Development and optimization of self-nanoemulsifying drug delivery system with enhanced bioavailability by Box-Behnken design and desirability function

Title
Development and optimization of self-nanoemulsifying drug delivery system with enhanced bioavailability by Box-Behnken design and desirability function
Author(s)
김종오용철순마라시니니르말엄의동포우델비자이최한곤[최한곤]
Keywords
ORAL ABSORPTION; INTESTINAL-ABSORPTION; FORMULATION APPROACH; DISSOLUTION; SOLUBILITY; RELEASE; SMEDDS; CLASSIFICATION; PERMEABILITY; GLYCERIDES
Issue Date
201212
Publisher
WILEY-BLACKWELL
Citation
JOURNAL OF PHARMACEUTICAL SCIENCES, v.101, no.12, pp.4584 - 4596
Abstract
The aim of our study was to characterize and optimize a self-nanoemulsifying drug delivery system (SNEDDS) formulation by a three-factor, three-level BoxBehnken design (BBD) combined with a desirability function. The independent factors were the amounts of Capryol PGMC (X1), Tween 20 (X2), and Transcutol HP (X3). The dependent variables were droplet size (Y1), equilibrium solubility (Y2), and cumulative percentage of drug released in 15 min (Y3) from the SNEDDS formulation. The responses were fitted to a second-order quadratic model and statistical validation of the fitted models was carried out by analysis of variance. Various response surface graphs and contour plots were constructed to understand the effects of different factor level combinations on the responses. The optimized SNEDDS formulation consisting of Capryol PGMCTween 20Transcutol HP at proportions of 5:58.4:40 (w/w) was prepared and a comparison of the predicted values and experimental values was found to be in close agreement. Furthermore, an in vivo pharmacokinetic study of the optimized SNEDDS formulation showed a 2.2-fold increase in relative oral bioavailability compared with that of the suspension. In conclusion, the BBD demonstrated its effectiveness in optimizing the SNEDDS formulation and in understanding the effects of formulation variables on the performance of SNEDDS. (c) 2012 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 101:45844596, 2012
URI
http://hdl.handle.net/YU.REPOSITORY/26807http://dx.doi.org/10.1002/jps.23333
ISSN
0022-3549
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약학대학 > 약학부 > Articles
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