Optimization of self-microemulsifying drug delivery system for telmisartan using Box-Behnken design and desirability function

Cho, Hyuk Jun, Lee, Dong Won, Marasini, Nirmal, Poudel, Bijay Kumar, Kim, Jeong Hwan, Ramasamy, Thiruganesh, Yoo, Bong Kyu, Choi, Han-Gon, Yong, Chul Soon and Kim, Jong Oh (2013) Optimization of self-microemulsifying drug delivery system for telmisartan using Box-Behnken design and desirability function. Journal of Pharmacy and Pharmacology, 65 10: 1440-1450. doi:10.1111/jphp.12115


Author Cho, Hyuk Jun
Lee, Dong Won
Marasini, Nirmal
Poudel, Bijay Kumar
Kim, Jeong Hwan
Ramasamy, Thiruganesh
Yoo, Bong Kyu
Choi, Han-Gon
Yong, Chul Soon
Kim, Jong Oh
Title Optimization of self-microemulsifying drug delivery system for telmisartan using Box-Behnken design and desirability function
Journal name Journal of Pharmacy and Pharmacology   Check publisher's open access policy
ISSN 0022-3573
2042-7158
Publication date 2013-10
Sub-type Article (original research)
DOI 10.1111/jphp.12115
Open Access Status Not Open Access
Volume 65
Issue 10
Start page 1440
End page 1450
Total pages 11
Place of publication Chichester, West Sussex United Kingdom
Publisher John Wiley & Sons
Language eng
Formatted abstract
Objectives
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.

Method
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).

Key findings
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.
Keyword Bioavailability
Box-Behnken design
Optimization
Self-microemulsifying drug delivery system
Telmisartan
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Article (original research)
Collection: School of Chemistry and Molecular Biosciences
 
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Created: Sat, 04 Jun 2016, 12:26:19 EST by Nirmal Marasini on behalf of School of Chemistry & Molecular Biosciences