS variables and to optimize the formulation.
authors.affiliation: College of Pharmacy, Yeungnam University, Gyungbuk, South Korea.
authors.forename: Hyuk Jun
authors.initials: HJ
authors.lastname: Cho
authors.forename: Dong Won
authors.initials: DW
authors.lastname: Lee
authors.forename: Nirmal
authors.initials: N
authors.lastname: Marasini
authors.forename: Bijay Kumar
authors.initials: BK
authors.lastname: Poudel
authors.forename: Jeong Hwan
authors.initials: JH
authors.lastname: Kim
authors.forename: Thiruganesh
authors.initials: T
authors.lastname: Ramasamy
authors.forename: Bong Kyu
authors.initials: BK
authors.lastname: Yoo
authors.forename: Han-Gon
authors.initials: HG
authors.lastname: Choi
authors.forename: Chul Soon
authors.initials: CS
authors.lastname: Yong
authors.forename: Jong Oh
authors.initials: JO
authors.lastname: Kim
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry; D001565:Benzoates / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D015195:Drug Design; D004355:Drug Stability; D004655:Emulsions; D005079:Excipients / Q000737:chemistry; D057230:Limit of Detection; D008297:Male; D008956:Models, Chemical; D010316:Particle Size; D044367:Phase Transition; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry; D000077333:Telmisartan
chemical_list: D001562:Benzimidazoles; D001565:Benzoates; D004337:Drug Carriers; D004655:Emulsions; D005079:Excipients; D013501:Surface-Active Agents; D000077333:Telmisartan
keywords: Box-Behnken design; bioavailability; optimization; self-microemulsifying drug delivery system; telmisartan